PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 34668334-2 2022 This study aimed to investigate an IVIVE for intestinal P-glycoprotein (Pgp, ABCB1)-mediated DDIs between three Pgp substrates, digoxin, dabigatran etexilate and quinidine, and two Pgp inhibitors, itraconazole and verapamil, via PBPK modeling. Itraconazole 197-209 ATP binding cassette subfamily B member 1 Homo sapiens 56-70 34668334-2 2022 This study aimed to investigate an IVIVE for intestinal P-glycoprotein (Pgp, ABCB1)-mediated DDIs between three Pgp substrates, digoxin, dabigatran etexilate and quinidine, and two Pgp inhibitors, itraconazole and verapamil, via PBPK modeling. Itraconazole 197-209 ATP binding cassette subfamily B member 1 Homo sapiens 72-75 34668334-2 2022 This study aimed to investigate an IVIVE for intestinal P-glycoprotein (Pgp, ABCB1)-mediated DDIs between three Pgp substrates, digoxin, dabigatran etexilate and quinidine, and two Pgp inhibitors, itraconazole and verapamil, via PBPK modeling. Itraconazole 197-209 ATP binding cassette subfamily B member 1 Homo sapiens 77-82 34668334-2 2022 This study aimed to investigate an IVIVE for intestinal P-glycoprotein (Pgp, ABCB1)-mediated DDIs between three Pgp substrates, digoxin, dabigatran etexilate and quinidine, and two Pgp inhibitors, itraconazole and verapamil, via PBPK modeling. Itraconazole 197-209 ATP binding cassette subfamily B member 1 Homo sapiens 181-184 34668334-4 2022 For Pgp inhibitors, PBPK models utilized the reported in vitro values of Pgp inhibition constants (Ki ), 1.0 muM for itraconazole and 2.0 muM for verapamil. Itraconazole 117-129 ATP binding cassette subfamily B member 1 Homo sapiens 73-76 34620694-6 2022 Three sensitive substrates were identified: avapritinib (CYP3A), lonafarnib (CYP3A), and relugolix (P-gp), with AUCRs of 7.00, 5.07, and 6.25 when co-administered with itraconazole, ketoconazole, and erythromycin, respectively. Itraconazole 168-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-62 34620694-6 2022 Three sensitive substrates were identified: avapritinib (CYP3A), lonafarnib (CYP3A), and relugolix (P-gp), with AUCRs of 7.00, 5.07, and 6.25 when co-administered with itraconazole, ketoconazole, and erythromycin, respectively. Itraconazole 168-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-82 34620694-6 2022 Three sensitive substrates were identified: avapritinib (CYP3A), lonafarnib (CYP3A), and relugolix (P-gp), with AUCRs of 7.00, 5.07, and 6.25 when co-administered with itraconazole, ketoconazole, and erythromycin, respectively. Itraconazole 168-180 phosphoglycolate phosphatase Homo sapiens 100-104 34716565-2 2022 These studies aimed to assess the pharmacokinetics of BI 425809, a potent glycine-transporter-1 inhibitor, when co-administered with a strong cytochrome P450 3A4 (CYP3A4) inhibitor (itraconazole) and inducer (rifampicin). Itraconazole 182-194 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 142-161 34716565-2 2022 These studies aimed to assess the pharmacokinetics of BI 425809, a potent glycine-transporter-1 inhibitor, when co-administered with a strong cytochrome P450 3A4 (CYP3A4) inhibitor (itraconazole) and inducer (rifampicin). Itraconazole 182-194 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 163-169 34495458-5 2021 The initial model based on in vitro-in vivo extrapolation was refined using sensitivity analysis and non-linear mixed effects modeling to optimize parameter estimates and to improve model fit to data from a clinical drug-drug interaction study with the strong CYP3A4 inhibitor, itraconazole. Itraconazole 278-290 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 260-266 34959655-8 2021 In the in vivo study that was carried out in rats, the AUC0-48h of the commercial formulation, Sporanox , was 1073.9 +- 314.7 ng h mL-1, and the bioavailability of the SD pellet (2969.7 +- 720.6 ng h mL-1) was three-fold higher than that of Sporanox (*** p < 0.001). Itraconazole 95-103 L1 cell adhesion molecule Mus musculus 131-135 34664792-3 2021 Phenotyping studies indicated cytochrome P450 (CYP) 3A are the major CYP isoform responsible for zanubrutinib metabolism, which was confirmed by a clinical DDI study with itraconazole and rifampin. Itraconazole 171-183 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-54 34426442-0 2021 Pharmacokinetics, Safety, and Efficacy of Trastuzumab Deruxtecan With Concomitant Ritonavir or Itraconazole in Patients With HER2-Expressing Advanced Solid Tumors. Itraconazole 95-107 erb-b2 receptor tyrosine kinase 2 Homo sapiens 125-129 34426442-1 2021 PURPOSE: To evaluate drug-drug interactions between the HER2-targeted antibody-drug conjugate trastuzumab deruxtecan (T-DXd; DS-8201a) and the OATP1B/CYP3A inhibitor ritonavir or the strong CYP3A inhibitor itraconazole. Itraconazole 206-218 erb-b2 receptor tyrosine kinase 2 Homo sapiens 56-60 34426442-1 2021 PURPOSE: To evaluate drug-drug interactions between the HER2-targeted antibody-drug conjugate trastuzumab deruxtecan (T-DXd; DS-8201a) and the OATP1B/CYP3A inhibitor ritonavir or the strong CYP3A inhibitor itraconazole. Itraconazole 206-218 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 190-195 34160163-9 2021 Among oral antifungals, the mean MIC of itraconazole was within the range (0.84 (0.252) mug/ mL), whereas high mean MIC values were reported for terbinafine (0.05 (0.043) mug/mL). Itraconazole 40-52 thrombopoietin Mus musculus 93-95 34589147-0 2021 Itraconazole improves survival outcomes in patients with colon cancer by inducing autophagic cell death and inhibiting transketolase expression. Itraconazole 0-12 transketolase Homo sapiens 119-132 34589147-10 2021 Notably, itraconazole induced autophagy by enhancing LC3B and p62 expression. Itraconazole 9-21 microtubule associated protein 1 light chain 3 beta Homo sapiens 53-57 34589147-10 2021 Notably, itraconazole induced autophagy by enhancing LC3B and p62 expression. Itraconazole 9-21 nucleoporin 62 Homo sapiens 62-65 34498807-2 2022 Three drug-drug interactions studies were conducted in healthy subjects to evaluate the effect of P-glycoprotein (P-gp) modulation (Study 1: P-gp inhibition by itraconazole; Study 2: P-gp induction by rifampin) on filgotinib pharmacokinetics and the potential of filgotinib to impact exposure of metformin, an organic cation transporter (OCT) 2 and multidrug and toxin extrusion (MATE) 1/2K substrate (Study 3). Itraconazole 160-172 ATP binding cassette subfamily B member 1 Homo sapiens 141-145 34260894-11 2021 Model-based simulations of dose staggering predicted the maximum inhibition of P-gp when DABE microdose was concomitantly administered with itraconazole solution; simulations also highlighted dosing intervals required to minimise the DDI risk depending on the DABE dose administered (microdose vs. therapeutic). Itraconazole 140-152 ATP binding cassette subfamily B member 1 Homo sapiens 79-83 34376577-0 2021 Itraconazole Exerts its Anti-Tumor Effect in Esophageal Cancer by Suppressing the HER2/AKT Signaling Pathway. Itraconazole 0-12 erb-b2 receptor tyrosine kinase 2 Mus musculus 82-86 34376577-0 2021 Itraconazole Exerts its Anti-Tumor Effect in Esophageal Cancer by Suppressing the HER2/AKT Signaling Pathway. Itraconazole 0-12 thymoma viral proto-oncogene 1 Mus musculus 87-90 34376577-4 2021 Using an unbiased kinase array, we found that itraconazole downregulated protein kinase AKT phosphorylation in OE33 esophageal adenocarcinoma cells. Itraconazole 46-58 AKT serine/threonine kinase 1 Homo sapiens 88-91 34376577-5 2021 Itraconazole also decreased phosphorylation of downstream ribosomal protein S6, transcriptional expression of the upstream receptor tyrosine kinase HER2, and phosphorylation of upstream PI3K in esophageal cancer cells. Itraconazole 0-12 ribosomal protein S6 Mus musculus 58-78 34376577-5 2021 Itraconazole also decreased phosphorylation of downstream ribosomal protein S6, transcriptional expression of the upstream receptor tyrosine kinase HER2, and phosphorylation of upstream PI3K in esophageal cancer cells. Itraconazole 0-12 erb-b2 receptor tyrosine kinase 2 Homo sapiens 148-152 34376577-8 2021 HER2 total protein and phosphorylation of AKT and S6 proteins were decreased in xenografts from itraconazole-treated mice compared to xenografts from placebo-treated mice. Itraconazole 96-108 erb-b2 receptor tyrosine kinase 2 Mus musculus 0-4 34376577-8 2021 HER2 total protein and phosphorylation of AKT and S6 proteins were decreased in xenografts from itraconazole-treated mice compared to xenografts from placebo-treated mice. Itraconazole 96-108 thymoma viral proto-oncogene 1 Mus musculus 42-45 34376577-9 2021 In an early phase I clinical trial (NCT02749513) in esophageal cancer patients, itraconazole decreased HER2 total protein expression and phosphorylation of AKT and S6 proteins in tumors. Itraconazole 80-92 erb-b2 receptor tyrosine kinase 2 Homo sapiens 103-107 34376577-9 2021 In an early phase I clinical trial (NCT02749513) in esophageal cancer patients, itraconazole decreased HER2 total protein expression and phosphorylation of AKT and S6 proteins in tumors. Itraconazole 80-92 AKT serine/threonine kinase 1 Homo sapiens 156-159 34376577-10 2021 These data demonstrate that itraconazole has potent anti-tumor properties in esophageal cancer, partially through blockade of HER2/AKT signaling. Itraconazole 28-40 erb-b2 receptor tyrosine kinase 2 Homo sapiens 126-130 34376577-10 2021 These data demonstrate that itraconazole has potent anti-tumor properties in esophageal cancer, partially through blockade of HER2/AKT signaling. Itraconazole 28-40 AKT serine/threonine kinase 1 Homo sapiens 131-134 34627431-8 2021 The protein levels of SMO and Glil were significantly down-regulated after treated by arsenic disulfide and itraconazole alone(P<0.01). Itraconazole 108-120 smoothened, frizzled class receptor Homo sapiens 22-25 34627431-11 2021 In addition, the combination of AS2S2 and itraconazole show a synergistic effects, which may be related with the down-regulated protein expression of SMO and Glil of Hedgehog signaling pathway. Itraconazole 42-54 smoothened, frizzled class receptor Homo sapiens 150-153 34480080-5 2021 Hh signalling appeared necessary to sustain cell growth, as SHH ligand depletion with Robotikinin or SMO inhibition, either with chemical inhibitors (Itraconazole or LDE-225) or SMO-specific siRNA, attenuated GLI1 activity and cell proliferation in both monolayer and organotypic raft culture. Itraconazole 150-162 sonic hedgehog signaling molecule Homo sapiens 60-63 34480080-5 2021 Hh signalling appeared necessary to sustain cell growth, as SHH ligand depletion with Robotikinin or SMO inhibition, either with chemical inhibitors (Itraconazole or LDE-225) or SMO-specific siRNA, attenuated GLI1 activity and cell proliferation in both monolayer and organotypic raft culture. Itraconazole 150-162 GLI family zinc finger 1 Homo sapiens 209-213 31290765-11 2021 Esophageal SHH levels were lower in itraconazole vs control (P = 0.12). Itraconazole 36-48 sonic hedgehog signaling molecule Homo sapiens 11-14 34429859-4 2021 Here, we report that the antifungal compound itraconazole (ICZ), but not its main metabolite hydroxy-ICZ or ketoconazole, disrupts the binding of Rab7 to ORP3-VAP-A complexes, leading to inhibition of EV-mediated pro-metastatic morphological changes including cell migration behaviour of colon cancer cells. Itraconazole 45-57 RAB7B, member RAS oncogene family Homo sapiens 146-150 34429859-4 2021 Here, we report that the antifungal compound itraconazole (ICZ), but not its main metabolite hydroxy-ICZ or ketoconazole, disrupts the binding of Rab7 to ORP3-VAP-A complexes, leading to inhibition of EV-mediated pro-metastatic morphological changes including cell migration behaviour of colon cancer cells. Itraconazole 45-57 oxysterol binding protein like 3 Homo sapiens 154-158 34429859-4 2021 Here, we report that the antifungal compound itraconazole (ICZ), but not its main metabolite hydroxy-ICZ or ketoconazole, disrupts the binding of Rab7 to ORP3-VAP-A complexes, leading to inhibition of EV-mediated pro-metastatic morphological changes including cell migration behaviour of colon cancer cells. Itraconazole 45-57 VAMP associated protein A Homo sapiens 159-164 34429859-4 2021 Here, we report that the antifungal compound itraconazole (ICZ), but not its main metabolite hydroxy-ICZ or ketoconazole, disrupts the binding of Rab7 to ORP3-VAP-A complexes, leading to inhibition of EV-mediated pro-metastatic morphological changes including cell migration behaviour of colon cancer cells. Itraconazole 59-62 RAB7B, member RAS oncogene family Homo sapiens 146-150 34429859-4 2021 Here, we report that the antifungal compound itraconazole (ICZ), but not its main metabolite hydroxy-ICZ or ketoconazole, disrupts the binding of Rab7 to ORP3-VAP-A complexes, leading to inhibition of EV-mediated pro-metastatic morphological changes including cell migration behaviour of colon cancer cells. Itraconazole 59-62 oxysterol binding protein like 3 Homo sapiens 154-158 34429859-4 2021 Here, we report that the antifungal compound itraconazole (ICZ), but not its main metabolite hydroxy-ICZ or ketoconazole, disrupts the binding of Rab7 to ORP3-VAP-A complexes, leading to inhibition of EV-mediated pro-metastatic morphological changes including cell migration behaviour of colon cancer cells. Itraconazole 59-62 VAMP associated protein A Homo sapiens 159-164 34140765-2 2021 This study aimed to evaluate the impact of the strong CYP3A4 inhibitor itraconazole on the safety and pharmacokinetics of pyrotinib in Chinese healthy adults. Itraconazole 71-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-60 34475046-6 2021 The 12/15-lipoxygenase inhibitor, which is involved in the conversion of 18-hydroxy-eicosapentaenoic acid to resolvin E3, attenuated the inhibitory effect of itraconazole. Itraconazole 158-170 arachidonate 15-lipoxygenase Homo sapiens 4-22 34145979-2 2021 A phase 1 open-label, 2-period, fixed-sequence, 2-part study (NCT03928327) characterized effects of a strong CYP3A4 inhibitor (itraconazole) and inducer (rifampin) on the pharmacokinetics (PK) of mobocertinib and its active metabolites, AP32960 and AP32914. Itraconazole 127-139 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 109-115 34145979-6 2021 Based on these results, the strong CYP3A inhibitor itraconazole and inducer rifampin significantly influenced the PK of mobocertinib and its active metabolites. Itraconazole 51-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-40 34267345-0 2022 Itraconazole and rifampicin, as CYP3A modulators but not P-gp modulators, affect the pharmacokinetics of almonertinib and active metabolite HAS-719 in healthy volunteers. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-37 34267345-3 2022 In this study, we investigated the effects of CYP3A inhibitor itraconazole and CYP3A inducer rifampicin on the pharmacokinetics of almonertinib and HAS-719 in 64 healthy volunteers. Itraconazole 62-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-51 31290765-13 2021 CONCLUSION: Itraconazole significantly decreases EAC development and SHH expression in a preclinical animal model of BM. Itraconazole 12-24 sonic hedgehog signaling molecule Homo sapiens 69-72 35218073-6 2022 Fosravuconazole is a novel broad-spectrum azole and a moderate inhibitor of Cyp3A4 that causes fewer drug interactions than itraconazole and voriconazole, indicating a promising drug for this disease. Itraconazole 124-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 35094205-0 2022 Itraconazole-Induced the Activation of Adenosine 5"-Monophosphate (Amp)-Activated Protein Kinase Inhibits Tumor Growth of Melanoma via Inhibiting ERK Signaling. Itraconazole 0-12 mitogen-activated protein kinase 1 Homo sapiens 146-149 35094205-3 2022 This work investigated the function of itraconazole-induced 5"-monophosphate (AMP)-activated protein kinase alpha (AMPKalpha) in melanoma progression through ERK signaling. Itraconazole 39-51 mitogen-activated protein kinase 1 Homo sapiens 158-161 35094205-11 2022 Itraconazole activated AMPK signaling and inhibited ERK signaling in melanoma cells. Itraconazole 0-12 protein kinase AMP-activated catalytic subunit alpha 2 Homo sapiens 23-27 35094205-11 2022 Itraconazole activated AMPK signaling and inhibited ERK signaling in melanoma cells. Itraconazole 0-12 mitogen-activated protein kinase 1 Homo sapiens 52-55 35094205-12 2022 Activation of ERK signaling reversed the effect of itraconazole on cellular process in melanoma. Itraconazole 51-63 mitogen-activated protein kinase 1 Homo sapiens 14-17 35094205-13 2022 Moreover, itraconazole-induced AMPKalpha inhibited melanoma tumor growth in vivo by inhibiting ERK signaling. Itraconazole 10-22 mitogen-activated protein kinase 1 Homo sapiens 95-98 35094205-14 2022 Itraconazole-induced AMPKalpha inhibits the progression of melanoma by inhibition of ERK signaling. Itraconazole 0-12 mitogen-activated protein kinase 1 Homo sapiens 85-88 35616006-4 2022 Asciminib exposure (area under the curve (AUC)) unexpectedly decreased by ~40% when administered concomitantly with the strong CYP3A inhibitor itraconazole oral solution, whereas maximum plasma concentration (Cmax ) decreased by ~50%. Itraconazole 143-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-132 35605912-3 2022 Then two clinical studies were performed to investigate the effects of itraconazole and rifampicin (potent CYP3A4/5 inhibitor and inducer, respectively) on the pharmacokinetics of youkenafil and its main metabolite, N-desethyl youkenafil (M1). Itraconazole 71-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-115 35246464-3 2022 The use of 3 microM itraconazole was successfully validated for estimation of fm,CYP3A4 by demonstration of fm values within a 2-fold of in vivo estimates for 10 out of 13 CYP3A4 substrates in a reference set of marketed drugs. Itraconazole 20-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 35344780-8 2022 The interference of CYP3A modulators itraconazole and rifampicin with the analytes, and the mutual interference between the analytes were also investigated producing acceptable results. Itraconazole 37-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-25 35517785-8 2022 Reduced cyclin D1 protein levels were consistent with G0/G1 phase arrest, especially when resulting from the combination of ITZ with rapamycin. Itraconazole 124-127 cyclin D1 Homo sapiens 8-17 35389533-0 2022 Cytochrome P450 reaction phenotyping of itraconazole hydroxylation in the dog. Itraconazole 40-52 Cytochrome P450 1A1 Canis lupus familiaris 0-15 35389533-6 2022 In rCYP experiments, CYP2D15 and CYP3A12 had highest activity for ITZ hydroxylation. Itraconazole 66-69 cytochrome P450 2D15 Canis lupus familiaris 21-28 35389533-6 2022 In rCYP experiments, CYP2D15 and CYP3A12 had highest activity for ITZ hydroxylation. Itraconazole 66-69 cytochrome P450 3A12 Canis lupus familiaris 33-40 35389533-7 2022 In inhibitor experiments, quinidine and erythromycin inhibited ITZ hydroxylation in CYP2D15 and CYP3A12, respectively, in an isoform-specific manner. Itraconazole 63-66 cytochrome P450 2D15 Canis lupus familiaris 84-91 35389533-7 2022 In inhibitor experiments, quinidine and erythromycin inhibited ITZ hydroxylation in CYP2D15 and CYP3A12, respectively, in an isoform-specific manner. Itraconazole 63-66 cytochrome P450 3A12 Canis lupus familiaris 96-103 35389533-10 2022 These findings support a role for CYP2D15 and CYP3A12 in ITZ biotransformation in canine liver. Itraconazole 57-60 cytochrome P450 2D15 Canis lupus familiaris 34-41 35389533-10 2022 These findings support a role for CYP2D15 and CYP3A12 in ITZ biotransformation in canine liver. Itraconazole 57-60 cytochrome P450 3A12 Canis lupus familiaris 46-53 35165925-1 2022 AIMS: Clinical drug interaction studies with itraconazole and rifampicin demonstrated acalabrutinib is a sensitive substrate of CYP3A. Itraconazole 45-57 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-133 35247290-1 2022 This phase 1, open-label study evaluated the effect of food and administration of the cytochrome P450 3A4 and P-glycoprotein inhibitor itraconazole (ITZ) on the pharmacokinetics of AMG 986. Itraconazole 135-147 ATP binding cassette subfamily B member 1 Homo sapiens 110-124 35247290-1 2022 This phase 1, open-label study evaluated the effect of food and administration of the cytochrome P450 3A4 and P-glycoprotein inhibitor itraconazole (ITZ) on the pharmacokinetics of AMG 986. Itraconazole 149-152 ATP binding cassette subfamily B member 1 Homo sapiens 110-124 35242038-0 2022 Itraconazole Inhibits the Growth of Cutaneous Squamous Cell Carcinoma by Targeting HMGCS1/ACSL4 Axis. Itraconazole 0-12 3-hydroxy-3-methylglutaryl-Coenzyme A synthase 1 Mus musculus 83-89 35242038-0 2022 Itraconazole Inhibits the Growth of Cutaneous Squamous Cell Carcinoma by Targeting HMGCS1/ACSL4 Axis. Itraconazole 0-12 acyl-CoA synthetase long-chain family member 4 Mus musculus 90-95 35242038-12 2022 An integrated analysis of transcriptomic and proteomic analyses identified that 3-hydroxy-3-methylglutaryl-CoA synthase 1 (HMGCS1) and acyl-CoA synthetase long-chain family member 4 (ACSL4) were significantly upregulated in A431 cells treated with itraconazole. Itraconazole 248-260 3-hydroxy-3-methylglutaryl-Coenzyme A synthase 1 Mus musculus 123-129 35242038-12 2022 An integrated analysis of transcriptomic and proteomic analyses identified that 3-hydroxy-3-methylglutaryl-CoA synthase 1 (HMGCS1) and acyl-CoA synthetase long-chain family member 4 (ACSL4) were significantly upregulated in A431 cells treated with itraconazole. Itraconazole 248-260 acyl-CoA synthetase long-chain family member 4 Mus musculus 135-181 35242038-13 2022 HMGCS1 silencing reversed the antiproliferative activity of itraconazole in A431 cells. Itraconazole 60-72 3-hydroxy-3-methylglutaryl-Coenzyme A synthase 1 Mus musculus 0-6 35242038-14 2022 Dual-luciferase assay showed that itraconazole could promote HMGCS1 transcription. Itraconazole 34-46 3-hydroxy-3-methylglutaryl-Coenzyme A synthase 1 Mus musculus 61-67 35242038-18 2022 Conclusion: We proved itraconazole inhibits the growth of cSCC by regulating HMGCS1/ACSL4 axis. Itraconazole 22-34 3-hydroxy-3-methylglutaryl-Coenzyme A synthase 1 Mus musculus 77-83 35242038-18 2022 Conclusion: We proved itraconazole inhibits the growth of cSCC by regulating HMGCS1/ACSL4 axis. Itraconazole 22-34 acyl-CoA synthetase long-chain family member 4 Mus musculus 84-89 35350119-4 2022 The addition of insulin or glucose at physiologic levels in RPMI medium alone altered the MIC in either a positive or negative fashion, depending on the organisms and drug tested, with C. glabrata most significantly altered with a 40, >32- and 46-fold increase in MIC for amphotericin B, itraconazole and miconazole, respectively. Itraconazole 288-300 insulin Homo sapiens 16-23 34989180-3 2022 This phase 1, fixed-sequence, open-label, crossover trial (ClinicalTrials.gov identifier NCT03173170) investigated the effect of itraconazole, a potent CYP3A4 inhibitor, on felcisetrag pharmacokinetics in healthy adults. Itraconazole 129-141 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 152-158 35370263-2 2022 An antifungal agent, itraconazole (ITCZ), that has antimicrobial activity against Aspergillus species, is used as a prophylactic agent against Aspergillus infection after LT. ITCZ and its metabolite, hydroxyitraconazole (OH-ITCZ), potently inhibit CYP3A and P-glycoprotein that metabolize or excrete calcineurin inhibitors (CNIs), which are the first-line immunosuppressants used after LT; thus, concomitant use of ITCZ and CNIs could induce an increase in the blood concentration of CNIs. Itraconazole 21-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 248-253 35370263-2 2022 An antifungal agent, itraconazole (ITCZ), that has antimicrobial activity against Aspergillus species, is used as a prophylactic agent against Aspergillus infection after LT. ITCZ and its metabolite, hydroxyitraconazole (OH-ITCZ), potently inhibit CYP3A and P-glycoprotein that metabolize or excrete calcineurin inhibitors (CNIs), which are the first-line immunosuppressants used after LT; thus, concomitant use of ITCZ and CNIs could induce an increase in the blood concentration of CNIs. Itraconazole 35-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 248-253 3030012-10 1987 The interaction with mammalian cytochrome P-450 decreases from miconazole greater than ketoconazole much greater than itraconazole and is much weaker than the interaction of the antimycotics with yeast cytochrome P-450. Itraconazole 118-130 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 31-47 2560935-1 1989 The effect of novel azole derivatives (itraconazole and fluconazole) on 5-lipoxygenase activity was examined using human polymorphonuclear leukocytes (PMNL) as the enzyme source. Itraconazole 39-51 arachidonate 5-lipoxygenase Homo sapiens 72-86 2560935-2 1989 The novel imidazole derivative itraconazole proved to be a potent inhibitor (IC50 2 X 10(-6) M) of 5-lipoxygenase activity. Itraconazole 31-43 arachidonate 5-lipoxygenase Homo sapiens 99-113 2850750-7 1988 The choice of itraconazole--with its improved tissue affinity, its lower therapeutic dose requirements, and its increased selectivity for fungal cytochrome P-450--demonstrates very well that the use of animal and human pharmacology helps in the design of an antifungal drug with as much effect as possible on the fungus and as little effect as possible on the host. Itraconazole 14-26 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 145-161 33201347-1 2021 PURPOSE: The antifungal drugs ketoconazole and itraconazole reduce serum concentrations of 4beta-hydroxycholesterol, which is a validated marker for hepatic cytochrome P450 (CYP) 3A4 activity. Itraconazole 47-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 157-182 33826998-8 2021 In conclusion, itraconazole has unique characteristics that are distinct from those shared by the other azole anti-fungal drugs ketoconazole, voriconazole, and fluconazole with regard to the influence of genetic variations on the inhibition of CYP3A4. Itraconazole 15-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 244-250 33387374-2 2021 Previous studies have reported that nadolol is a substrate of P-glycoprotein, and the coadministration with itraconazole, a typical P-glycoprotein inhibitor, results in elevated plasma concentrations and cumulative urinary excretion of nadolol. Itraconazole 108-120 ATP binding cassette subfamily B member 1 Homo sapiens 62-76 33387374-2 2021 Previous studies have reported that nadolol is a substrate of P-glycoprotein, and the coadministration with itraconazole, a typical P-glycoprotein inhibitor, results in elevated plasma concentrations and cumulative urinary excretion of nadolol. Itraconazole 108-120 ATP binding cassette subfamily B member 1 Homo sapiens 132-146 33387374-7 2021 In the drug interactions of nadolol with itraconazole, rifampicin, a well-known P-glycoprotein inducer, or grapefruit juice, there were significant correlations between the differences in AUC0-48 and those in Ae, 0-48 from the controls in individual subjects. Itraconazole 41-53 ATP binding cassette subfamily B member 1 Homo sapiens 80-94 34049965-2 2021 Ipatasertib was metabolized by CYP3A4 to its major metabolite, M1 (G-037720), and was a P-gp substrate and OATP1B1/1B3 inhibitor in vitro A Phase I drug-drug interaction (DDI) study (n=15) was conducted in healthy subjects to evaluate the effect of itraconazole (200 mg solution QD, 4 days), a strong CYP3A4 and P-gp inhibitor, on pharmacokinetics of ipatasertib (100 mg single dose). Itraconazole 249-261 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 33964991-4 2021 We thus conducted this study to investigate the effect of itraconazole (ICZ), a strong inhibitor of CYP3A and a moderate inhibitor of P-gp, on the pharmacokinetics (PK) of FDV. Itraconazole 58-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-105 33964991-4 2021 We thus conducted this study to investigate the effect of itraconazole (ICZ), a strong inhibitor of CYP3A and a moderate inhibitor of P-gp, on the pharmacokinetics (PK) of FDV. Itraconazole 58-70 phosphoglycolate phosphatase Homo sapiens 134-138 33964991-4 2021 We thus conducted this study to investigate the effect of itraconazole (ICZ), a strong inhibitor of CYP3A and a moderate inhibitor of P-gp, on the pharmacokinetics (PK) of FDV. Itraconazole 72-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-105 33964991-4 2021 We thus conducted this study to investigate the effect of itraconazole (ICZ), a strong inhibitor of CYP3A and a moderate inhibitor of P-gp, on the pharmacokinetics (PK) of FDV. Itraconazole 72-75 phosphoglycolate phosphatase Homo sapiens 134-138 33665257-4 2021 Also, we evaluated the inhibitory effect of itraconazole on P-gp using specific in vivo biodistribution through 99mTc-MIBI uptake. Itraconazole 44-56 phosphoglycolate phosphatase Mus musculus 60-64 33905526-4 2021 In the mouse Leydig cell line TM3, used as a proxy for ovarian theca cells, itraconazole exposure had a suppressing effect on genes downstream of HH signaling, such as Gli1. Itraconazole 76-88 GLI-Kruppel family member GLI1 Mus musculus 168-172 33905526-5 2021 Exposing explanted rat ovaries (gestational day 22 or postnatal day 3) to 30 microM itraconazole for 72 h induced significant suppression of genes in the HH signaling pathway with altered Ihh, Gli1, Ptch1, and Smo expression similar to those previously observed in Ihh/Dhh knock-out mice. Itraconazole 84-96 Indian hedgehog signaling molecule Rattus norvegicus 188-191 33905526-5 2021 Exposing explanted rat ovaries (gestational day 22 or postnatal day 3) to 30 microM itraconazole for 72 h induced significant suppression of genes in the HH signaling pathway with altered Ihh, Gli1, Ptch1, and Smo expression similar to those previously observed in Ihh/Dhh knock-out mice. Itraconazole 84-96 GLI family zinc finger 1 Rattus norvegicus 193-197 33905526-5 2021 Exposing explanted rat ovaries (gestational day 22 or postnatal day 3) to 30 microM itraconazole for 72 h induced significant suppression of genes in the HH signaling pathway with altered Ihh, Gli1, Ptch1, and Smo expression similar to those previously observed in Ihh/Dhh knock-out mice. Itraconazole 84-96 patched 1 Rattus norvegicus 199-204 33905526-5 2021 Exposing explanted rat ovaries (gestational day 22 or postnatal day 3) to 30 microM itraconazole for 72 h induced significant suppression of genes in the HH signaling pathway with altered Ihh, Gli1, Ptch1, and Smo expression similar to those previously observed in Ihh/Dhh knock-out mice. Itraconazole 84-96 smoothened, frizzled class receptor Rattus norvegicus 210-213 33905526-5 2021 Exposing explanted rat ovaries (gestational day 22 or postnatal day 3) to 30 microM itraconazole for 72 h induced significant suppression of genes in the HH signaling pathway with altered Ihh, Gli1, Ptch1, and Smo expression similar to those previously observed in Ihh/Dhh knock-out mice. Itraconazole 84-96 Indian hedgehog signaling molecule Rattus norvegicus 265-268 33905526-5 2021 Exposing explanted rat ovaries (gestational day 22 or postnatal day 3) to 30 microM itraconazole for 72 h induced significant suppression of genes in the HH signaling pathway with altered Ihh, Gli1, Ptch1, and Smo expression similar to those previously observed in Ihh/Dhh knock-out mice. Itraconazole 84-96 desert hedgehog signaling molecule Rattus norvegicus 269-272 33497608-0 2021 Itraconazole synergistically increases therapeutic effect of paclitaxel and 99mTc-MIBI accumulation, as a probe of P-gp activity, in HT-29 tumor-bearing nude mice. Itraconazole 0-12 phosphoglycolate phosphatase Mus musculus 115-119 33497608-4 2021 Itraconazole successfully inhibited P-gp mediated 99mTc-MIBI efflux, increasing its in vitro accumulation in itraconazole-receiving dishes. Itraconazole 0-12 phosphoglycolate phosphatase Mus musculus 36-40 33497608-4 2021 Itraconazole successfully inhibited P-gp mediated 99mTc-MIBI efflux, increasing its in vitro accumulation in itraconazole-receiving dishes. Itraconazole 109-121 phosphoglycolate phosphatase Mus musculus 36-40 32928702-3 2021 This case highlights the dangerous and preventable combination of high glucose intake, glucocorticoids and itraconazole inhibition of CYP3A4 (with resultant glucocorticoid accumulation) that can result in a state of life- threatening HHS in an adolescent with previously stable CFRD. Itraconazole 107-119 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 134-140 33786369-0 2021 Drug Repurposing of Itraconazole and Estradiol Benzoate against COVID-19 by Blocking SARS-CoV-2 Spike Protein-Mediated Membrane Fusion. Itraconazole 20-32 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 96-101 28520375-4 2012 In CYP2D6 poor metabolizers who are taking concomitant strong CYP3A4 inhibitors (e.g., itraconazole, clarithromycin), a quarter of the usual dose should be used (Table 1) (2). Itraconazole 87-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 3-9 33665257-6 2021 The data presented in this article are related to the research paper entitled "Itraconazole synergistically increases therapeutic effect of paclitaxel and 99mTc-MIBI accumulation, as a probe of P-gp activity, in HT-29 tumor-bearing nude mice". Itraconazole 79-91 phosphoglycolate phosphatase Mus musculus 194-198 33387577-3 2021 Recently, the azole antifungals itraconazole and posaconazole were identified to potently inhibit human 11beta-HSD2, and several case studies described patients with acquired AME. Itraconazole 32-44 hydroxysteroid 11-beta dehydrogenase 2 Homo sapiens 104-115 33387577-4 2021 To begin to understand why this adverse drug effect was missed during preclinical investigations, the inhibitory potential of itraconazole, its main metabolite hydroxyitraconazole (OHI) and posaconazole against 11beta-HSD2 from human and three commonly used experimental animals was assessed. Itraconazole 126-138 hydroxysteroid 11-beta dehydrogenase 2 Homo sapiens 211-222 32602215-1 2021 The effects of itraconazole, a strong CYP3A4 inhibitor, on the steady-state pharmacokinetics of vemurafenib were evaluated in a phase 1, multicenter, open-label, fixed-sequence study. Itraconazole 15-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 33315900-5 2020 A photo-crosslinking study confirmed direct binding of itraconazole to a representative folding-defective mutant protein, NPC1-I1061T. Itraconazole 55-67 NPC intracellular cholesterol transporter 1 Homo sapiens 122-126 33387577-7 2021 Exchange of the C-terminus and substitution of residues Leu170,Ile172 in mouse 11beta-HSD2 by the corresponding residues His170,Glu172 of the human enzyme resulted in a gain of sensitivity to itraconazole and posaconazole, resembling human 11beta-HSD2. Itraconazole 192-204 hydroxysteroid 11-beta dehydrogenase 2 Mus musculus 79-90 33387577-7 2021 Exchange of the C-terminus and substitution of residues Leu170,Ile172 in mouse 11beta-HSD2 by the corresponding residues His170,Glu172 of the human enzyme resulted in a gain of sensitivity to itraconazole and posaconazole, resembling human 11beta-HSD2. Itraconazole 192-204 hydroxysteroid 11-beta dehydrogenase 2 Homo sapiens 240-251 33107218-3 2021 We report on how two acumapimod clinical DDI studies and a physiologically based pharmacokinetic (PBPK) model assessing how co-administration of a weak (azithromycin) and strong (itraconazole) CYP3A4 inhibitor affected acumapimod systemic exposure, informed decision-making and supported concomitant use of CYP3A4 and P-gp inhibitors. Itraconazole 179-191 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 193-199 32847935-11 2020 Greater itraconazole levels were significantly and meaningfully associated with reduction in tumor volume (Spearman correlation -0.71; P=0.05) and tumor perfusion (Ktrans) (correlation -0.71; P=0.01), decreases in the pro-angiogenic cytokines interleukin 1b (correlation -0.73; P=0.01) and GM-CSF (correlation -1.00; P<0.001), and reduction in tumor microvessel density (correlation -0.69; P=0.03). Itraconazole 8-20 colony stimulating factor 2 Homo sapiens 290-296 32535897-3 2020 This observation was made in a drug-drug interaction study with the BTK inhibitor fenebrutinib and itraconazole, in which, relative to the control group, the expected increase in fenebrutinib Cmax was not observed in the itraconazole group, and a delay in Tmax was observed in the itraconazole group. Itraconazole 99-111 Bruton tyrosine kinase Canis lupus familiaris 68-71 33312948-4 2020 This study aimed to investigate the effects of vismodegib and itraconazole on the expression of Hedgehog (HH) genes (PTCH1, SMO, and GLI1), cell cycle and cell death in OSCC cells. Itraconazole 62-74 patched 1 Homo sapiens 117-122 33211216-1 2021 The inhibiting effects of itraconazole, an antifungal drug on vascular endothelial growth factor (VEGF) have recently been discovered. Itraconazole 26-38 vascular endothelial growth factor A Homo sapiens 62-96 33211216-1 2021 The inhibiting effects of itraconazole, an antifungal drug on vascular endothelial growth factor (VEGF) have recently been discovered. Itraconazole 26-38 vascular endothelial growth factor A Homo sapiens 98-102 33211216-2 2021 By inhibiting VEGF, itraconazole has shown potential in clinical trials as anti-cancer treatment. Itraconazole 20-32 vascular endothelial growth factor A Homo sapiens 14-18 32935287-6 2020 Itraconazole 200 mg/day elevated steady-state exposure to 5 mg/day balovaptan approximately 4.5-5.5-fold (Day 15 GMR [90% CI], 4.46 [4.06-4.90] for Cmax and 5.57 [5.00-6.21] for AUC) and extended the time to steady state from ~ 5 days to ~ 13-14 days. Itraconazole 0-12 colony stimulating factor 2 receptor subunit alpha Homo sapiens 113-116 32942154-0 2020 Itraconazole exerts anti-liver cancer potential through the Wnt, PI3K/AKT/mTOR, and ROS pathways. Itraconazole 0-12 AKT serine/threonine kinase 1 Homo sapiens 70-73 32942154-0 2020 Itraconazole exerts anti-liver cancer potential through the Wnt, PI3K/AKT/mTOR, and ROS pathways. Itraconazole 0-12 mechanistic target of rapamycin kinase Homo sapiens 74-78 32942154-12 2020 Furthermore, itraconazole inhibited HCC cell growth and promoted apoptosis through the Hh, Wnt/catenin, AKT/mTOR/S6K, ROS and death receptor pathways. Itraconazole 13-25 AKT serine/threonine kinase 1 Homo sapiens 104-107 32942154-12 2020 Furthermore, itraconazole inhibited HCC cell growth and promoted apoptosis through the Hh, Wnt/catenin, AKT/mTOR/S6K, ROS and death receptor pathways. Itraconazole 13-25 mechanistic target of rapamycin kinase Homo sapiens 108-112 33139055-1 2020 PURPOSE: This drug-drug interaction study determined whether the metabolism and distribution of the Polo-like kinase 1 inhibitor, volasertib, is affected by co-administration of the P-glycoprotein and cytochrome P-450 3A4 inhibitor, itraconazole. Itraconazole 233-245 polo like kinase 1 Homo sapiens 100-118 33312948-4 2020 This study aimed to investigate the effects of vismodegib and itraconazole on the expression of Hedgehog (HH) genes (PTCH1, SMO, and GLI1), cell cycle and cell death in OSCC cells. Itraconazole 62-74 smoothened, frizzled class receptor Homo sapiens 124-127 33312948-4 2020 This study aimed to investigate the effects of vismodegib and itraconazole on the expression of Hedgehog (HH) genes (PTCH1, SMO, and GLI1), cell cycle and cell death in OSCC cells. Itraconazole 62-74 GLI family zinc finger 1 Homo sapiens 133-137 33312948-10 2020 Gene expression of PTCH1, SMO, and GLI1 decreased in response to 24 h of treatment with vismodegib or itraconazole. Itraconazole 102-114 patched 1 Homo sapiens 19-24 33312948-10 2020 Gene expression of PTCH1, SMO, and GLI1 decreased in response to 24 h of treatment with vismodegib or itraconazole. Itraconazole 102-114 smoothened, frizzled class receptor Homo sapiens 26-29 33312948-10 2020 Gene expression of PTCH1, SMO, and GLI1 decreased in response to 24 h of treatment with vismodegib or itraconazole. Itraconazole 102-114 GLI family zinc finger 1 Homo sapiens 35-39 33312948-12 2020 An increase in the DNA fragmentation was observed after treatment and both inhibitors induced apoptosis after 72 h. In conclusion, SMO inhibitors vismodegib and itraconazole demonstrably reduced the expression of HH genes in CAL27 OSCC cell line. Itraconazole 161-173 smoothened, frizzled class receptor Homo sapiens 131-134 32515832-7 2020 Parsaclisib maximum plasma drug concentration (Cmax ) and area under the concentration-time curve extrapolated to infinity (AUC0- ) were increased by 21% and 107% with concomitant itraconazole versus parsaclisib alone (GMR, 1.21; 90%CI, 1.14-1.29; and 2.07; 90%CI, 1.97-2.17, respectively). Itraconazole 181-193 colony stimulating factor 2 receptor subunit alpha Homo sapiens 220-223 33879433-0 2020 Hepato-protective role of itraconazole mediated cytochrome p450 pathway inhibition in liver fibrosis. Itraconazole 26-38 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 48-63 33879433-6 2020 Based upon this fact, present study is aimed to evaluate the repurposing of Itraconazole in the prevention of hepatic fibrosis via inhibition of cytochrome P450 pathway. Itraconazole 76-88 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 145-160 32649934-4 2020 By blocking VEGF/VEGFR-2 binding via pre-treatment with itraconazole we demonstrated that animals" condition was deteriorated soon at 1-2 h post-PNV exposure concurrently with decreased expression of VEGF, BBB-associated proteins, ZO-1, beta-catenin, laminin, P-gp (P-glycoprotein), Neu-N (neuron"s viability marker) and MAPKphosphorylated-p38, while phosphorylated-ERK and Src pathways were increased. Itraconazole 56-68 vascular endothelial growth factor A Rattus norvegicus 12-16 32649934-4 2020 By blocking VEGF/VEGFR-2 binding via pre-treatment with itraconazole we demonstrated that animals" condition was deteriorated soon at 1-2 h post-PNV exposure concurrently with decreased expression of VEGF, BBB-associated proteins, ZO-1, beta-catenin, laminin, P-gp (P-glycoprotein), Neu-N (neuron"s viability marker) and MAPKphosphorylated-p38, while phosphorylated-ERK and Src pathways were increased. Itraconazole 56-68 kinase insert domain receptor Rattus norvegicus 17-24 32649934-4 2020 By blocking VEGF/VEGFR-2 binding via pre-treatment with itraconazole we demonstrated that animals" condition was deteriorated soon at 1-2 h post-PNV exposure concurrently with decreased expression of VEGF, BBB-associated proteins, ZO-1, beta-catenin, laminin, P-gp (P-glycoprotein), Neu-N (neuron"s viability marker) and MAPKphosphorylated-p38, while phosphorylated-ERK and Src pathways were increased. Itraconazole 56-68 vascular endothelial growth factor A Rattus norvegicus 17-21 32968519-5 2020 As the detection limits were down to 0.013 and 0.1 microg ml-1 and quantitation limits were 0.04 and 0.032 microg ml-1 for terbinafine and itraconazole, respectively; the in vitro determination of terbinafine and itraconazole in spiked plasma samples was applicable. Itraconazole 139-151 interleukin 17F Homo sapiens 114-118 32459872-0 2020 Pharmacokinetic Drug Interactions of an Orally Available TRH Analog (Rovatirelin) With a CYP3A4/5 and P-Glycoprotein Inhibitor (Itraconazole). Itraconazole 128-140 thyrotropin releasing hormone Homo sapiens 57-60 32459872-0 2020 Pharmacokinetic Drug Interactions of an Orally Available TRH Analog (Rovatirelin) With a CYP3A4/5 and P-Glycoprotein Inhibitor (Itraconazole). Itraconazole 128-140 ATP binding cassette subfamily B member 1 Homo sapiens 102-116 32459872-9 2020 Itraconazole has the potential to inhibit drug transport via intestinal P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP); therefore, substrate assessments of rovatirelin for the 2 transporters were evaluated using Caco-2 cell monolayers. Itraconazole 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 72-86 32459872-9 2020 Itraconazole has the potential to inhibit drug transport via intestinal P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP); therefore, substrate assessments of rovatirelin for the 2 transporters were evaluated using Caco-2 cell monolayers. Itraconazole 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 88-92 32459872-9 2020 Itraconazole has the potential to inhibit drug transport via intestinal P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP); therefore, substrate assessments of rovatirelin for the 2 transporters were evaluated using Caco-2 cell monolayers. Itraconazole 0-12 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 98-130 32459872-9 2020 Itraconazole has the potential to inhibit drug transport via intestinal P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP); therefore, substrate assessments of rovatirelin for the 2 transporters were evaluated using Caco-2 cell monolayers. Itraconazole 0-12 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 132-136 32459872-11 2020 The current study shows that itraconazole"s effect on rovatirelin pharmacokinetics is mediated through inhibition of CYP3A4/5 and intestinal P-gp. Itraconazole 29-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-125 32459872-11 2020 The current study shows that itraconazole"s effect on rovatirelin pharmacokinetics is mediated through inhibition of CYP3A4/5 and intestinal P-gp. Itraconazole 29-41 ATP binding cassette subfamily B member 1 Homo sapiens 141-145 33102531-6 2020 The long-tailed inhibitors (posaconazole and itraconazole) have stronger binding affinities than short-tailed inhibitors (fluconazole and voriconazole) because long-tailed inhibitors can form more hydrophobic interactions with CYP51. Itraconazole 45-57 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 227-232 32407849-8 2020 Itraconazole downregulated the protein expression of Hedgehog pathway to inhibit proliferation and migration of oral squamous cell carcinoma cells, which can be revised by recombinant human sonic hedgehog protein (rSHH). Itraconazole 0-12 sonic hedgehog signaling molecule Homo sapiens 190-212 32407849-8 2020 Itraconazole downregulated the protein expression of Hedgehog pathway to inhibit proliferation and migration of oral squamous cell carcinoma cells, which can be revised by recombinant human sonic hedgehog protein (rSHH). Itraconazole 0-12 sonic hedgehog signaling molecule Rattus norvegicus 214-218 32681018-10 2020 After using the Hedgehog agonist recombinant human Sonic Hedgehog (rhshh), itraconazole could counteract the activation of rhshh. Itraconazole 75-87 sonic hedgehog signaling molecule Homo sapiens 51-65 31578565-6 2020 Pb-infected mice treated with PTX/ITC presented a reduction in the pulmonary concentrations of OH-proline, associated with lower concentrations of interleukin (IL)-6, IL-17, and transforming growth factor (TGF)-beta1 and higher concentrations of IL-10 compared to the controls. Itraconazole 34-37 interleukin 6 Mus musculus 147-165 32080863-10 2020 The PBPK model predicted 3.78- and 7.15-fold increases in the AUC of the potency-adjusted unbound active species with strong CYP3A4 inhibitors itraconazole and ketoconazole, respectively; and 1.62- and 2.37-fold increases with the concomitant use of moderate CYP3A4 inhibitors verapamil and diltiazem, respectively. Itraconazole 143-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 32080863-10 2020 The PBPK model predicted 3.78- and 7.15-fold increases in the AUC of the potency-adjusted unbound active species with strong CYP3A4 inhibitors itraconazole and ketoconazole, respectively; and 1.62- and 2.37-fold increases with the concomitant use of moderate CYP3A4 inhibitors verapamil and diltiazem, respectively. Itraconazole 143-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 259-265 32401271-14 2020 Ever itraconazole exposure was associated with increased SCC risk (AHR, 1.20; 95% CI, 1.00-1.45). Itraconazole 5-17 serpin family B member 3 Homo sapiens 57-60 31578565-6 2020 Pb-infected mice treated with PTX/ITC presented a reduction in the pulmonary concentrations of OH-proline, associated with lower concentrations of interleukin (IL)-6, IL-17, and transforming growth factor (TGF)-beta1 and higher concentrations of IL-10 compared to the controls. Itraconazole 34-37 interleukin 17A Mus musculus 167-172 31578565-6 2020 Pb-infected mice treated with PTX/ITC presented a reduction in the pulmonary concentrations of OH-proline, associated with lower concentrations of interleukin (IL)-6, IL-17, and transforming growth factor (TGF)-beta1 and higher concentrations of IL-10 compared to the controls. Itraconazole 34-37 transforming growth factor, beta 1 Mus musculus 178-216 31578565-6 2020 Pb-infected mice treated with PTX/ITC presented a reduction in the pulmonary concentrations of OH-proline, associated with lower concentrations of interleukin (IL)-6, IL-17, and transforming growth factor (TGF)-beta1 and higher concentrations of IL-10 compared to the controls. Itraconazole 34-37 interleukin 10 Mus musculus 246-251 31287236-2 2020 A 3-arm, open-label, randomized, single-dose, fixed-sequence crossover study was conducted to characterize the effects of the strong inhibitors gemfibrozil (of CYP2C8) and itraconazole (of CYP3A) and the strong inducer rifampin (of CYP3A) on the single-dose pharmacokinetics of brigatinib. Itraconazole 172-184 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 189-194 31578565-8 2020 The mice treated with ITC/Thal and CMX/Thal showed intense weight loss, increased deposition of reticulin fibers, high pulmonary concentrations of CCL3, IFN-gamma and VEGF, and decreased concentrations of IL-6, IL-1beta, IL-17, and TGF-beta1. Itraconazole 22-25 chemokine (C-C motif) ligand 3 Mus musculus 147-151 31578565-8 2020 The mice treated with ITC/Thal and CMX/Thal showed intense weight loss, increased deposition of reticulin fibers, high pulmonary concentrations of CCL3, IFN-gamma and VEGF, and decreased concentrations of IL-6, IL-1beta, IL-17, and TGF-beta1. Itraconazole 22-25 interferon gamma Mus musculus 153-162 31578565-8 2020 The mice treated with ITC/Thal and CMX/Thal showed intense weight loss, increased deposition of reticulin fibers, high pulmonary concentrations of CCL3, IFN-gamma and VEGF, and decreased concentrations of IL-6, IL-1beta, IL-17, and TGF-beta1. Itraconazole 22-25 vascular endothelial growth factor A Mus musculus 167-171 31578565-8 2020 The mice treated with ITC/Thal and CMX/Thal showed intense weight loss, increased deposition of reticulin fibers, high pulmonary concentrations of CCL3, IFN-gamma and VEGF, and decreased concentrations of IL-6, IL-1beta, IL-17, and TGF-beta1. Itraconazole 22-25 interleukin 6 Mus musculus 205-209 31578565-8 2020 The mice treated with ITC/Thal and CMX/Thal showed intense weight loss, increased deposition of reticulin fibers, high pulmonary concentrations of CCL3, IFN-gamma and VEGF, and decreased concentrations of IL-6, IL-1beta, IL-17, and TGF-beta1. Itraconazole 22-25 interleukin 1 beta Mus musculus 211-219 31578565-8 2020 The mice treated with ITC/Thal and CMX/Thal showed intense weight loss, increased deposition of reticulin fibers, high pulmonary concentrations of CCL3, IFN-gamma and VEGF, and decreased concentrations of IL-6, IL-1beta, IL-17, and TGF-beta1. Itraconazole 22-25 interleukin 17A Mus musculus 221-226 31578565-8 2020 The mice treated with ITC/Thal and CMX/Thal showed intense weight loss, increased deposition of reticulin fibers, high pulmonary concentrations of CCL3, IFN-gamma and VEGF, and decreased concentrations of IL-6, IL-1beta, IL-17, and TGF-beta1. Itraconazole 22-25 transforming growth factor, beta 1 Mus musculus 232-241 31893546-3 2020 In this study, a novel brain targeting drug delivery system based on bovine serum albumin (BSA) was constructed for enhancing ITZ distribution in brain. Itraconazole 126-129 albumin Mus musculus 76-89 32391164-1 2020 Background: Itraconazole (ITZ), a triazole antifungal agent, is metabolized to hydroxy-ITZ (OH-ITZ), keto-ITZ (KT-ITZ), and N-desalkyl ITZ (ND-ITZ) by cytochrome P450 3A4. Itraconazole 12-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 151-170 32391164-1 2020 Background: Itraconazole (ITZ), a triazole antifungal agent, is metabolized to hydroxy-ITZ (OH-ITZ), keto-ITZ (KT-ITZ), and N-desalkyl ITZ (ND-ITZ) by cytochrome P450 3A4. Itraconazole 26-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 151-170 31982514-4 2020 Compared to previous experiments revealing a threefold more potent inhibition of 11beta-HSD2 by itraconazole than with posaconazole, the current study found sevenfold stronger CYP11B1 inhibition by posaconazole over itraconazole. Itraconazole 96-108 hydroxysteroid 11-beta dehydrogenase 2 Homo sapiens 81-92 31982514-7 2020 Molecular modeling assessed the binding of posaconazole, itraconazole and OHI to 11beta-HSD2 and the relevant CYP enzymes, and predicted important interactions not formed by the other systemically used azole antifungals, thus providing an initial explanation for the observed inhibitory activities. Itraconazole 57-69 hydroxysteroid 11-beta dehydrogenase 2 Homo sapiens 81-92 31982514-8 2020 Together with available clinical observations, the presented data suggest that itraconazole primarily causes pseudohyperaldosteronism through cortisol-induced MR activation due to 11beta-HSD2 inhibition, and posaconazole by CYP11B1 inhibition and accumulation of the mineralocorticoids 11-deoxycorticosterone and 11-deoxycortisol because of feedback activation. Itraconazole 79-91 hydroxysteroid 11-beta dehydrogenase 2 Homo sapiens 180-191 32331453-4 2020 A recent cryo-EM structure has revealed an itraconazole binding site (IBS) in the SSD of human NPC1. Itraconazole 43-55 NPC intracellular cholesterol transporter 1 Homo sapiens 95-99 31875923-3 2020 We evaluated the effect of steady-state rifampin (a strong CYP3A inducer) and steady-state itraconazole (a strong CYP3A inhibitor) on the pharmacokinetics (PK), safety, and tolerability of zanubrutinib in healthy Asian and non-Asian subjects. Itraconazole 91-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-119 32077323-4 2020 Aim: In the present research, we evaluated the synergistic effects of ketamine with two azole derivatives, itraconazole and fluconazole, on strains of Candida spp. Itraconazole 107-119 histocompatibility minor 13 Homo sapiens 159-162 31673875-12 2020 CONCLUSION: Coadministration of fluconazole or itraconazole or other moderate/strong CYP2C9 or CYP3A4 inhibitors may increase exposure to erdafitinib in healthy adults and thus may warrant erdafitinib dose reduction or use of alternative concomitant medications with no or minimal CYP2C9 or CYP3A4 inhibition potential. Itraconazole 47-59 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 281-287 31673875-12 2020 CONCLUSION: Coadministration of fluconazole or itraconazole or other moderate/strong CYP2C9 or CYP3A4 inhibitors may increase exposure to erdafitinib in healthy adults and thus may warrant erdafitinib dose reduction or use of alternative concomitant medications with no or minimal CYP2C9 or CYP3A4 inhibition potential. Itraconazole 47-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 291-297 32077323-7 2020 Results: Our achievements showed a synergistic effect between ketamine in addition to the two antifungal agents (fluconazole and itraconazole) against planktonic cells and biofilms of Candida spp. Itraconazole 129-141 histocompatibility minor 13 Homo sapiens 192-195 31514064-3 2019 It is shown how the transversal action of the azoles - fluconazole, posaconazole and itraconazole - in both fungi and Leishmania is due to the occurrence of the same target, lanosterol 14-alpha-demethylase, in these two groups of species. Itraconazole 85-97 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 174-205 31728714-2 2020 CYP3A plays a major role in lorlatinib metabolism; therefore, a drug-drug interaction study was warranted to evaluate the impact of the strong CYP3A inhibitor, itraconazole, on lorlatinib plasma exposure. Itraconazole 160-172 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 31728714-2 2020 CYP3A plays a major role in lorlatinib metabolism; therefore, a drug-drug interaction study was warranted to evaluate the impact of the strong CYP3A inhibitor, itraconazole, on lorlatinib plasma exposure. Itraconazole 160-172 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 143-148 31960187-6 2020 RESULT: This review tries to highlight the effect of itraconazole on smoothened receptor (SMO) in the Hedgehog pathway, thereby reducing the glioma-associated oncogene homolog (GLI) release and finally exhibiting a range of anticancer effects, promoting apoptosis of cancer cells, and inhibiting proliferation by indirect inhibition of NF-kappaB pathway and inflammation, moreover, promoting the expression of cyclin-dependent kinase inhibitors, inhibiting the expression of target genes transcribed by GLI such as BCL-2 and Cyclin-D1. Itraconazole 53-65 smoothened, frizzled class receptor Homo sapiens 69-88 31960187-6 2020 RESULT: This review tries to highlight the effect of itraconazole on smoothened receptor (SMO) in the Hedgehog pathway, thereby reducing the glioma-associated oncogene homolog (GLI) release and finally exhibiting a range of anticancer effects, promoting apoptosis of cancer cells, and inhibiting proliferation by indirect inhibition of NF-kappaB pathway and inflammation, moreover, promoting the expression of cyclin-dependent kinase inhibitors, inhibiting the expression of target genes transcribed by GLI such as BCL-2 and Cyclin-D1. Itraconazole 53-65 smoothened, frizzled class receptor Homo sapiens 90-93 31960187-6 2020 RESULT: This review tries to highlight the effect of itraconazole on smoothened receptor (SMO) in the Hedgehog pathway, thereby reducing the glioma-associated oncogene homolog (GLI) release and finally exhibiting a range of anticancer effects, promoting apoptosis of cancer cells, and inhibiting proliferation by indirect inhibition of NF-kappaB pathway and inflammation, moreover, promoting the expression of cyclin-dependent kinase inhibitors, inhibiting the expression of target genes transcribed by GLI such as BCL-2 and Cyclin-D1. Itraconazole 53-65 nuclear factor kappa B subunit 1 Homo sapiens 336-345 31960187-6 2020 RESULT: This review tries to highlight the effect of itraconazole on smoothened receptor (SMO) in the Hedgehog pathway, thereby reducing the glioma-associated oncogene homolog (GLI) release and finally exhibiting a range of anticancer effects, promoting apoptosis of cancer cells, and inhibiting proliferation by indirect inhibition of NF-kappaB pathway and inflammation, moreover, promoting the expression of cyclin-dependent kinase inhibitors, inhibiting the expression of target genes transcribed by GLI such as BCL-2 and Cyclin-D1. Itraconazole 53-65 GLI family zinc finger 1 Homo sapiens 177-180 31960187-6 2020 RESULT: This review tries to highlight the effect of itraconazole on smoothened receptor (SMO) in the Hedgehog pathway, thereby reducing the glioma-associated oncogene homolog (GLI) release and finally exhibiting a range of anticancer effects, promoting apoptosis of cancer cells, and inhibiting proliferation by indirect inhibition of NF-kappaB pathway and inflammation, moreover, promoting the expression of cyclin-dependent kinase inhibitors, inhibiting the expression of target genes transcribed by GLI such as BCL-2 and Cyclin-D1. Itraconazole 53-65 BCL2 apoptosis regulator Homo sapiens 515-520 31960187-6 2020 RESULT: This review tries to highlight the effect of itraconazole on smoothened receptor (SMO) in the Hedgehog pathway, thereby reducing the glioma-associated oncogene homolog (GLI) release and finally exhibiting a range of anticancer effects, promoting apoptosis of cancer cells, and inhibiting proliferation by indirect inhibition of NF-kappaB pathway and inflammation, moreover, promoting the expression of cyclin-dependent kinase inhibitors, inhibiting the expression of target genes transcribed by GLI such as BCL-2 and Cyclin-D1. Itraconazole 53-65 cyclin D1 Homo sapiens 525-534 31960187-7 2020 Besides, itraconazole increases the number of Bnip3, subsequently, inducing the dissociation of the Beclin-1/BCL-2 binding complex, as a result of ultimately promoting autophagy of cancer cells. Itraconazole 9-21 BCL2 interacting protein 3 Homo sapiens 46-51 31960187-7 2020 Besides, itraconazole increases the number of Bnip3, subsequently, inducing the dissociation of the Beclin-1/BCL-2 binding complex, as a result of ultimately promoting autophagy of cancer cells. Itraconazole 9-21 beclin 1 Homo sapiens 100-108 31960187-7 2020 Besides, itraconazole increases the number of Bnip3, subsequently, inducing the dissociation of the Beclin-1/BCL-2 binding complex, as a result of ultimately promoting autophagy of cancer cells. Itraconazole 9-21 BCL2 apoptosis regulator Homo sapiens 109-114 31965399-5 2020 The itraconazole encapsulated nanoparticles, conjugated with R5K peptide, were fabricated to allow multivalent binding interactions with VEGF. Itraconazole 4-16 vascular endothelial growth factor A Homo sapiens 137-141 31965399-6 2020 The R5K peptide blocked VEGF binding to its receptor, while itraconazole altered the signaling pathway of VEGF stimulation. Itraconazole 60-72 vascular endothelial growth factor A Homo sapiens 106-110 31888155-7 2019 At the molecular level, ITR NPs were more effective than ITR solution in inducing pro-apoptotic Bax and p53 while reducing anti-apoptotic Bcl2 protein expression. Itraconazole 24-27 BCL2 associated X, apoptosis regulator Homo sapiens 96-99 31888155-7 2019 At the molecular level, ITR NPs were more effective than ITR solution in inducing pro-apoptotic Bax and p53 while reducing anti-apoptotic Bcl2 protein expression. Itraconazole 24-27 tumor protein p53 Homo sapiens 104-107 31888155-7 2019 At the molecular level, ITR NPs were more effective than ITR solution in inducing pro-apoptotic Bax and p53 while reducing anti-apoptotic Bcl2 protein expression. Itraconazole 24-27 BCL2 apoptosis regulator Homo sapiens 138-142 31888155-7 2019 At the molecular level, ITR NPs were more effective than ITR solution in inducing pro-apoptotic Bax and p53 while reducing anti-apoptotic Bcl2 protein expression. Itraconazole 57-60 BCL2 associated X, apoptosis regulator Homo sapiens 96-99 31888155-7 2019 At the molecular level, ITR NPs were more effective than ITR solution in inducing pro-apoptotic Bax and p53 while reducing anti-apoptotic Bcl2 protein expression. Itraconazole 57-60 tumor protein p53 Homo sapiens 104-107 31888155-7 2019 At the molecular level, ITR NPs were more effective than ITR solution in inducing pro-apoptotic Bax and p53 while reducing anti-apoptotic Bcl2 protein expression. Itraconazole 57-60 BCL2 apoptosis regulator Homo sapiens 138-142 31833479-8 2019 RESULTS Itraconazole reduced the expression of stemness molecules CD133, ABCG2, and ALDH1 in A549 and NCI-H460 human lung cancer cells, and the numbers of sphere-forming cells were reduced. Itraconazole 8-20 prominin 1 Homo sapiens 66-71 31833479-8 2019 RESULTS Itraconazole reduced the expression of stemness molecules CD133, ABCG2, and ALDH1 in A549 and NCI-H460 human lung cancer cells, and the numbers of sphere-forming cells were reduced. Itraconazole 8-20 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 73-78 31833479-8 2019 RESULTS Itraconazole reduced the expression of stemness molecules CD133, ABCG2, and ALDH1 in A549 and NCI-H460 human lung cancer cells, and the numbers of sphere-forming cells were reduced. Itraconazole 8-20 aldehyde dehydrogenase 1 family member A1 Homo sapiens 84-89 31129789-0 2019 Physiologically Based Pharmacokinetic Models for Prediction of Complex CYP2C8 and OATP1B1 (SLCO1B1) Drug-Drug-Gene Interactions: A Modeling Network of Gemfibrozil, Repaglinide, Pioglitazone, Rifampicin, Clarithromycin and Itraconazole. Itraconazole 222-234 solute carrier organic anion transporter family member 1B1 Homo sapiens 82-89 31129789-0 2019 Physiologically Based Pharmacokinetic Models for Prediction of Complex CYP2C8 and OATP1B1 (SLCO1B1) Drug-Drug-Gene Interactions: A Modeling Network of Gemfibrozil, Repaglinide, Pioglitazone, Rifampicin, Clarithromycin and Itraconazole. Itraconazole 222-234 solute carrier organic anion transporter family member 1B1 Homo sapiens 91-98 31728714-7 2020 Results During daily dosing with itraconazole (Period 2), the ratios of the adjusted geometric means for area under the plasma concentration-time profile extrapolated to infinity (AUCinf) and maximum plasma concentration (Cmax) of single-dose lorlatinib 100 mg were 141.79% (90% confidence interval, 128.71%, 156.21%) and 124.39% (110.20%, 140.41%), respectively, compared with Period 1 (lorlatinib alone). Itraconazole 33-45 period circadian regulator 2 Homo sapiens 47-55 31919352-0 2020 Structural basis for itraconazole-mediated NPC1 inhibition. Itraconazole 21-33 NPC intracellular cholesterol transporter 1 Homo sapiens 43-47 31919352-3 2020 Previous studies suggest that mutation of the NPC1-SSD or the addition of the anti-fungal drug itraconazole abolishes NPC1 activity in cells. Itraconazole 95-107 NPC intracellular cholesterol transporter 1 Homo sapiens 118-122 31919352-5 2020 Here, we report a cryo-EM structure of human NPC1 bound to itraconazole, which reveals how this binding site in the center of NPC1 blocks a putative lumenal tunnel linked to the SSD. Itraconazole 59-71 NPC intracellular cholesterol transporter 1 Homo sapiens 45-49 31919352-5 2020 Here, we report a cryo-EM structure of human NPC1 bound to itraconazole, which reveals how this binding site in the center of NPC1 blocks a putative lumenal tunnel linked to the SSD. Itraconazole 59-71 NPC intracellular cholesterol transporter 1 Homo sapiens 126-130 31172535-6 2019 Avadomide exposures, when coadministered with the CYP3A inhibitor itraconazole, were 100.0% and 93.64% of that when administered alone, for AUC0-inf and Cmax , respectively. Itraconazole 66-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-55 31392364-0 2019 Siponimod pharmacokinetics, safety, and tolerability in combination with the potent CYP3A4 inhibitor itraconazole in healthy subjects with different CYP2C9 genotypes. Itraconazole 101-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 31773379-8 2019 Other Shh inhibitors, including the antifungal itraconazole, have been investigated in small trials, but further research is needed before recommending their routine clinical use. Itraconazole 47-59 sonic hedgehog signaling molecule Homo sapiens 6-9 31668109-0 2022 Itraconazole Versus Propranolol: Therapeutic and Pharmacologic Effect On Serum Angiopoietin-2 In Patients With Infantile Hemangioma. Itraconazole 0-12 angiopoietin 2 Homo sapiens 79-93 31668109-2 2022 Itraconazole is a world-wide tolerated antifungal but only a few studies have focused on its assessment in the treatment of IH.Objective: This study aim was to investigate the newly proposed antifungal drug ICZ and characterize different aspects of its usage as antiangiogenic drug.Methods: This is an interventional clinical trial to assess the efficacy of ICZ versus propranolol in the treatment of infantile hemangioma with studying the change in serum Ang2. Itraconazole 0-12 angiopoietin 2 Homo sapiens 456-460 31668109-6 2022 We observed a decrease in serum ang2 level after usage of ICZ & propranolol and the change in serum angiopoietin2 level before and after treatment in each group was statistically significant (p < 0.001).Conclusion: Oral itraconazole can be an equivalent option for oral propranolol while safer and shorter treatment periods. Itraconazole 227-239 angiopoietin 2 Homo sapiens 32-36 31668109-6 2022 We observed a decrease in serum ang2 level after usage of ICZ & propranolol and the change in serum angiopoietin2 level before and after treatment in each group was statistically significant (p < 0.001).Conclusion: Oral itraconazole can be an equivalent option for oral propranolol while safer and shorter treatment periods. Itraconazole 227-239 angiopoietin 2 Homo sapiens 104-117 31692536-5 2019 The most important mechanism of ITZ in the treatment of cancer is inhibition of the Hh pathway through the inhibition of smoothened receptors (SMO), glioma-associated oncogene homologs (GLI), and their downstream targets. Itraconazole 32-35 GLI family zinc finger 1 Homo sapiens 186-189 31479680-4 2019 RESULTS: The rates of synergy for the combination of MTX with fluconazole (FLC), itraconazole (ITC), and voriconazole (VRZ) were 91.3%, 65.2%, and 87% in checkerboard testing. Itraconazole 95-98 metaxin 1 Homo sapiens 53-56 31215774-1 2019 Regulatory agencies currently recommend itraconazole (ITZ) as a strong cytochrome P450 3A (CYP3A) inhibitor for clinical drug-drug interaction (DDI) studies. Itraconazole 40-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-89 31215774-1 2019 Regulatory agencies currently recommend itraconazole (ITZ) as a strong cytochrome P450 3A (CYP3A) inhibitor for clinical drug-drug interaction (DDI) studies. Itraconazole 40-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-96 31215774-1 2019 Regulatory agencies currently recommend itraconazole (ITZ) as a strong cytochrome P450 3A (CYP3A) inhibitor for clinical drug-drug interaction (DDI) studies. Itraconazole 54-57 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-89 31215774-1 2019 Regulatory agencies currently recommend itraconazole (ITZ) as a strong cytochrome P450 3A (CYP3A) inhibitor for clinical drug-drug interaction (DDI) studies. Itraconazole 54-57 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-96 31271764-2 2019 The structurally-diverse small molecule compounds OSW-1, itraconazole (ITZ), T-00127-HEV2 (THEV) and TTP-8307 (TTP) inhibit viral replication through interaction with the OSBP protein. Itraconazole 57-69 oxysterol binding protein Homo sapiens 171-175 31271764-2 2019 The structurally-diverse small molecule compounds OSW-1, itraconazole (ITZ), T-00127-HEV2 (THEV) and TTP-8307 (TTP) inhibit viral replication through interaction with the OSBP protein. Itraconazole 71-74 oxysterol binding protein Homo sapiens 171-175 31044521-4 2019 The model reasonably predicted clinically observed acalabrutinib DDI with the CYP3A perpetrators itraconazole (4.80-fold vs. 5.21-fold observed) and rifampicin (0.21-fold vs. 0.23-fold observed). Itraconazole 97-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-83 30845347-1 2019 AIMS: This phase I study evaluated the effects of the moderate cytochrome P450 (CYP) 3A inhibitor fluconazole and the strong CYP3A/P-glycoprotein (P-gp) inhibitor itraconazole on the pharmacokinetics of the investigational neural precursor cell expressed, developmentally downregulated 8 (NEDD8)-activating enzyme inhibitor pevonedistat in patients with advanced solid tumours. Itraconazole 163-175 phosphoglycolate phosphatase Homo sapiens 125-145 30845347-1 2019 AIMS: This phase I study evaluated the effects of the moderate cytochrome P450 (CYP) 3A inhibitor fluconazole and the strong CYP3A/P-glycoprotein (P-gp) inhibitor itraconazole on the pharmacokinetics of the investigational neural precursor cell expressed, developmentally downregulated 8 (NEDD8)-activating enzyme inhibitor pevonedistat in patients with advanced solid tumours. Itraconazole 163-175 phosphoglycolate phosphatase Homo sapiens 147-151 30845347-1 2019 AIMS: This phase I study evaluated the effects of the moderate cytochrome P450 (CYP) 3A inhibitor fluconazole and the strong CYP3A/P-glycoprotein (P-gp) inhibitor itraconazole on the pharmacokinetics of the investigational neural precursor cell expressed, developmentally downregulated 8 (NEDD8)-activating enzyme inhibitor pevonedistat in patients with advanced solid tumours. Itraconazole 163-175 NEDD8 ubiquitin like modifier Homo sapiens 223-287 30845347-1 2019 AIMS: This phase I study evaluated the effects of the moderate cytochrome P450 (CYP) 3A inhibitor fluconazole and the strong CYP3A/P-glycoprotein (P-gp) inhibitor itraconazole on the pharmacokinetics of the investigational neural precursor cell expressed, developmentally downregulated 8 (NEDD8)-activating enzyme inhibitor pevonedistat in patients with advanced solid tumours. Itraconazole 163-175 NEDD8 ubiquitin like modifier Homo sapiens 289-294 30813555-9 2019 Itraconazole (ITZ) is an antifungal agent that targets sterol-transport molecules such as OSBP and OSBP-related protein 4 (ORP4). Itraconazole 0-12 oxysterol binding protein Homo sapiens 90-94 30690033-0 2019 Itraconazole Induces Regression of Infantile Hemangioma via Downregulation of the Platelet-Derived Growth Factor-D/PI3K/Akt/mTOR Pathway. Itraconazole 0-12 platelet-derived growth factor, D polypeptide Mus musculus 82-114 30690033-0 2019 Itraconazole Induces Regression of Infantile Hemangioma via Downregulation of the Platelet-Derived Growth Factor-D/PI3K/Akt/mTOR Pathway. Itraconazole 0-12 thymoma viral proto-oncogene 1 Mus musculus 120-123 30690033-0 2019 Itraconazole Induces Regression of Infantile Hemangioma via Downregulation of the Platelet-Derived Growth Factor-D/PI3K/Akt/mTOR Pathway. Itraconazole 0-12 mechanistic target of rapamycin kinase Mus musculus 124-128 30690033-6 2019 Importantly, itraconazole significantly reduced platelet-derived growth factor-D level, resulting in suppression of platelet-derived growth factor-beta activation and inhibition of its downstream effectors, such as PI3K, Akt, 4E-BP1, and p70S6K, which are important for cellular growth and survival of infantile hemangioma. Itraconazole 13-25 platelet-derived growth factor, D polypeptide Mus musculus 48-80 30690033-6 2019 Importantly, itraconazole significantly reduced platelet-derived growth factor-D level, resulting in suppression of platelet-derived growth factor-beta activation and inhibition of its downstream effectors, such as PI3K, Akt, 4E-BP1, and p70S6K, which are important for cellular growth and survival of infantile hemangioma. Itraconazole 13-25 thymoma viral proto-oncogene 1 Mus musculus 221-224 30690033-6 2019 Importantly, itraconazole significantly reduced platelet-derived growth factor-D level, resulting in suppression of platelet-derived growth factor-beta activation and inhibition of its downstream effectors, such as PI3K, Akt, 4E-BP1, and p70S6K, which are important for cellular growth and survival of infantile hemangioma. Itraconazole 13-25 eukaryotic translation initiation factor 4E binding protein 1 Mus musculus 226-232 30690033-6 2019 Importantly, itraconazole significantly reduced platelet-derived growth factor-D level, resulting in suppression of platelet-derived growth factor-beta activation and inhibition of its downstream effectors, such as PI3K, Akt, 4E-BP1, and p70S6K, which are important for cellular growth and survival of infantile hemangioma. Itraconazole 13-25 ribosomal protein S6 kinase, polypeptide 1 Mus musculus 238-244 30690033-7 2019 In conclusion, our results suggest that platelet-derived growth factor-D is a target of itraconazole in infantile hemangioma. Itraconazole 88-100 platelet-derived growth factor, D polypeptide Mus musculus 40-72 31235707-4 2019 At sub-MIC concentrations, fluconazole and miconazole stimulate catalase activity 2-3-fold but, unexpectedly, deletion of cytosolic catalase (ctt1) makes cells more resistant to these azoles and to clotrimazole, itraconazole and posaconazole. Itraconazole 212-224 catalase T Saccharomyces cerevisiae S288C 142-146 30260036-0 2019 Itraconazole inhibits proliferation of pancreatic cancer cells through activation of Bak-1. Itraconazole 0-12 BCL2 antagonist/killer 1 Homo sapiens 85-90 30260036-6 2019 These data suggested that itraconazole exhibited antiproliferative effects in pancreatic cancer cells by inducing apoptosis through Bak-1 activation. Itraconazole 26-38 BCL2 antagonist/killer 1 Homo sapiens 132-137 31140972-5 2019 CONCLUSION: Our study illustrated varying degrees of synergism between caspofungin or terbinafine and itraconazole, voriconazole, posaconazole or amphotericin B towards Chaetomium spp., which could be a reference for the clinical treatment of Chaetomium spp. Itraconazole 102-114 histocompatibility minor 13 Homo sapiens 180-183 30985942-7 2019 The PBPK model predicted that the AUC for mirabegron with itraconazole (a CYP3A4 inhibitor) was 4.12-times that in healthy elderly subjects administered mirabegron alone, and predicted that the proportional change in AUC for desipramine (a CYP2D6 substrate) with mirabegron was greater than that in healthy subjects. Itraconazole 58-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 74-80 30985942-7 2019 The PBPK model predicted that the AUC for mirabegron with itraconazole (a CYP3A4 inhibitor) was 4.12-times that in healthy elderly subjects administered mirabegron alone, and predicted that the proportional change in AUC for desipramine (a CYP2D6 substrate) with mirabegron was greater than that in healthy subjects. Itraconazole 58-70 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 240-246 31024507-14 2019 Fusarium keratoplasticum showed high MIC values (8->32 mug mL-1) for itraconazole, voriconazole, posaconazole, and isavuconazole. Itraconazole 72-84 2'-5' oligoadenylate synthetase 1B Mus musculus 62-66 30813555-9 2019 Itraconazole (ITZ) is an antifungal agent that targets sterol-transport molecules such as OSBP and OSBP-related protein 4 (ORP4). Itraconazole 0-12 oxysterol binding protein 2 Homo sapiens 99-121 30813555-9 2019 Itraconazole (ITZ) is an antifungal agent that targets sterol-transport molecules such as OSBP and OSBP-related protein 4 (ORP4). Itraconazole 0-12 oxysterol binding protein 2 Homo sapiens 123-127 30813555-9 2019 Itraconazole (ITZ) is an antifungal agent that targets sterol-transport molecules such as OSBP and OSBP-related protein 4 (ORP4). Itraconazole 14-17 oxysterol binding protein Homo sapiens 90-94 30813555-9 2019 Itraconazole (ITZ) is an antifungal agent that targets sterol-transport molecules such as OSBP and OSBP-related protein 4 (ORP4). Itraconazole 14-17 oxysterol binding protein 2 Homo sapiens 99-121 30813555-9 2019 Itraconazole (ITZ) is an antifungal agent that targets sterol-transport molecules such as OSBP and OSBP-related protein 4 (ORP4). Itraconazole 14-17 oxysterol binding protein 2 Homo sapiens 123-127 31449848-6 2019 The flo8/flo8 mutation isolates exhibited increased resistance to fluconazole, voriconazole, and itraconazole compared with the wild-type and drug sensitivity was restored by FLO8 overexpression (flo8/flo8::FLO8). Itraconazole 97-109 FLO8 Saccharomyces cerevisiae S288C 4-8 29989304-2 2019 We investigated whether an individual"s baseline in vivo CYP3A4 activity, assessed using the oral midazolam (MDZ) probe, could be used to predict the magnitude of drug-drug interaction between tacrolimus and the potent CYP3A4 inhibitor itraconazole. Itraconazole 236-248 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 29989304-2 2019 We investigated whether an individual"s baseline in vivo CYP3A4 activity, assessed using the oral midazolam (MDZ) probe, could be used to predict the magnitude of drug-drug interaction between tacrolimus and the potent CYP3A4 inhibitor itraconazole. Itraconazole 236-248 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 219-225 31449848-6 2019 The flo8/flo8 mutation isolates exhibited increased resistance to fluconazole, voriconazole, and itraconazole compared with the wild-type and drug sensitivity was restored by FLO8 overexpression (flo8/flo8::FLO8). Itraconazole 97-109 FLO8 Saccharomyces cerevisiae S288C 9-13 31449848-6 2019 The flo8/flo8 mutation isolates exhibited increased resistance to fluconazole, voriconazole, and itraconazole compared with the wild-type and drug sensitivity was restored by FLO8 overexpression (flo8/flo8::FLO8). Itraconazole 97-109 FLO8 Saccharomyces cerevisiae S288C 9-13 30327180-13 2019 CONCLUSION: Itraconazole modulates serum PSA levels without lowering serum testosterone. Itraconazole 12-24 kallikrein related peptidase 3 Homo sapiens 41-44 30341799-7 2019 Reduced susceptibility to fluconazole (FLU), 5-flucytosine (5-FC) and itraconazole (ITR) was observed among C. neoformans isolates from Chinese paediatric patients, particularly among the ST5 isolates, which was similar to observations made on C. neoformans isolates from Chinese adult patients. Itraconazole 70-82 DENN domain containing 2B Homo sapiens 188-191 30341799-7 2019 Reduced susceptibility to fluconazole (FLU), 5-flucytosine (5-FC) and itraconazole (ITR) was observed among C. neoformans isolates from Chinese paediatric patients, particularly among the ST5 isolates, which was similar to observations made on C. neoformans isolates from Chinese adult patients. Itraconazole 84-87 DENN domain containing 2B Homo sapiens 188-191 30302786-2 2019 The objectives of this entry-into-human study were to assess the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics of risdiplam, and the effect of the strong CYP3A inhibitor itraconazole on the PK of risdiplam in healthy male volunteers. Itraconazole 189-201 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 173-178 31449848-6 2019 The flo8/flo8 mutation isolates exhibited increased resistance to fluconazole, voriconazole, and itraconazole compared with the wild-type and drug sensitivity was restored by FLO8 overexpression (flo8/flo8::FLO8). Itraconazole 97-109 FLO8 Saccharomyces cerevisiae S288C 9-13 30342850-2 2018 Our chemical suppressor screening in zebrafish embryos identified antifungal azoles including clotrimazole, miconazole, and itraconazole, as Wnt/beta-catenin signaling inhibitors. Itraconazole 124-136 catenin (cadherin-associated protein), beta 1 Danio rerio 145-157 29320899-0 2019 In vitro analysis of itraconazole cis-diastereoisomers inhibition of nine cytochrome P450 enzymes: stereoselective inhibition of CYP3A. Itraconazole 21-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-134 30481027-0 2018 Novel Tetrazole-Containing Analogues of Itraconazole as Potent Antiangiogenic Agents with Reduced Cytochrome P450 3A4 Inhibition. Itraconazole 40-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-117 30481027-2 2018 The wider use of itraconazole in the treatment of cancer, however, has been limited by its potent inhibition of the drug metabolizing enzyme cytochrome P450 3A4 (CYP3A4). Itraconazole 17-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-160 30481027-2 2018 The wider use of itraconazole in the treatment of cancer, however, has been limited by its potent inhibition of the drug metabolizing enzyme cytochrome P450 3A4 (CYP3A4). Itraconazole 17-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 162-168 30166405-4 2018 Additional analyses in 16 healthy volunteers showed that dual pharmacological inhibition of CYP3A4 and P-glycoprotein using itraconazole resulted in increased tacrolimus metabolite/parent ratios (+65%, +112%, and 25% for 13-, 15-, and 31-DMT, respectively; P < 0.01). Itraconazole 124-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 30166405-4 2018 Additional analyses in 16 healthy volunteers showed that dual pharmacological inhibition of CYP3A4 and P-glycoprotein using itraconazole resulted in increased tacrolimus metabolite/parent ratios (+65%, +112%, and 25% for 13-, 15-, and 31-DMT, respectively; P < 0.01). Itraconazole 124-136 ATP binding cassette subfamily B member 1 Homo sapiens 103-117 30091221-0 2018 PBPK Models for CYP3A4 and P-gp DDI Prediction: A Modeling Network of Rifampicin, Itraconazole, Clarithromycin, Midazolam, Alfentanil, and Digoxin. Itraconazole 82-94 phosphoglycolate phosphatase Homo sapiens 27-31 30075232-3 2018 We investigated whether VEGF has a neuroprotective role by inhibiting its binding to receptor Flk-1 by itraconazole (ITZ). Itraconazole 103-115 vascular endothelial growth factor A Rattus norvegicus 24-28 30075232-3 2018 We investigated whether VEGF has a neuroprotective role by inhibiting its binding to receptor Flk-1 by itraconazole (ITZ). Itraconazole 103-115 kinase insert domain receptor Rattus norvegicus 94-99 30075232-3 2018 We investigated whether VEGF has a neuroprotective role by inhibiting its binding to receptor Flk-1 by itraconazole (ITZ). Itraconazole 117-120 vascular endothelial growth factor A Rattus norvegicus 24-28 30075232-3 2018 We investigated whether VEGF has a neuroprotective role by inhibiting its binding to receptor Flk-1 by itraconazole (ITZ). Itraconazole 117-120 kinase insert domain receptor Rattus norvegicus 94-99 29930379-9 2018 Using molecular docking simulations, we identify itraconazole as a C1GALT1 inhibitor that directly binds C1GALT1 and promotes its proteasomal degradation, leading to significant blockade of C1GALT1-mediated effects in HNSCC cells in vitro and in vivo. Itraconazole 49-61 core 1 synthase, glycoprotein-N-acetylgalactosamine 3-beta-galactosyltransferase 1 Homo sapiens 67-74 30068519-0 2018 Physiologically Based Pharmacokinetic Model of Itraconazole and Two of Its Metabolites to Improve the Predictions and the Mechanistic Understanding of CYP3A4 Drug-Drug Interactions. Itraconazole 47-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 151-157 30068519-1 2018 Physiologically based pharmacokinetic (PBPK) modeling for itraconazole using a bottom-up approach is challenging, not only due to complex saturable pharmacokinetics (PK) and the presence of three metabolites exhibiting CYP3A4 inhibition, but also because of discrepancies in reported in vitro data. Itraconazole 58-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 219-225 30068519-7 2018 In addition, itraconazole DDIs with midazolam and other CYP3A4 substrates were successfully predicted within a 2-fold error. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 29930379-9 2018 Using molecular docking simulations, we identify itraconazole as a C1GALT1 inhibitor that directly binds C1GALT1 and promotes its proteasomal degradation, leading to significant blockade of C1GALT1-mediated effects in HNSCC cells in vitro and in vivo. Itraconazole 49-61 core 1 synthase, glycoprotein-N-acetylgalactosamine 3-beta-galactosyltransferase 1 Homo sapiens 105-112 29930379-9 2018 Using molecular docking simulations, we identify itraconazole as a C1GALT1 inhibitor that directly binds C1GALT1 and promotes its proteasomal degradation, leading to significant blockade of C1GALT1-mediated effects in HNSCC cells in vitro and in vivo. Itraconazole 49-61 core 1 synthase, glycoprotein-N-acetylgalactosamine 3-beta-galactosyltransferase 1 Homo sapiens 105-112 30250932-0 2018 Itraconazole perturbs colorectal cancer dormancy through SUFU-mediated WNT inhibition. Itraconazole 0-12 SUFU negative regulator of hedgehog signaling Homo sapiens 57-61 30171694-1 2018 This study investigated the effect of itraconazole, a strong dual inhibitor of cytochrome P450 (CYP) 3A4 and P-glycoprotein (P-gp), on the single dose pharmacokinetics of leniolisib. Itraconazole 38-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 79-104 30171694-1 2018 This study investigated the effect of itraconazole, a strong dual inhibitor of cytochrome P450 (CYP) 3A4 and P-glycoprotein (P-gp), on the single dose pharmacokinetics of leniolisib. Itraconazole 38-50 ATP binding cassette subfamily B member 1 Homo sapiens 125-129 30171694-7 2018 These findings suggest that the interaction with itraconazole occurred mainly systemically through inhibition of CYP3A, and corroborate our in vitro findings that leniolisib is neither a sensitive CYP3A substrate nor a relevant in vivo substrate for intestinal or hepatic P-gp. Itraconazole 49-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 113-118 30171694-8 2018 Assuming itraconazole levels achieved complete inhibition of CYP3A, the fractional contribution of CYP3A to the overall disposition of leniolisib is estimated to be about 50%. Itraconazole 9-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-66 30028640-9 2018 CONCLUSIONS: The use of the reference-scaling approach with 3-period design (TRR, RTR, and RRT) was an efficient way to demonstrate that two commercially available oral itraconazole formulations met the predetermined bioequivalence criteria. Itraconazole 169-181 nuclear receptor subfamily 6 group A member 1 Homo sapiens 82-85 30127974-9 2018 Itraconazole treatment inhibited the proliferation and altered cell cycle in SGC-7901 cells while promoting early apoptosis and DNA damage. Itraconazole 0-12 sarcoglycan beta Homo sapiens 77-80 30127974-11 2018 Combination itraconazole and 5-FU treatment showed a synergetic anticancer effect in SGC-7901 cells. Itraconazole 12-24 sarcoglycan beta Homo sapiens 85-88 29136186-8 2018 Only two heterozygous amino acid substitutions (A18P/A and R365G/R) in Erg3p were found in two isolates with cross-resistance to fluconazole, itraconazole, and voriconazole. Itraconazole 142-154 ETS transcription factor ERG Homo sapiens 71-76 29807040-0 2018 Structure-activity relationship study of itraconazole, a broad-range inhibitor of picornavirus replication that targets oxysterol-binding protein (OSBP). Itraconazole 41-53 oxysterol binding protein Homo sapiens 120-145 29807040-0 2018 Structure-activity relationship study of itraconazole, a broad-range inhibitor of picornavirus replication that targets oxysterol-binding protein (OSBP). Itraconazole 41-53 oxysterol binding protein Homo sapiens 147-151 29550418-6 2018 Short hairpin RNA (shRNA)-mediated knockdown of SOX9, as well as smoothened inhibition by itraconazole and vismodegib, reduces mTOR expression and the phosphorylation of known downstream mTOR targets. Itraconazole 90-102 mechanistic target of rapamycin kinase Homo sapiens 127-131 29550418-6 2018 Short hairpin RNA (shRNA)-mediated knockdown of SOX9, as well as smoothened inhibition by itraconazole and vismodegib, reduces mTOR expression and the phosphorylation of known downstream mTOR targets. Itraconazole 90-102 mechanistic target of rapamycin kinase Homo sapiens 187-191 29027194-2 2018 The aim of this study was to characterize the pediatric predictive performance of the PBPK approach for 10 drugs extensively metabolized by CYP1A2 (theophylline), CYP2C8 (desloratidine, montelukast), CYP2C9 (diclofenac), CYP2C19 (esomeprazole, lansoprazole), CYP2D6 (tramadol), and CYP3A4 (itraconazole, ondansetron, sufentanil). Itraconazole 290-302 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 140-146 29684903-1 2018 In this work, we aimed at developing an improved topical SLN formulation combining itraconazole delivery with a coating layer of didodecyldimethylammonium bromide, thus repurposing the drug effectiveness by synergistic skin anticancer effectiveness. Itraconazole 83-95 sarcolipin Homo sapiens 57-60 29684903-8 2018 Ours results demonstrate the potentiality of repurposing itraconazole activity by using the combined nanoencapsulation strategy with the positively charged coating layer on SLN, which can be further investigated as a promising stable and safe approach to significantly reduce the viability of skin cancer cells. Itraconazole 57-69 sarcolipin Homo sapiens 173-176 29568906-0 2018 miR-124/MCP-1 signaling pathway modulates the protective effect of itraconazole on acute kidney injury in a mouse model of disseminated candidiasis. Itraconazole 67-79 chemokine (C-C motif) ligand 2 Mus musculus 8-13 29469197-8 2018 Moderate DDI with itraconazole was predicted in subjects with wild-type CYP2C19 or UGT1A4. Itraconazole 18-30 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 72-79 29469197-8 2018 Moderate DDI with itraconazole was predicted in subjects with wild-type CYP2C19 or UGT1A4. Itraconazole 18-30 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 83-89 29172026-9 2018 A reduction of the enzymatic activity of the UGT2B7 was recorded in the presence of 9 of the 14 drugs under investigation (ketoconazole, miconazole, itraconazole, diclofenac, ibuprofen, clonazepam, lorazepam, lormetazepam, and triazolam), with a consequent significant reduction of the levels of the glucuronide metabolites. Itraconazole 149-161 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 45-51 29469197-12 2018 DDI with itraconazole is likely to be dependent on the genotypes of CYP2C19 and UGT1A4. Itraconazole 9-21 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 68-75 29469197-12 2018 DDI with itraconazole is likely to be dependent on the genotypes of CYP2C19 and UGT1A4. Itraconazole 9-21 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 80-86 28436712-13 2018 Mechanistic static modeling that incorporated small non-CYP-mediated metabolic clearance and renal clearance components predicted an AUC ratio of 4.7 for the effect of itraconazole, a strong CYP3A4 inhibitor, on galunisertib. Itraconazole 168-180 peptidylprolyl isomerase G Homo sapiens 56-59 29592879-0 2018 Itraconazole-Induced Inhibition on Human Esophageal Cancer Cell Growth Requires AMPK Activation. Itraconazole 0-12 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 80-84 29592879-3 2018 Itraconazole activated AMPK signaling, which was required for subsequent esophageal cancer cell death. Itraconazole 0-12 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 23-27 29592879-4 2018 Pharmacologic AMPK inhibition, AMPKalpha1 shRNA, or dominant negative mutation (T172A) almost completely abolished itraconazole-induced cytotoxicity against esophageal cancer cells. Itraconazole 115-127 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 14-18 29592879-5 2018 Significantly, itraconazole induced AMPK-dependent autophagic cell death (but not apoptosis) in esophageal cancer cells. Itraconazole 15-27 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 36-40 29592879-6 2018 Furthermore, AMPK activation by itraconazole induced multiple receptor tyrosine kinases (RTKs: EGFR, PDGFRalpha, and PDGFRbeta), lysosomal translocation, and degradation to inhibit downstream Akt activation. Itraconazole 32-44 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 13-17 29592879-6 2018 Furthermore, AMPK activation by itraconazole induced multiple receptor tyrosine kinases (RTKs: EGFR, PDGFRalpha, and PDGFRbeta), lysosomal translocation, and degradation to inhibit downstream Akt activation. Itraconazole 32-44 epidermal growth factor receptor Homo sapiens 95-99 29592879-6 2018 Furthermore, AMPK activation by itraconazole induced multiple receptor tyrosine kinases (RTKs: EGFR, PDGFRalpha, and PDGFRbeta), lysosomal translocation, and degradation to inhibit downstream Akt activation. Itraconazole 32-44 platelet derived growth factor receptor alpha Homo sapiens 101-111 29592879-6 2018 Furthermore, AMPK activation by itraconazole induced multiple receptor tyrosine kinases (RTKs: EGFR, PDGFRalpha, and PDGFRbeta), lysosomal translocation, and degradation to inhibit downstream Akt activation. Itraconazole 32-44 platelet derived growth factor receptor beta Homo sapiens 117-126 29592879-6 2018 Furthermore, AMPK activation by itraconazole induced multiple receptor tyrosine kinases (RTKs: EGFR, PDGFRalpha, and PDGFRbeta), lysosomal translocation, and degradation to inhibit downstream Akt activation. Itraconazole 32-44 AKT serine/threonine kinase 1 Homo sapiens 192-195 29592879-10 2018 AMPK activation, RTK degradation, and Akt inhibition were observed in itraconazole-treated tumors. Itraconazole 70-82 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 0-4 29592879-10 2018 AMPK activation, RTK degradation, and Akt inhibition were observed in itraconazole-treated tumors. Itraconazole 70-82 AKT serine/threonine kinase 1 Homo sapiens 38-41 29592879-11 2018 Together, itraconazole inhibits esophageal cancer cell growth via activating AMPK signaling. Itraconazole 10-22 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 77-81 29635947-7 2018 P-gp inducers, carbamazepine, and inhibitors such as itraconazole and verapamil show greater effects on the pharmacokinetics of (S)-fexofenadine. Itraconazole 53-65 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 29385285-1 2018 We describe a case of apparent mineralocorticoid excess (hypertension, hypokalemia, metabolic alkalosis and low plasma renin activity) secondary to itraconazole therapy. Itraconazole 148-160 renin Homo sapiens 119-124 29634721-12 2018 However we have demonstrated itraconazole and voriconazole are modestly effective for CPA, especially if given for 12 months, but fewer than 50% of patients manage this duration. Itraconazole 29-41 carboxypeptidase A1 Homo sapiens 86-89 29484419-0 2018 Itraconazole inhibits invasion and migration of pancreatic cancer cells by suppressing TGF-beta/SMAD2/3 signaling. Itraconazole 0-12 transforming growth factor, beta 1 Mus musculus 87-95 29484419-0 2018 Itraconazole inhibits invasion and migration of pancreatic cancer cells by suppressing TGF-beta/SMAD2/3 signaling. Itraconazole 0-12 SMAD family member 2 Mus musculus 96-103 28679023-0 2017 Notable Drug-Drug Interaction Between Etizolam and Itraconazole in Poor Metabolizers of Cytochrome P450 2C19. Itraconazole 51-63 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 88-108 29434820-10 2018 Conversely, silencing of AMPK by small interfering RNA resulted in an increase of ITCZ-reduced gluconeogenesis and inhibition of ITCZ-induced glucose uptake with relative upregulation of PEPCK and G6Pase and downregulation of GLUT4 in the presence of 50 microg/ml ITCZ (P<0.05). Itraconazole 82-86 solute carrier family 2 member 4 Homo sapiens 226-231 28782144-7 2018 The ADIs can be explained by VDS accumulation owing to inherent loss of CYP3A5 (*3/*3) function, and inhibition of CYP3A4 activity by itraconazole. Itraconazole 134-146 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 28782144-8 2018 WHAT IS NEW AND CONCLUSION: Syndrome of inappropriate antidiuretic hormone from co-administration of itraconazole and VDS has not previously been reported to our knowledge. Itraconazole 101-113 arginine vasopressin Homo sapiens 54-74 28940733-9 2018 Fluconazole, econazole, itraconazole and terbinafine inhibited fungal growth with MIC values ranging from 0.031 to >64 mug mL-1 . Itraconazole 24-36 L1 cell adhesion molecule Mus musculus 126-130 30472702-0 2018 Itraconazole Attenuates Peritoneal Fibrosis Through Its Effect on the Sonic Hedgehog Signaling Pathway in Mice. Itraconazole 0-12 sonic hedgehog Mus musculus 70-84 30472702-5 2018 Itraconazole, an anti-fungal agent, was also recently recognized as an inhibitor of the SHH signaling pathway. Itraconazole 0-12 sonic hedgehog Mus musculus 88-91 30472702-12 2018 The expression of the following SHH signaling pathway components was upregulated in the CG group and suppressed by itraconazole treatment: SHH, patched, smoothened, and glioma-associated oncogene transcription factor 1. Itraconazole 115-127 sonic hedgehog Mus musculus 32-35 30472702-12 2018 The expression of the following SHH signaling pathway components was upregulated in the CG group and suppressed by itraconazole treatment: SHH, patched, smoothened, and glioma-associated oncogene transcription factor 1. Itraconazole 115-127 sonic hedgehog Mus musculus 139-142 30472702-16 2018 It also demonstrates that itraconazole treatment has protective effects on peritoneal fibrosis through the regulation of the SHH signaling pathway. Itraconazole 26-38 sonic hedgehog Mus musculus 125-128 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 0-12 vascular endothelial growth factor A Homo sapiens 249-283 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 0-12 vascular endothelial growth factor A Homo sapiens 285-289 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 0-12 fibroblast growth factor 2 Homo sapiens 292-322 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 0-12 fibroblast growth factor 2 Homo sapiens 324-328 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 0-12 kinase insert domain receptor Homo sapiens 331-376 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 0-12 kinase insert domain receptor Homo sapiens 378-384 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 0-12 mechanistic target of rapamycin kinase Homo sapiens 405-434 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 0-12 mechanistic target of rapamycin kinase Homo sapiens 436-440 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 14-17 vascular endothelial growth factor A Homo sapiens 249-283 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 14-17 vascular endothelial growth factor A Homo sapiens 285-289 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 14-17 fibroblast growth factor 2 Homo sapiens 292-322 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 14-17 fibroblast growth factor 2 Homo sapiens 324-328 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 14-17 kinase insert domain receptor Homo sapiens 331-376 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 14-17 kinase insert domain receptor Homo sapiens 378-384 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 14-17 mechanistic target of rapamycin kinase Homo sapiens 405-434 29068216-1 2017 Itraconazole (ITA), an old and widely prescribed antifungal drug with excellent safety profile, has more recently been demonstrated to be a multitarget antiangiogenesis agent affecting multiple angiogenic stimulatory signals and pathways, including vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and mammalian target of rapamycin (mTOR). Itraconazole 14-17 mechanistic target of rapamycin kinase Homo sapiens 436-440 29181306-6 2017 The itraconazole group showed reduced expression of VEGF-A, VEGFR-2, TNF-alpha, IL-6 than the PBS group (all P<0.05). Itraconazole 4-16 vascular endothelial growth factor A Mus musculus 52-58 29181306-6 2017 The itraconazole group showed reduced expression of VEGF-A, VEGFR-2, TNF-alpha, IL-6 than the PBS group (all P<0.05). Itraconazole 4-16 kinase insert domain protein receptor Mus musculus 60-67 29181306-6 2017 The itraconazole group showed reduced expression of VEGF-A, VEGFR-2, TNF-alpha, IL-6 than the PBS group (all P<0.05). Itraconazole 4-16 tumor necrosis factor Mus musculus 69-78 29181306-6 2017 The itraconazole group showed reduced expression of VEGF-A, VEGFR-2, TNF-alpha, IL-6 than the PBS group (all P<0.05). Itraconazole 4-16 interleukin 6 Mus musculus 80-84 29022838-6 2017 Expert opinion: Currently studies demonstrating the pharmacogenomic influences on itraconazole, posaconazole and isavuconazole are minimal and limited to their inhibitory effects on CYP3A4 in expressors of CYP3A5 variants. Itraconazole 82-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 206-212 28993551-11 2017 DDIs perpetrated by FLV and itraconazole were successfully predicted by use of the present method where two DDI predictors [perpetrator-specific inhibitory activities toward CYP isoforms (pAi, CYPs) and victim-specific fractional CYP-isoform contributions to the clearance (vfm, CYPs)] are determined successively as shown in the graphical abstract. Itraconazole 28-40 serpin family E member 1 Homo sapiens 188-191 28679023-2 2017 The effect of itraconazole (a strong CYP3A inhibitor) on the pharmacokinetics of etizolam (a substrate of CYP2C19 and CYP3A) was assessed in both extensive metabolizers (EMs) and poor metabolizers (PMs) of CYP2C19. Itraconazole 14-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-42 28679023-2 2017 The effect of itraconazole (a strong CYP3A inhibitor) on the pharmacokinetics of etizolam (a substrate of CYP2C19 and CYP3A) was assessed in both extensive metabolizers (EMs) and poor metabolizers (PMs) of CYP2C19. Itraconazole 14-26 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 106-113 30108741-5 2017 4 mug mL-1 for itraconazole). Itraconazole 15-27 L1 cell adhesion molecule Mus musculus 6-10 28789339-1 2017 Itraconazole, a common anti-fungal agent, has demonstrated potential anticancer activity, including reversing chemoresistance mediated by P-glycoprotein, modulating the signal transduction pathways of Hedgehog, mechanistic target of rapamycin and Wnt/beta-catenin in cancer cells, inhibiting angiogenesis and lymphangiogenesis, and possibly interfering with cancer-stromal cell interactions. Itraconazole 0-12 mechanistic target of rapamycin kinase Homo sapiens 211-242 27858342-6 2017 RESULTS: The statin models reasonably predicted the observed exposure change due to Organic Anion Transporting Polypeptide (OATP) 1B1 polymorphism or clinical DDIs with itraconazole, erythromycin, and gemfibrozil, while under-predicted the observed DDIs caused by rifampin and cyclosporine. Itraconazole 169-181 solute carrier organic anion transporter family member 1B1 Homo sapiens 84-133 28495568-4 2017 DDIs with rifampicin and itraconazole were simulated using in vivo Rdif (ratio of diffusional uptake to active uptake) and beta (the fraction of the sum of intrinsic clearances for metabolism and biliary excretion in all possible itineraries of intracellular drugs including basolateral efflux) estimated by static analyses based on the extended clearance concept, in vivo inhibition constant (Ki) for hepatic OATPs reported previously, and in vivo Ki for CYP3A determined from DDI data with midazolam and itraconazole. Itraconazole 25-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 456-461 28823259-6 2017 CONCLUSION: Arsenic trioxide combined with itraconazole can inhibit the KG1a cell proliferation and induce apoptosis, which may be related with the inhibition of Hh signaling pathway and upregulation of both Caspase-3 and BAX protein expression, and provided experimental data of arsenic trioxide combined with itraconazole for the treatment of refractory AML. Itraconazole 43-55 caspase 3 Homo sapiens 208-217 28823259-6 2017 CONCLUSION: Arsenic trioxide combined with itraconazole can inhibit the KG1a cell proliferation and induce apoptosis, which may be related with the inhibition of Hh signaling pathway and upregulation of both Caspase-3 and BAX protein expression, and provided experimental data of arsenic trioxide combined with itraconazole for the treatment of refractory AML. Itraconazole 43-55 BCL2 associated X, apoptosis regulator Homo sapiens 222-225 28789339-1 2017 Itraconazole, a common anti-fungal agent, has demonstrated potential anticancer activity, including reversing chemoresistance mediated by P-glycoprotein, modulating the signal transduction pathways of Hedgehog, mechanistic target of rapamycin and Wnt/beta-catenin in cancer cells, inhibiting angiogenesis and lymphangiogenesis, and possibly interfering with cancer-stromal cell interactions. Itraconazole 0-12 catenin beta 1 Homo sapiens 251-263 28747628-9 2017 These results suggest that itraconazole selectively inhibits endothelial cells rather than cancer cells by targeting multiple pathways including hedgehog, and mTOR pathways and angiogenesis. Itraconazole 27-39 mechanistic target of rapamycin kinase Homo sapiens 159-163 28668841-0 2017 Itraconazole Modulates Hedgehog, WNT/beta-catenin, as well as Akt Signalling, and Inhibits Proliferation of Cervical Cancer Cells. Itraconazole 0-12 catenin beta 1 Homo sapiens 37-49 28668841-0 2017 Itraconazole Modulates Hedgehog, WNT/beta-catenin, as well as Akt Signalling, and Inhibits Proliferation of Cervical Cancer Cells. Itraconazole 0-12 AKT serine/threonine kinase 1 Homo sapiens 62-65 28668841-7 2017 The microarray analysis showed an 8-fold down-regulation in the expression of GLI1, WNT4 and WNT10A among itraconazole-treated CaSki cells. Itraconazole 106-118 GLI family zinc finger 1 Homo sapiens 78-82 28666022-10 2017 Quantitative RT-PCR showed significantly lower expression of VEGFR2 mRNA in the RPE-choroid complexes of itraconazole-injected eyes than those of BSS-injected eyes on days 7 and 14 (p = 0.003 and p = 0.006). Itraconazole 105-117 kinase insert domain receptor Rattus norvegicus 61-67 28668841-7 2017 The microarray analysis showed an 8-fold down-regulation in the expression of GLI1, WNT4 and WNT10A among itraconazole-treated CaSki cells. Itraconazole 106-118 Wnt family member 4 Homo sapiens 84-88 28668841-7 2017 The microarray analysis showed an 8-fold down-regulation in the expression of GLI1, WNT4 and WNT10A among itraconazole-treated CaSki cells. Itraconazole 106-118 Wnt family member 10A Homo sapiens 93-99 28666022-11 2017 Western blots indicated that VEGFR2 was downregulated after itraconazole treatment. Itraconazole 60-72 kinase insert domain receptor Rattus norvegicus 29-35 28666022-12 2017 ELISA showed a significant difference in VEGF level between itraconazole-injected and BSS-injected eyes on days 7 and 14 (p = 0.04 and p = 0.001). Itraconazole 60-72 vascular endothelial growth factor A Rattus norvegicus 41-45 28666022-14 2017 Itraconazole had anti-angiogenic activity along with the reduction of VEGFR2 and VEGF levels. Itraconazole 0-12 kinase insert domain receptor Rattus norvegicus 70-76 28666022-14 2017 Itraconazole had anti-angiogenic activity along with the reduction of VEGFR2 and VEGF levels. Itraconazole 0-12 vascular endothelial growth factor A Rattus norvegicus 70-74 28390928-0 2017 Itraconazole cis-diastereoisomers activate aryl hydrocarbon receptor AhR and pregnane X receptor PXR and induce CYP1A1 in human cell lines and human hepatocytes. Itraconazole 0-12 aryl hydrocarbon receptor Homo sapiens 69-72 28390928-0 2017 Itraconazole cis-diastereoisomers activate aryl hydrocarbon receptor AhR and pregnane X receptor PXR and induce CYP1A1 in human cell lines and human hepatocytes. Itraconazole 0-12 nuclear receptor subfamily 1 group I member 2 Homo sapiens 97-100 28390928-0 2017 Itraconazole cis-diastereoisomers activate aryl hydrocarbon receptor AhR and pregnane X receptor PXR and induce CYP1A1 in human cell lines and human hepatocytes. Itraconazole 0-12 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 112-118 28390928-4 2017 Therefore, we have prepared 4 pure cis-diastereoisomers of itraconazole and investigated their effects on transcriptional activities of xenoreceptors aryl hydrocarbon receptor AhR and pregnane X receptor PXR. Itraconazole 59-71 aryl hydrocarbon receptor Homo sapiens 176-179 28390928-4 2017 Therefore, we have prepared 4 pure cis-diastereoisomers of itraconazole and investigated their effects on transcriptional activities of xenoreceptors aryl hydrocarbon receptor AhR and pregnane X receptor PXR. Itraconazole 59-71 nuclear receptor subfamily 1 group I member 2 Homo sapiens 204-207 28390928-5 2017 Gene reporter assays showed that itraconazole dose-dependently activated both AhR and PXR, and the activation of AhR but not of PXR was enantiospecific. Itraconazole 33-45 aryl hydrocarbon receptor Homo sapiens 78-81 28390928-5 2017 Gene reporter assays showed that itraconazole dose-dependently activated both AhR and PXR, and the activation of AhR but not of PXR was enantiospecific. Itraconazole 33-45 nuclear receptor subfamily 1 group I member 2 Homo sapiens 86-89 28390928-5 2017 Gene reporter assays showed that itraconazole dose-dependently activated both AhR and PXR, and the activation of AhR but not of PXR was enantiospecific. Itraconazole 33-45 aryl hydrocarbon receptor Homo sapiens 113-116 28390928-6 2017 Itraconazole diastereoisomers transformed AhR and PXR into their DNA-binding forms, as demonstrated by electromobility shift assays. Itraconazole 0-12 aryl hydrocarbon receptor Homo sapiens 42-45 28390928-6 2017 Itraconazole diastereoisomers transformed AhR and PXR into their DNA-binding forms, as demonstrated by electromobility shift assays. Itraconazole 0-12 nuclear receptor subfamily 1 group I member 2 Homo sapiens 50-53 28390928-7 2017 Cytochrome P450 CYP1A1 mRNA and protein were induced by itraconazole diastereoisomers in human hepatoma cells HepG2, human skin cells HaCaT, and in primary human hepatocytes. Itraconazole 56-68 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 0-22 28390928-9 2017 Collectively, we show that itraconazole is a dual activator of AhR and PXR, with differential effects on the target genes for xenoreceptors. Itraconazole 27-39 aryl hydrocarbon receptor Homo sapiens 63-66 28390928-9 2017 Collectively, we show that itraconazole is a dual activator of AhR and PXR, with differential effects on the target genes for xenoreceptors. Itraconazole 27-39 nuclear receptor subfamily 1 group I member 2 Homo sapiens 71-74 28131847-7 2017 The most potent 11beta-HSD2 inhibition, using cell lysates expressing recombinant human 11beta-HSD2, was obtained for itraconazole (IC50 139+-14nM), its active metabolite hydroxyitraconazole (IC50 223+-31nM) and posaconazole (IC50 460+-98nM). Itraconazole 118-130 hydroxysteroid 11-beta dehydrogenase 2 Homo sapiens 16-27 28212537-0 2017 Itraconazole exerts its anti-melanoma effect by suppressing Hedgehog, Wnt, and PI3K/mTOR signaling pathways. Itraconazole 0-12 mechanistic target of rapamycin kinase Mus musculus 84-88 28212537-8 2017 Moreover, we demonstrate that itraconazole significantly down-regulates Gli-1, Gli-2, Wnt3A, beta-catenin and cyclin D1, while it up-regulates Gli-3 and Axin-1, indicating potent inhibitory effects of itraconazole on Hedgehog (Hh) and Wnt signaling pathways. Itraconazole 30-42 GLI-Kruppel family member GLI1 Mus musculus 72-77 28212537-8 2017 Moreover, we demonstrate that itraconazole significantly down-regulates Gli-1, Gli-2, Wnt3A, beta-catenin and cyclin D1, while it up-regulates Gli-3 and Axin-1, indicating potent inhibitory effects of itraconazole on Hedgehog (Hh) and Wnt signaling pathways. Itraconazole 30-42 GLI-Kruppel family member GLI2 Mus musculus 79-84 28212537-8 2017 Moreover, we demonstrate that itraconazole significantly down-regulates Gli-1, Gli-2, Wnt3A, beta-catenin and cyclin D1, while it up-regulates Gli-3 and Axin-1, indicating potent inhibitory effects of itraconazole on Hedgehog (Hh) and Wnt signaling pathways. Itraconazole 30-42 wingless-type MMTV integration site family, member 3A Mus musculus 86-91 28212537-8 2017 Moreover, we demonstrate that itraconazole significantly down-regulates Gli-1, Gli-2, Wnt3A, beta-catenin and cyclin D1, while it up-regulates Gli-3 and Axin-1, indicating potent inhibitory effects of itraconazole on Hedgehog (Hh) and Wnt signaling pathways. Itraconazole 30-42 catenin (cadherin associated protein), beta 1 Mus musculus 93-105 28212537-8 2017 Moreover, we demonstrate that itraconazole significantly down-regulates Gli-1, Gli-2, Wnt3A, beta-catenin and cyclin D1, while it up-regulates Gli-3 and Axin-1, indicating potent inhibitory effects of itraconazole on Hedgehog (Hh) and Wnt signaling pathways. Itraconazole 30-42 cyclin D1 Mus musculus 110-119 28212537-8 2017 Moreover, we demonstrate that itraconazole significantly down-regulates Gli-1, Gli-2, Wnt3A, beta-catenin and cyclin D1, while it up-regulates Gli-3 and Axin-1, indicating potent inhibitory effects of itraconazole on Hedgehog (Hh) and Wnt signaling pathways. Itraconazole 30-42 GLI-Kruppel family member GLI3 Mus musculus 143-148 28212537-8 2017 Moreover, we demonstrate that itraconazole significantly down-regulates Gli-1, Gli-2, Wnt3A, beta-catenin and cyclin D1, while it up-regulates Gli-3 and Axin-1, indicating potent inhibitory effects of itraconazole on Hedgehog (Hh) and Wnt signaling pathways. Itraconazole 30-42 axin 1 Mus musculus 153-159 28212537-9 2017 Furthermore, itraconazole significantly suppresses the PI3K/mTOR signaling pathway - indicated by the down-regulated phosphorylation of p70S6K, 4E-BP1 and AKT - but has no effect on the phosphorylation of MEK or ERK. Itraconazole 13-25 mechanistic target of rapamycin kinase Mus musculus 60-64 28212537-9 2017 Furthermore, itraconazole significantly suppresses the PI3K/mTOR signaling pathway - indicated by the down-regulated phosphorylation of p70S6K, 4E-BP1 and AKT - but has no effect on the phosphorylation of MEK or ERK. Itraconazole 13-25 thymoma viral proto-oncogene 1 Mus musculus 155-158 28212537-9 2017 Furthermore, itraconazole significantly suppresses the PI3K/mTOR signaling pathway - indicated by the down-regulated phosphorylation of p70S6K, 4E-BP1 and AKT - but has no effect on the phosphorylation of MEK or ERK. Itraconazole 13-25 midkine Mus musculus 205-208 28212537-9 2017 Furthermore, itraconazole significantly suppresses the PI3K/mTOR signaling pathway - indicated by the down-regulated phosphorylation of p70S6K, 4E-BP1 and AKT - but has no effect on the phosphorylation of MEK or ERK. Itraconazole 13-25 mitogen-activated protein kinase 1 Mus musculus 212-215 28212537-10 2017 Our data suggest that itraconazole inhibits melanoma growth through an interacting regulatory network that includes Hh, Wnt, and PI3K/mTOR signaling pathways. Itraconazole 22-34 mechanistic target of rapamycin kinase Mus musculus 134-138 28159723-8 2017 This covalent binding of apolipoproteinE to the surface of a drug delivery system enables targeting of low density lipoprotein receptor (LDLR) expressed on endothelial brain capillary cell membranes, making our novel highly loaded itraconazole poly(butyl cyanoacrylate) nanocapsules a promising drug delivery system for treatment of cryptococcal meningitis. Itraconazole 231-243 low density lipoprotein receptor Homo sapiens 103-135 28159723-8 2017 This covalent binding of apolipoproteinE to the surface of a drug delivery system enables targeting of low density lipoprotein receptor (LDLR) expressed on endothelial brain capillary cell membranes, making our novel highly loaded itraconazole poly(butyl cyanoacrylate) nanocapsules a promising drug delivery system for treatment of cryptococcal meningitis. Itraconazole 231-243 low density lipoprotein receptor Homo sapiens 137-141 28131847-7 2017 The most potent 11beta-HSD2 inhibition, using cell lysates expressing recombinant human 11beta-HSD2, was obtained for itraconazole (IC50 139+-14nM), its active metabolite hydroxyitraconazole (IC50 223+-31nM) and posaconazole (IC50 460+-98nM). Itraconazole 118-130 hydroxysteroid 11-beta dehydrogenase 2 Homo sapiens 88-99 27822915-4 2017 Multiple regression analysis showed that concomitant use of oral itraconazole or voriconazole significantly increased the (C/Dpo)/(C/Div) of tacrolimus (p = 0.002), probably owing to the inhibition of enterohepatic cytochrome P450 3A4. Itraconazole 65-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 215-234 28399898-10 2017 In vitro, studies showed that the expression of glioma-associated zinc finger transcription factor 1 (Gli1) was decreased at both transcriptional and translational levels after treatment with itraconazole. Itraconazole 192-204 GLI family zinc finger 1 Homo sapiens 102-106 28399898-11 2017 Dual luciferase assay also indicated that itraconazole could inhibit the transcription of Gli1. Itraconazole 42-54 GLI family zinc finger 1 Homo sapiens 90-94 28399898-13 2017 CONCLUSIONS: Hh signaling is activated in gastric tumor and itraconazole can inhibit the growth of gastric cancer cells by inhibiting Gli1 expression. Itraconazole 60-72 GLI family zinc finger 1 Homo sapiens 134-138 28281345-1 2017 Photoinduced dehalogenation of the antifungal drug itraconazole (ITR) in acetonitrile (ACN) and ACN/water mixed solutions was investigated using femtosecond and nanosecond time-resolved transient absorption (fs-TA and ns-TA, respectively) and nanosecond time-resolved resonance Raman spectroscopy (ns-TR3) experiments. Itraconazole 51-63 nuclear receptor subfamily 4 group A member 1 Homo sapiens 301-304 28281345-1 2017 Photoinduced dehalogenation of the antifungal drug itraconazole (ITR) in acetonitrile (ACN) and ACN/water mixed solutions was investigated using femtosecond and nanosecond time-resolved transient absorption (fs-TA and ns-TA, respectively) and nanosecond time-resolved resonance Raman spectroscopy (ns-TR3) experiments. Itraconazole 65-68 nuclear receptor subfamily 4 group A member 1 Homo sapiens 301-304 28179296-0 2017 Itraconazole Inhibits AKT/mTOR Signaling and Proliferation in Endometrial Cancer Cells. Itraconazole 0-12 AKT serine/threonine kinase 1 Homo sapiens 22-25 28179296-0 2017 Itraconazole Inhibits AKT/mTOR Signaling and Proliferation in Endometrial Cancer Cells. Itraconazole 0-12 mechanistic target of rapamycin kinase Homo sapiens 26-30 28179296-5 2017 Itraconazole did not suppress GLI1 or GLI2 transcription but did inhibit the expression of mammalian target of rapamycin (mTOR) signaling components in AN3-CA and HEC-1A cells, while inducing that of microtubule-associated protein 1A/1B-light chain 3-II, a marker of autophagy. Itraconazole 0-12 mechanistic target of rapamycin kinase Homo sapiens 91-120 28179296-5 2017 Itraconazole did not suppress GLI1 or GLI2 transcription but did inhibit the expression of mammalian target of rapamycin (mTOR) signaling components in AN3-CA and HEC-1A cells, while inducing that of microtubule-associated protein 1A/1B-light chain 3-II, a marker of autophagy. Itraconazole 0-12 mechanistic target of rapamycin kinase Homo sapiens 122-126 28179296-7 2017 CONCLUSION: Itraconazole treatment suppresses the growth of EC cells by inhibiting AKT/mTOR signalling. Itraconazole 12-24 AKT serine/threonine kinase 1 Homo sapiens 83-86 28179296-7 2017 CONCLUSION: Itraconazole treatment suppresses the growth of EC cells by inhibiting AKT/mTOR signalling. Itraconazole 12-24 mechanistic target of rapamycin kinase Homo sapiens 87-91 28103683-0 2017 Simultaneous Targeting of NPC1 and VDAC1 by Itraconazole Leads to Synergistic Inhibition of mTOR Signaling and Angiogenesis. Itraconazole 44-56 NPC intracellular cholesterol transporter 1 Homo sapiens 26-30 27810405-4 2017 Itraconazole treatment inhibited hedgehog pathway key molecular expression, such as SHH and Gli1, resulting in promotion of apoptosis and autophagy. Itraconazole 0-12 GLI family zinc finger 1 Homo sapiens 92-96 27810405-5 2017 The anti-proliferation effect of itraconazole-induced apoptosis and autophagy via hedgehog pathway inhibition was confirmed with Gli1 inhibitor GANT61 and SHH siRNA, GANT61 and SHH siRNA synergistically enhanced cytotoxicity induced by itraconazole. Itraconazole 33-45 GLI family zinc finger 1 Homo sapiens 129-133 27810405-5 2017 The anti-proliferation effect of itraconazole-induced apoptosis and autophagy via hedgehog pathway inhibition was confirmed with Gli1 inhibitor GANT61 and SHH siRNA, GANT61 and SHH siRNA synergistically enhanced cytotoxicity induced by itraconazole. Itraconazole 33-45 sonic hedgehog signaling molecule Homo sapiens 155-158 27810405-5 2017 The anti-proliferation effect of itraconazole-induced apoptosis and autophagy via hedgehog pathway inhibition was confirmed with Gli1 inhibitor GANT61 and SHH siRNA, GANT61 and SHH siRNA synergistically enhanced cytotoxicity induced by itraconazole. Itraconazole 33-45 sonic hedgehog signaling molecule Homo sapiens 177-180 27810405-2 2017 We report that itraconazole was cytotoxic to MCF-7 and SKBR-3 breast cancer cell lines via apoptosis by altering mitochondria membrane potential, reducing BCL-2 expression and elevating caspase-3 activity. Itraconazole 15-27 BCL2 apoptosis regulator Homo sapiens 155-160 27810405-2 2017 We report that itraconazole was cytotoxic to MCF-7 and SKBR-3 breast cancer cell lines via apoptosis by altering mitochondria membrane potential, reducing BCL-2 expression and elevating caspase-3 activity. Itraconazole 15-27 caspase 3 Homo sapiens 186-195 27810405-3 2017 Itraconazole also induced autophagic cell death via LC3-II expression upregulation, P62/SQSTM1 degradation, autophagosome formation and increases in autophagic puncta. Itraconazole 0-12 sequestosome 1 Homo sapiens 84-87 27810405-3 2017 Itraconazole also induced autophagic cell death via LC3-II expression upregulation, P62/SQSTM1 degradation, autophagosome formation and increases in autophagic puncta. Itraconazole 0-12 sequestosome 1 Homo sapiens 88-94 27810405-4 2017 Itraconazole treatment inhibited hedgehog pathway key molecular expression, such as SHH and Gli1, resulting in promotion of apoptosis and autophagy. Itraconazole 0-12 sonic hedgehog signaling molecule Homo sapiens 84-87 28103683-0 2017 Simultaneous Targeting of NPC1 and VDAC1 by Itraconazole Leads to Synergistic Inhibition of mTOR Signaling and Angiogenesis. Itraconazole 44-56 voltage dependent anion channel 1 Homo sapiens 35-40 28103683-0 2017 Simultaneous Targeting of NPC1 and VDAC1 by Itraconazole Leads to Synergistic Inhibition of mTOR Signaling and Angiogenesis. Itraconazole 44-56 mechanistic target of rapamycin kinase Homo sapiens 92-96 28103683-2 2017 Itraconazole has been shown to exert its antiangiogenic activity through inhibition of the mTOR signaling pathway, but the molecular mechanism of action was unknown. Itraconazole 0-12 mechanistic target of rapamycin kinase Homo sapiens 91-95 28103683-3 2017 We recently identified the mitochondrial protein VDAC1 as a target of itraconazole and a mediator of its activation of AMPK, an upstream regulator of mTOR. Itraconazole 70-82 voltage dependent anion channel 1 Homo sapiens 49-54 28103683-5 2017 In this study, we demonstrate that cholesterol trafficking inhibition by itraconazole is due to direct inhibition of the lysosomal protein NPC1. Itraconazole 73-85 NPC intracellular cholesterol transporter 1 Homo sapiens 139-143 28103683-6 2017 We further map the binding site of itraconazole to the sterol-sensing domain of NPC1 using mutagenesis, competition with U18666A, and molecular docking. Itraconazole 35-47 NPC intracellular cholesterol transporter 1 Homo sapiens 80-84 27449014-5 2017 In particular, the first x-ray co-crystal structures of fungal CYP51 complexed with lanosterol and itraconazole are compared with co-crystal structures of other protozoal CYP51 enzymes. Itraconazole 99-111 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 63-68 27449014-5 2017 In particular, the first x-ray co-crystal structures of fungal CYP51 complexed with lanosterol and itraconazole are compared with co-crystal structures of other protozoal CYP51 enzymes. Itraconazole 99-111 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 171-176 27225997-2 2016 A clinical drug-drug interaction (DDI) study with the potent CYP3A4 inhibitor itraconazole resulted in an approximately sevenfold increase in cobimetinib exposure. Itraconazole 78-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-67 27812353-17 2016 In conclusion, INK128 could enhance the in vitro antifungal activity of voriconazole, itraconazole and posaconazole against Exophiala spp. Itraconazole 86-98 histocompatibility minor 13 Homo sapiens 134-137 28124646-6 2016 Th1 and Th2 type cells were differentiated in the presence of varying concentrations of itraconazole. Itraconazole 88-100 negative elongation factor complex member C/D Homo sapiens 0-3 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 BCL2 associated X, apoptosis regulator Homo sapiens 237-240 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 caspase 3 Homo sapiens 250-259 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 ceramide synthase 1 Homo sapiens 287-292 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 BCL2 apoptosis regulator Homo sapiens 360-365 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 AKT serine/threonine kinase 1 Homo sapiens 498-501 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 CREB regulated transcription coactivator 1 Mus musculus 508-514 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 AKT serine/threonine kinase 1 Homo sapiens 584-587 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 CREB regulated transcription coactivator 1 Mus musculus 594-600 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 ceramide synthase 1 Homo sapiens 618-624 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 98-110 BCL2 associated X, apoptosis regulator Homo sapiens 237-240 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 98-110 BCL2 associated X, apoptosis regulator Homo sapiens 237-240 27852416-6 2016 Conclusion: Itraconazole induces apoptosis of PC-3 cell through increasing the intracellular ceramide content, which might relate to upregulation of cleavage-caspase 3 and Bax, downregulation of Bcl-2 and inactivation of Akt-mTORC signal pathway. Itraconazole 12-24 caspase 3 Homo sapiens 158-167 27852416-6 2016 Conclusion: Itraconazole induces apoptosis of PC-3 cell through increasing the intracellular ceramide content, which might relate to upregulation of cleavage-caspase 3 and Bax, downregulation of Bcl-2 and inactivation of Akt-mTORC signal pathway. Itraconazole 12-24 BCL2 associated X, apoptosis regulator Homo sapiens 172-175 27852416-6 2016 Conclusion: Itraconazole induces apoptosis of PC-3 cell through increasing the intracellular ceramide content, which might relate to upregulation of cleavage-caspase 3 and Bax, downregulation of Bcl-2 and inactivation of Akt-mTORC signal pathway. Itraconazole 12-24 BCL2 apoptosis regulator Homo sapiens 195-200 27852416-6 2016 Conclusion: Itraconazole induces apoptosis of PC-3 cell through increasing the intracellular ceramide content, which might relate to upregulation of cleavage-caspase 3 and Bax, downregulation of Bcl-2 and inactivation of Akt-mTORC signal pathway. Itraconazole 12-24 AKT serine/threonine kinase 1 Homo sapiens 221-224 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 BCL2 associated X, apoptosis regulator Homo sapiens 38-41 27852416-5 2016 Western blot analysis showed that the Bax, cleaved-caspase 3 expression of itraconazole group and itraconazole+ PDMP group was significantly higher than control group, while Bcl-2 expression was significantly lower than the control; the Bax, cleaved-caspase 3 expression ofitraconazole+ CerS1-shRNA group was significantly lower than itraconazole group, while Bcl-2 expression was significantly higher than the itraconazole group.After 5, 10, 20 mumol/L itraconazole treatment, the expression of p-Akt and p-mTORC1 were significantly lower than the control group; the expression of p-Akt and p-mTORC1 in itraconazole+ CerS-1-shRNA group were significantly higher than itraconazole group. Itraconazole 75-87 caspase 3 Homo sapiens 51-60 33597793-2 2016 Recent studies indicate that itraconazole can also inhibit the growth of basal cell carcinoma (BCC) through suppression of the Sonic Hedgehog (SHH) signaling pathway. Itraconazole 29-41 sonic hedgehog signaling molecule Homo sapiens 127-141 27112167-7 2016 The antifungal azoles, posaconazole, itraconazole, and ketoconazole, significantly inhibited MDR3-mediated phosphatidylcholine secretion. Itraconazole 37-49 ATP binding cassette subfamily B member 4 Homo sapiens 93-97 25670260-9 2016 DISCUSSION: Itraconazole has been shown to have many mechanisms by which it could potentially suppress tumor cell growth, which includes inhibition of the Hedgehog pathway, vascular endothelial growth factor receptor-2, and P-glycoprotein efflux pump. Itraconazole 12-24 kinase insert domain receptor Homo sapiens 173-218 25670260-9 2016 DISCUSSION: Itraconazole has been shown to have many mechanisms by which it could potentially suppress tumor cell growth, which includes inhibition of the Hedgehog pathway, vascular endothelial growth factor receptor-2, and P-glycoprotein efflux pump. Itraconazole 12-24 ATP binding cassette subfamily B member 1 Homo sapiens 224-238 27001813-4 2016 Fifty percent inhibitory concentrations (IC50s) for P-gp and BCRP were both 2 muM for itraconazole, 5 and 12 muM for hydroxyitraconazole, 3 and 6 muM for posaconazole, and 3 and 11 muM for isavuconazole, respectively. Itraconazole 86-98 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 27001813-4 2016 Fifty percent inhibitory concentrations (IC50s) for P-gp and BCRP were both 2 muM for itraconazole, 5 and 12 muM for hydroxyitraconazole, 3 and 6 muM for posaconazole, and 3 and 11 muM for isavuconazole, respectively. Itraconazole 86-98 BCR pseudogene 1 Homo sapiens 61-65 27001813-4 2016 Fifty percent inhibitory concentrations (IC50s) for P-gp and BCRP were both 2 muM for itraconazole, 5 and 12 muM for hydroxyitraconazole, 3 and 6 muM for posaconazole, and 3 and 11 muM for isavuconazole, respectively. Itraconazole 86-98 latexin Homo sapiens 78-81 27001813-5 2016 BSEP was strongly inhibited by itraconazole and hydroxyitraconazole (3 and 17 muM, respectively). Itraconazole 31-43 ATP binding cassette subfamily B member 11 Homo sapiens 0-4 27001813-5 2016 BSEP was strongly inhibited by itraconazole and hydroxyitraconazole (3 and 17 muM, respectively). Itraconazole 31-43 latexin Homo sapiens 78-81 27784375-7 2016 qPCR and Western blot results confirmed that the ATO combined with ITRA could significantly down-regulated expression of Gli1, leading to significantly decrease of cyclinD1 and BCL-2 expression levels. Itraconazole 67-71 GLI-Kruppel family member GLI1 Mus musculus 121-125 27784375-7 2016 qPCR and Western blot results confirmed that the ATO combined with ITRA could significantly down-regulated expression of Gli1, leading to significantly decrease of cyclinD1 and BCL-2 expression levels. Itraconazole 67-71 cyclin D1 Mus musculus 164-172 27784375-7 2016 qPCR and Western blot results confirmed that the ATO combined with ITRA could significantly down-regulated expression of Gli1, leading to significantly decrease of cyclinD1 and BCL-2 expression levels. Itraconazole 67-71 B cell leukemia/lymphoma 2 Mus musculus 177-182 27105861-0 2016 Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024(Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin. Itraconazole 103-115 androgen receptor Homo sapiens 51-68 26823493-4 2016 The antifungal itraconazole was demonstrated to be a potent SMO antagonist with a distinct mechanism of action from that of current SMO inhibitors. Itraconazole 15-27 smoothened, frizzled class receptor Homo sapiens 60-63 26823493-4 2016 The antifungal itraconazole was demonstrated to be a potent SMO antagonist with a distinct mechanism of action from that of current SMO inhibitors. Itraconazole 15-27 smoothened, frizzled class receptor Homo sapiens 132-135 26765315-3 2016 OBJECTIVE: To determine whether administration of intravenous arsenic trioxide and oral itraconazole in patients with metastatic BCC is associated with a reduction in GLI1 messenger RNA expression in tumor and/or normal skin biopsy samples. Itraconazole 88-100 GLI family zinc finger 1 Homo sapiens 167-171 26765315-11 2016 Overall, arsenic trioxide and itraconazole reduced GLI1 messenger RNA levels by 75% from baseline (P < .001). Itraconazole 30-42 GLI family zinc finger 1 Homo sapiens 51-55 33597793-2 2016 Recent studies indicate that itraconazole can also inhibit the growth of basal cell carcinoma (BCC) through suppression of the Sonic Hedgehog (SHH) signaling pathway. Itraconazole 29-41 sonic hedgehog signaling molecule Homo sapiens 143-146 26722041-5 2016 Itraconazole also suppressed monocyte chemoattractant protein-1 secretion and the growth of CAFs. Itraconazole 0-12 C-C motif chemokine ligand 2 Homo sapiens 29-63 26668209-8 2016 The results indicate that, like ketoconazole, the alternative clinical CYP3A4/5 inhibitors ritonavir, clarithromycin, and itraconazole each have unique transporter inhibition profiles. Itraconazole 122-134 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 26171880-8 2015 Encapsulation efficiency (EE (%)), absolute drug loading (AL (%)) and release rate of itraconazole from PBCA-NSP in vitro were measured by reversed phase high-performance liquid chromatography (RP-HPLC). Itraconazole 86-98 PBCA Homo sapiens 104-108 26467209-0 2016 Prediction of area under the curve for a p-glycoprotein, a CYP3A4 and a CYP2C9 substrate using a single time point strategy: assessment using fexofenadine, itraconazole and losartan and metabolites. Itraconazole 156-168 ATP binding cassette subfamily B member 1 Homo sapiens 41-55 28057172-3 2016 The effects of five azole antifungal agents, fluconazole, itraconazole, ketoconazole, miconazole, and voriconazole, on the aminopyrine N-demethylation activity by CYP2C8 were investigated. Itraconazole 58-70 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 163-169 26655341-0 2015 Antifungal drug itraconazole targets VDAC1 to modulate the AMPK/mTOR signaling axis in endothelial cells. Itraconazole 16-28 voltage dependent anion channel 1 Homo sapiens 37-42 26655341-0 2015 Antifungal drug itraconazole targets VDAC1 to modulate the AMPK/mTOR signaling axis in endothelial cells. Itraconazole 16-28 mechanistic target of rapamycin kinase Homo sapiens 64-68 26655341-2 2015 Previous mechanistic studies have shown that itraconazole inhibits the mechanistic target of rapamycin (mTOR) signaling pathway, which is known to be a critical regulator of endothelial cell function and angiogenesis. Itraconazole 45-57 mechanistic target of rapamycin kinase Homo sapiens 71-102 26655341-2 2015 Previous mechanistic studies have shown that itraconazole inhibits the mechanistic target of rapamycin (mTOR) signaling pathway, which is known to be a critical regulator of endothelial cell function and angiogenesis. Itraconazole 45-57 mechanistic target of rapamycin kinase Homo sapiens 104-108 26655341-4 2015 Here we identify the major target of itraconazole in endothelial cells as the mitochondrial protein voltage-dependent anion channel 1 (VDAC1), which regulates mitochondrial metabolism by controlling the passage of ions and small metabolites through the outer mitochondrial membrane. Itraconazole 37-49 voltage dependent anion channel 1 Homo sapiens 100-133 26655341-4 2015 Here we identify the major target of itraconazole in endothelial cells as the mitochondrial protein voltage-dependent anion channel 1 (VDAC1), which regulates mitochondrial metabolism by controlling the passage of ions and small metabolites through the outer mitochondrial membrane. Itraconazole 37-49 voltage dependent anion channel 1 Homo sapiens 135-140 26655341-6 2015 Inhibition of VDAC1 by itraconazole disrupts mitochondrial metabolism, leading to an increase in the cellular AMP:ATP ratio and activation of the AMP-activated protein kinase (AMPK), an upstream regulator of mTOR. Itraconazole 23-35 voltage dependent anion channel 1 Homo sapiens 14-19 26655341-6 2015 Inhibition of VDAC1 by itraconazole disrupts mitochondrial metabolism, leading to an increase in the cellular AMP:ATP ratio and activation of the AMP-activated protein kinase (AMPK), an upstream regulator of mTOR. Itraconazole 23-35 mechanistic target of rapamycin kinase Homo sapiens 208-212 26655341-7 2015 VDAC1-knockout cells are resistant to AMPK activation and mTOR inhibition by itraconazole, demonstrating that VDAC1 is the mediator of this activity. Itraconazole 77-89 voltage dependent anion channel 1 Homo sapiens 0-5 26655341-7 2015 VDAC1-knockout cells are resistant to AMPK activation and mTOR inhibition by itraconazole, demonstrating that VDAC1 is the mediator of this activity. Itraconazole 77-89 mechanistic target of rapamycin kinase Homo sapiens 58-62 26617583-6 2015 Chemical inhibition of Hsp90 resulted in increased susceptibility of the fungus to itraconazole and micafungin, and decreased its growth in human nails in vitro. Itraconazole 83-95 heat shock protein 90 alpha family class A member 1 Homo sapiens 23-28 26549342-4 2015 Prednisolone 0.5 mg/kg/day and Itraconazole improved his symptoms and IgE levels. Itraconazole 31-43 immunoglobulin heavy constant epsilon Homo sapiens 70-73 26171880-3 2015 Therefore, poly(butyl cyanoacrylate) nanospheres (PBCA-NSP) have been developed as a potential delivery system for transport of itraconazole. Itraconazole 128-140 PBCA Homo sapiens 50-54 26171880-4 2015 One possible application of itraconazole loaded PBCA-NSP could be to treat cryptococcal meningitis. Itraconazole 28-40 PBCA Homo sapiens 48-52 26171880-10 2015 Lyophilization of itraconazole loaded PBCA-NSP was needed to increase the stability of formulations, which was achieved by evaluating different sugar cryoprotectants. Itraconazole 18-30 PBCA Homo sapiens 38-42 26171880-11 2015 In this study, PBCA-NSPs were successfully generated as a delivery system for itraconazole providing a promising approach to improve the therapy of fungal infections of specific organs such as the brain infection cryptococcal meningitis. Itraconazole 78-90 PBCA Homo sapiens 15-19 26045286-5 2015 Presumably, itraconazole by inhibiting CYP3A4 enzyme caused an increase in plasma methylprednisolone levels. Itraconazole 12-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 26710539-6 2015 Amphotericin B, itraconazole and voriconazole were the most potent antifungal drugs against Paracoccidioides spp (CMI: 0.03-1 microg/mL). Itraconazole 16-28 histocompatibility minor 13 Homo sapiens 109-112 26184414-0 2015 Effect of CYP3A5 and ABCB1 polymorphisms on the interaction between tacrolimus and itraconazole in patients with connective tissue disease. Itraconazole 83-95 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 26184414-0 2015 Effect of CYP3A5 and ABCB1 polymorphisms on the interaction between tacrolimus and itraconazole in patients with connective tissue disease. Itraconazole 83-95 ATP binding cassette subfamily B member 1 Homo sapiens 21-26 26184414-1 2015 PURPOSE: The aim of this study was to investigate the effect of itraconazole (ITCZ), a potent inhibitor of CYP3A4 and P-glycoprotein, on the blood concentration 12 h after tacrolimus administration (C 12h) in relation to CYP3A5 6986A>G and ABCB1 3435C>T genotype status in patients with connective tissue disease (CTD). Itraconazole 64-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-113 26184414-1 2015 PURPOSE: The aim of this study was to investigate the effect of itraconazole (ITCZ), a potent inhibitor of CYP3A4 and P-glycoprotein, on the blood concentration 12 h after tacrolimus administration (C 12h) in relation to CYP3A5 6986A>G and ABCB1 3435C>T genotype status in patients with connective tissue disease (CTD). Itraconazole 64-76 ATP binding cassette subfamily B member 1 Homo sapiens 118-132 26184414-1 2015 PURPOSE: The aim of this study was to investigate the effect of itraconazole (ITCZ), a potent inhibitor of CYP3A4 and P-glycoprotein, on the blood concentration 12 h after tacrolimus administration (C 12h) in relation to CYP3A5 6986A>G and ABCB1 3435C>T genotype status in patients with connective tissue disease (CTD). Itraconazole 64-76 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 221-227 26184414-1 2015 PURPOSE: The aim of this study was to investigate the effect of itraconazole (ITCZ), a potent inhibitor of CYP3A4 and P-glycoprotein, on the blood concentration 12 h after tacrolimus administration (C 12h) in relation to CYP3A5 6986A>G and ABCB1 3435C>T genotype status in patients with connective tissue disease (CTD). Itraconazole 64-76 ATP binding cassette subfamily B member 1 Homo sapiens 243-248 25907295-0 2015 Itraconazole and clarithromycin inhibit P-glycoprotein activity in primary human sinonasal epithelial cells. Itraconazole 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 40-54 25907295-9 2015 RESULTS: Both itraconazole and clarithromycin demonstrated a dose-response curve for P-gp inhibition similar to that of Zosuquidar. Itraconazole 14-26 ATP binding cassette subfamily B member 1 Homo sapiens 85-89 26126827-5 2015 Moreover calcitriol strongly synergizes with itraconazole (ITZ) in Smo inhibition, which did not result from elevated calcitriol bioavailability due to ITZ-mediated 24-hydroxylase inhibition but rather from a direct interaction of the compounds at the level of Smo. Itraconazole 45-57 smoothened, frizzled class receptor Homo sapiens 67-70 26126827-5 2015 Moreover calcitriol strongly synergizes with itraconazole (ITZ) in Smo inhibition, which did not result from elevated calcitriol bioavailability due to ITZ-mediated 24-hydroxylase inhibition but rather from a direct interaction of the compounds at the level of Smo. Itraconazole 45-57 smoothened, frizzled class receptor Homo sapiens 261-264 26126827-5 2015 Moreover calcitriol strongly synergizes with itraconazole (ITZ) in Smo inhibition, which did not result from elevated calcitriol bioavailability due to ITZ-mediated 24-hydroxylase inhibition but rather from a direct interaction of the compounds at the level of Smo. Itraconazole 59-62 smoothened, frizzled class receptor Homo sapiens 67-70 26126827-5 2015 Moreover calcitriol strongly synergizes with itraconazole (ITZ) in Smo inhibition, which did not result from elevated calcitriol bioavailability due to ITZ-mediated 24-hydroxylase inhibition but rather from a direct interaction of the compounds at the level of Smo. Itraconazole 59-62 smoothened, frizzled class receptor Homo sapiens 261-264 26065977-2 2015 Recently, it has been discovered that itraconazole, a widely used systemic antifungal drug, has an effect on cell morphology, acting as an inhibitor of the morphogen Sonic Hedgehog (Shh) and of the mammalian target of rapamycin mTOR pathways. Itraconazole 38-50 sonic hedgehog signaling molecule Homo sapiens 166-180 26065977-2 2015 Recently, it has been discovered that itraconazole, a widely used systemic antifungal drug, has an effect on cell morphology, acting as an inhibitor of the morphogen Sonic Hedgehog (Shh) and of the mammalian target of rapamycin mTOR pathways. Itraconazole 38-50 sonic hedgehog signaling molecule Homo sapiens 182-185 26065977-2 2015 Recently, it has been discovered that itraconazole, a widely used systemic antifungal drug, has an effect on cell morphology, acting as an inhibitor of the morphogen Sonic Hedgehog (Shh) and of the mammalian target of rapamycin mTOR pathways. Itraconazole 38-50 mechanistic target of rapamycin kinase Homo sapiens 228-232 26065977-5 2015 Our results show for the first time a strong alteration of neurons morphology and an inhibitory effect of differentiation by itraconazole, probably due to cholesterol trafficking reduction, mTOR and Shh pathways inhibition. Itraconazole 125-137 mechanistic target of rapamycin kinase Mus musculus 190-194 26065977-5 2015 Our results show for the first time a strong alteration of neurons morphology and an inhibitory effect of differentiation by itraconazole, probably due to cholesterol trafficking reduction, mTOR and Shh pathways inhibition. Itraconazole 125-137 sonic hedgehog Mus musculus 199-202 26124377-1 2015 BACKGROUND: We evaluated chemotherapy with itraconazole (a common anti-fungal agent that is a potent inhibitor of the Hedgehog pathway, P-glycoprotein, and angiogenesis) for treating progressive pancreatic cancer. Itraconazole 43-55 ATP binding cassette subfamily B member 1 Homo sapiens 136-150 26071720-2 2015 The pressure coefficients of the glass transition temperature (dT(g)/dp) for itraconazole and ketoconazole were determined to be equal to 183 and 228 K/GPa, respectively. Itraconazole 77-89 glycophorin A (MNS blood group) Homo sapiens 152-155 26071720-3 2015 However, for itraconazole, the additional transition to the nematic phase was observed and characterized by the pressure coefficient dT(n)/dp = 258 K/GPa. Itraconazole 13-25 glycophorin A (MNS blood group) Homo sapiens 150-153 25907295-10 2015 The respective maximal inhibitory concentrations of Zosuquidar, itraconazole, and clarithromycin prior to induction of cytotoxicity were 0.31, 3.13, and 1.56 muM, respectively, as demonstrated by a statistically significant increase in total intracellular fluorescence (p < 0.05 in all groups). Itraconazole 64-76 latexin Homo sapiens 158-161 25907295-11 2015 CONCLUSION: Both itraconazole and clarithromycin are capable of inhibiting sinonasal epithelial cell associated P-gp. Itraconazole 17-29 ATP binding cassette subfamily B member 1 Homo sapiens 112-116 25907295-3 2015 Both itraconazole and clarithromycin have also been shown to have P-gp inhibitory properties in other tissues, suggesting a novel explanation for their immunomodulatory effects in CRS. Itraconazole 5-17 ATP binding cassette subfamily B member 1 Homo sapiens 66-70 25907295-7 2015 A dose-response curve was generated for itraconazole and clarithromycin (maximal concentration 100 muM) and compared to that of Zosuquidar, a highly specific known P-gp inhibitor. Itraconazole 40-52 latexin Homo sapiens 99-102 25515245-7 2015 The interaction between 3A3 and 3A4 with itraconazole proved to be synergistic and indifferent, respectively. Itraconazole 41-53 DNA segment, 3a4 Mus musculus 32-35 25640182-0 2015 Itraconazole inhibits enterovirus replication by targeting the oxysterol-binding protein. Itraconazole 0-12 oxysterol binding protein Homo sapiens 63-88 24952675-14 2014 Itraconazole may induce a resistant hypertension with low renin. Itraconazole 0-12 renin Homo sapiens 58-63 26736983-1 2015 The mechanism of drug-drug interaction between saquinavir, a protease inhibitor used effectively for HIV/AIDS treatment, and itraconazole, an azole antifungal agent, is hypothesized to involve competitive inhibition at CYP3A4 enzyme, an important drug metabolizing enzyme in humans. Itraconazole 125-137 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 219-225 26736984-1 2015 BACKGROUND: Concomitant use of simvastatin, a HMG-CoA reductase inhibitor, with a potent CYP3A4 inhibitor, itraconazole, can result in a serious drug-drug interaction induced severe adverse event, rhabdomyolysis. Itraconazole 107-119 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 25216238-8 2014 Possible alternatives to ketoconazole as prototype CYP3A inhibitors include ritonavir and potentially itraconazole, but not clarithromycin. Itraconazole 102-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-56 24905460-5 2014 Functional studies revealed that itraconazole retarded the trafficking of cholesterol from late endosomes and lysosomes to the plasma membrane by reducing the levels of SCP2, resulting in repression of AKT1-MTOR signaling, induction of autophagy, and finally inhibition of cell proliferation. Itraconazole 33-45 sterol carrier protein 2 Homo sapiens 169-173 24905460-5 2014 Functional studies revealed that itraconazole retarded the trafficking of cholesterol from late endosomes and lysosomes to the plasma membrane by reducing the levels of SCP2, resulting in repression of AKT1-MTOR signaling, induction of autophagy, and finally inhibition of cell proliferation. Itraconazole 33-45 AKT serine/threonine kinase 1 Homo sapiens 202-206 24905460-5 2014 Functional studies revealed that itraconazole retarded the trafficking of cholesterol from late endosomes and lysosomes to the plasma membrane by reducing the levels of SCP2, resulting in repression of AKT1-MTOR signaling, induction of autophagy, and finally inhibition of cell proliferation. Itraconazole 33-45 mechanistic target of rapamycin kinase Homo sapiens 207-211 25385095-8 2015 We then characterized 19 distinct ERG11 alleles by introducing them into the wild-type azole-susceptible C. albicans SC5314 strain and testing them for susceptibilities to FLC, itraconazole (ITC), and voriconazole (VRC). Itraconazole 191-194 cytochrome P450 lanosterol 14-alpha -demethylase Candida albicans SC5314 34-39 24495175-0 2015 Itraconazole inhibits TNF-alpha-induced CXCL10 expression in oral fibroblasts. Itraconazole 0-12 tumor necrosis factor Homo sapiens 22-31 24495175-0 2015 Itraconazole inhibits TNF-alpha-induced CXCL10 expression in oral fibroblasts. Itraconazole 0-12 C-X-C motif chemokine ligand 10 Homo sapiens 40-46 24495175-3 2015 We examined the anti-inflammatory potential of ICZ against TNF-alpha-induced chemokines in oral fibroblasts. Itraconazole 47-50 tumor necrosis factor Homo sapiens 59-68 24495175-4 2015 MATERIALS AND METHODS: We investigated the effects of ICZ on mRNA expressions of various TNF-alpha-induced chemokines in immortalized oral keratinocytes (RT7) and oral fibroblasts (GT1) using quantitative PCR analysis. Itraconazole 54-57 tumor necrosis factor Homo sapiens 89-98 24495175-5 2015 Subsequently, the effects of ICZ and fluconazole (FLZ) on TNF-alpha-induced CXCL10 proteins in GT1 and primary fibroblasts were examined using enzyme-linked immunosorbent assays (ELISA). Itraconazole 29-32 tumor necrosis factor Homo sapiens 58-67 24495175-11 2015 CONCLUSION: ICZ may be useful as therapy for Th1-mediated oral inflammatory disease. Itraconazole 12-15 negative elongation factor complex member C/D Homo sapiens 45-48 24972669-10 2014 Here, it down-regulates vitamin D receptor expression which following itraconazole therapy is rescued concurrent with decreased Th2 cytokine (IL-5 and IL-13) concentrations in the CF airway. Itraconazole 70-82 vitamin D receptor Homo sapiens 24-42 25106415-0 2014 Clinical CYP3A inhibitor alternatives to ketoconazole, clarithromycin and itraconazole, are not transported into the liver by hepatic organic anion transporting polypeptides and organic cation transporter 1. Itraconazole 74-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 9-14 25106415-1 2014 Ketoconazole is no longer available for clinical determination of worst-case victim drug-drug interaction (DDI) potential for cytochrome P450 3A (CYP3A)-substrate drugs; clarithromycin and itraconazole are the proposed replacements. Itraconazole 189-201 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-151 25106415-3 2014 At present, transport of clarithromycin, itraconazole, and hydroxyitraconazole by hepatic organic anion transporting polypeptides (OATPs) and organic cation transporter 1 (OCT1) was examined in vitro and in vivo. Itraconazole 41-53 solute carrier family 22 member 1 Homo sapiens 172-176 25106415-4 2014 As for ketoconazole, uptake of clarithromycin, itraconazole, and hydroxyitraconazole into OATP1B1, OATP1B3, OATP2B1, and OCT1 expressing human embryonic kidney 293 (HEK293) cells was not greater than in vector controls. Itraconazole 47-59 solute carrier organic anion transporter family member 1B1 Homo sapiens 90-97 25359648-7 2014 However, patients taking anticoagulants or cytochrome P450 3A4 substrates (such as clarithromycin, erythromycin, ketoconazole, itraconazole, midazolam and triazolam) in addition to specific vitamin or mineral supplements (vitamins D, E, K, calcium, fluoride, iron, magnesium, selenium or zinc) may face additional challenges. Itraconazole 127-139 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-62 24212378-4 2014 From a set of potential P-gp inhibitors, clarithromycin, cyclosporin A, itraconazole, ketoconazole, quinidine, and ritonavir inhibited P-gp-mediated transport of dabigatran etexilate over a concentration range that may hypothetically occur in the intestine. Itraconazole 72-84 ATP binding cassette subfamily B member 1 Homo sapiens 24-28 24405193-0 2014 Longitudinal monitoring of CYP3A activity in patients receiving 3 cycles of itraconazole pulse therapy for onychomycosis. Itraconazole 76-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-32 24405193-1 2014 WHAT IS KNOWN AND OBJECTIVE: Itraconazole, a CYP3A inhibitor, is used for the treatment for onychomycosis with a three-cycle pulse therapy over 3 months, but its effects on in vivo CYP3A activity during the entire course remain unknown. Itraconazole 29-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-50 24405193-1 2014 WHAT IS KNOWN AND OBJECTIVE: Itraconazole, a CYP3A inhibitor, is used for the treatment for onychomycosis with a three-cycle pulse therapy over 3 months, but its effects on in vivo CYP3A activity during the entire course remain unknown. Itraconazole 29-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 181-186 24405193-5 2014 WHAT IS NEW AND CONCLUSION: The inhibitory effect of itraconazole pulse therapy on the in vivo CYP3A activity appears clinically relevant at the end of each cycle, but the inhibition resolves, on average, within 3 weeks. Itraconazole 53-65 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-100 24386966-13 2014 Co-administration of itraconazole and indomethacin as P-gp and MRP2 inhibitors, respectively revealed the potential of S-SNEDDS in reducing the efflux activities. Itraconazole 21-33 ATP binding cassette subfamily B member 1 Homo sapiens 54-58 24386966-13 2014 Co-administration of itraconazole and indomethacin as P-gp and MRP2 inhibitors, respectively revealed the potential of S-SNEDDS in reducing the efflux activities. Itraconazole 21-33 ATP binding cassette subfamily C member 2 Homo sapiens 63-67 24599432-6 2014 Voriconazole was replaced with itraconazole, and after 3 weeks, the patient stopped complaining of bone pain concomitant with the decrease in ALP. Itraconazole 31-43 alkaline phosphatase, placental Homo sapiens 142-145 24212378-4 2014 From a set of potential P-gp inhibitors, clarithromycin, cyclosporin A, itraconazole, ketoconazole, quinidine, and ritonavir inhibited P-gp-mediated transport of dabigatran etexilate over a concentration range that may hypothetically occur in the intestine. Itraconazole 72-84 ATP binding cassette subfamily B member 1 Homo sapiens 135-139 24114622-10 2013 Moreover, concomitant use with strong CYP3A4 inhibitors (such as ketoconazole, itraconazole, clarithromycin, ritonavir, telithromycin, etc.) Itraconazole 79-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 24471457-14 2014 The antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine and amorolfine may suppress the M. restricta-induced production of CXCL10 by inhibiting STAT1 through an increase in 15d-PGJ2 production in keratinocytes. Itraconazole 17-29 C-X-C motif chemokine ligand 10 Homo sapiens 150-156 24471457-14 2014 The antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine and amorolfine may suppress the M. restricta-induced production of CXCL10 by inhibiting STAT1 through an increase in 15d-PGJ2 production in keratinocytes. Itraconazole 17-29 signal transducer and activator of transcription 1 Homo sapiens 171-176 24127168-2 2013 Cohort data were used to determine whether primary prophylaxis with 100 mg itraconazole for patients with CD4 counts < 150/mm(3) was cost-effective with different scenarios. Itraconazole 75-87 CD4 molecule Homo sapiens 106-109 24471457-10 2014 The antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine and amorolfine suppressed M. restricta extract-induced CXCL10 mRNA and protein expression and STAT1 activity and phosphorylation. Itraconazole 17-29 C-X-C motif chemokine ligand 10 Homo sapiens 138-144 24471457-10 2014 The antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine and amorolfine suppressed M. restricta extract-induced CXCL10 mRNA and protein expression and STAT1 activity and phosphorylation. Itraconazole 17-29 signal transducer and activator of transcription 1 Homo sapiens 177-182 25429674-2 2014 In in vitro interaction studies, itraconazole, ketoconazole, and miconazole were found to have higher inhibitory effects on cytochrome P450 (P450 or CYP) 3A4 and 3A5 activities than the other azoles or echinocandins did. Itraconazole 33-45 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 141-157 25429674-3 2014 Fluconazole, itraconazole, and voriconazole were relatively less potent inhibitors of CYP3A5 than of CYP3A4. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 86-92 25429674-3 2014 Fluconazole, itraconazole, and voriconazole were relatively less potent inhibitors of CYP3A5 than of CYP3A4. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-107 25429674-4 2014 The inhibitory effects of fluconazole, itraconazole, ketoconazole, and voriconazole against CYP3A4 and CYP3A5 seemed to be correlated with their dissociation constants for CYP51 (lanosterol 14alpha-demethylase) from Candida albicans. Itraconazole 39-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 25429674-4 2014 The inhibitory effects of fluconazole, itraconazole, ketoconazole, and voriconazole against CYP3A4 and CYP3A5 seemed to be correlated with their dissociation constants for CYP51 (lanosterol 14alpha-demethylase) from Candida albicans. Itraconazole 39-51 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 103-109 25429674-5 2014 In in vivo pharmacokinetic studies, itraconazole was found to be a potent clinically important inhibitor of CYP3A4/5 substrates, and fluconazole and voriconazole increased the blood/plasma concentrations of not only CYP3A4/5 substrates but also CYP2C9 substrates. Itraconazole 36-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 108-114 25429674-5 2014 In in vivo pharmacokinetic studies, itraconazole was found to be a potent clinically important inhibitor of CYP3A4/5 substrates, and fluconazole and voriconazole increased the blood/plasma concentrations of not only CYP3A4/5 substrates but also CYP2C9 substrates. Itraconazole 36-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 216-222 25429674-5 2014 In in vivo pharmacokinetic studies, itraconazole was found to be a potent clinically important inhibitor of CYP3A4/5 substrates, and fluconazole and voriconazole increased the blood/plasma concentrations of not only CYP3A4/5 substrates but also CYP2C9 substrates. Itraconazole 36-48 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 245-251 24484539-5 2014 Among the substrates that are preferably metabolized by CYP3A4, including carebastine, itraconazole, haloperidol, and fluvastatin, the former three compounds were found to closely dock to the heme region of CYP3A4 but not to that of CYP3A5. Itraconazole 87-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 24484539-5 2014 Among the substrates that are preferably metabolized by CYP3A4, including carebastine, itraconazole, haloperidol, and fluvastatin, the former three compounds were found to closely dock to the heme region of CYP3A4 but not to that of CYP3A5. Itraconazole 87-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 207-213 24484539-5 2014 Among the substrates that are preferably metabolized by CYP3A4, including carebastine, itraconazole, haloperidol, and fluvastatin, the former three compounds were found to closely dock to the heme region of CYP3A4 but not to that of CYP3A5. Itraconazole 87-99 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 233-239 23598928-3 2013 Additional therapy with itraconazole leads to the decrease of total IgE to the limits recommended for proper omalizumab dosing (30-1500 kUA/l). Itraconazole 24-36 immunoglobulin heavy constant epsilon Homo sapiens 68-71 23688403-10 2013 The antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine, and amorolfine suppressed the secretion and mRNA expression of TSLP, NF-kappaB activity, and IkappaBalpha degradation induced by poly I:C plus IL-4. Itraconazole 17-29 thymic stromal lymphopoietin Homo sapiens 147-151 23688403-10 2013 The antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine, and amorolfine suppressed the secretion and mRNA expression of TSLP, NF-kappaB activity, and IkappaBalpha degradation induced by poly I:C plus IL-4. Itraconazole 17-29 NFKB inhibitor alpha Homo sapiens 177-189 23688403-10 2013 The antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine, and amorolfine suppressed the secretion and mRNA expression of TSLP, NF-kappaB activity, and IkappaBalpha degradation induced by poly I:C plus IL-4. Itraconazole 17-29 interleukin 4 Homo sapiens 227-231 23688403-14 2013 CONCLUSIONS: Antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine, and amorolfine may suppress poly I:C plus IL-4-induced production of TSLP by inhibiting NF-kappaB via increasing 15d-PGJ2 production in keratinocytes. Itraconazole 26-38 interleukin 4 Homo sapiens 135-139 23688403-14 2013 CONCLUSIONS: Antimycotics itraconazole, ketoconazole, luliconazole, terbinafine, butenafine, and amorolfine may suppress poly I:C plus IL-4-induced production of TSLP by inhibiting NF-kappaB via increasing 15d-PGJ2 production in keratinocytes. Itraconazole 26-38 thymic stromal lymphopoietin Homo sapiens 162-166 23598928-4 2013 Itraconazole, used as bridge therapy, provided us the opportunity to start anti-IgE treatment in a patient with high levels of total IgE, beyond the upper limits recommended for proper prescription of omalizumab. Itraconazole 0-12 immunoglobulin heavy constant epsilon Homo sapiens 80-83 23598928-4 2013 Itraconazole, used as bridge therapy, provided us the opportunity to start anti-IgE treatment in a patient with high levels of total IgE, beyond the upper limits recommended for proper prescription of omalizumab. Itraconazole 0-12 immunoglobulin heavy constant epsilon Homo sapiens 133-136 23462027-8 2013 Other antibiotics that are strong CYP3A4 inhibitors include itraconazole and telithromycin, whereas erythromycin and fluconazole are moderate inhibitors of the isoenzyme CYP3A4. Itraconazole 60-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 23099620-1 2013 PURPOSE: We assessed possible drug interactions of tramadol given concomitantly with the potent CYP2B6 inhibitor ticlopidine, alone or together with the potent CYP3A4 and P-glycoprotein inhibitor itraconazole. Itraconazole 196-208 ATP binding cassette subfamily B member 1 Homo sapiens 171-185 23291299-0 2013 Itraconazole and arsenic trioxide inhibit Hedgehog pathway activation and tumor growth associated with acquired resistance to smoothened antagonists. Itraconazole 0-12 smoothened, frizzled class receptor Mus musculus 126-136 23089896-5 2013 Coadministration of the inhibitor itraconazole reduced the skin and plasma concentrations of Rho123 in the wild-type mice, but not in mdr1a/1b/bcrp-/- mice, and a marked decrease of Rho123 concentration was seen in the dermis, demonstrating that the functional activities of these transporters can be modulated in vivo. Itraconazole 34-46 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 134-139 23139378-4 2013 The plasma concentration profiles of repaglinide were then analyzed by a PBPK model, together with those of the inhibitors, assuming a competitive inhibition of CYP3A4 by itraconazole, mechanism-based inhibition of CYP2C8 by gemfibrozil glucuronide, and inhibition of organic anion transporting polypeptide (OATP) 1B1 by gemfibrozil and its glucuronide. Itraconazole 171-183 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-167 23291299-4 2013 Here, we report that itraconazole and arsenic trioxide, two agents in clinical use that inhibit Hedgehog signaling by mechanisms distinct from that of current Smoothened antagonists, retain inhibitory activity in vitro in the context of all reported resistance-conferring Smoothened mutants and GLI2 overexpression. Itraconazole 21-33 smoothened, frizzled class receptor Mus musculus 159-169 23291299-4 2013 Here, we report that itraconazole and arsenic trioxide, two agents in clinical use that inhibit Hedgehog signaling by mechanisms distinct from that of current Smoothened antagonists, retain inhibitory activity in vitro in the context of all reported resistance-conferring Smoothened mutants and GLI2 overexpression. Itraconazole 21-33 smoothened, frizzled class receptor Mus musculus 272-282 23291299-4 2013 Here, we report that itraconazole and arsenic trioxide, two agents in clinical use that inhibit Hedgehog signaling by mechanisms distinct from that of current Smoothened antagonists, retain inhibitory activity in vitro in the context of all reported resistance-conferring Smoothened mutants and GLI2 overexpression. Itraconazole 21-33 GLI-Kruppel family member GLI2 Mus musculus 295-299 23291299-5 2013 Itraconazole and arsenic trioxide, alone or in combination, inhibit the growth of medulloblastoma and basal cell carcinoma in vivo, and prolong survival of mice with intracranial drug-resistant SMO(D477G) medulloblastoma. Itraconazole 0-12 smoothened, frizzled class receptor Mus musculus 194-197 23419354-2 2013 Pretreatment with itraconazole (ICZ, P-gp inhibitor, 50 mg/kg) for 30 min before oral administration of NDL (10 mg/kg) significantly increased the area under the plasma concentration-time curve (AUC0- )of NDL by 1.7-fold compared with control. Itraconazole 18-30 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 37-41 23054991-1 2012 Cocrystals of itraconazole, an antifungal drug with poor bioavailability, and succinic acid, a water-soluble dicarboxylic acid, were formed by gas antisolvent (GAS) cocrystallization using pressurized CO(2) to improve itraconazole dissolution. Itraconazole 14-26 gastrin Homo sapiens 143-146 23729559-6 2013 RESULTS: Mean IC50 values of ketoconazole, itraconazole and verapamil were 0.056, 0.061 and 23 muM (conventional method) compared to 0.05, 0.057 and 26 muM (column-switching method), respectively. Itraconazole 43-55 latexin Homo sapiens 95-98 22894166-0 2013 Improved antifungal activity of itraconazole-loaded PEG/PLA nanoparticles. Itraconazole 32-44 progestagen associated endometrial protein Homo sapiens 52-55 22894166-1 2013 Poly(ethylene glycol)/polylactic acid (PEG/PLA) nanoparticles (NPs) containing the hydrophobic antifungal itraconazole (ITZ) were developed to provide a controlled release pattern of ITZ as well as to improve its aqueous dispersibility and hence enhance its antifungal action. Itraconazole 106-118 progestagen associated endometrial protein Homo sapiens 39-42 22894166-1 2013 Poly(ethylene glycol)/polylactic acid (PEG/PLA) nanoparticles (NPs) containing the hydrophobic antifungal itraconazole (ITZ) were developed to provide a controlled release pattern of ITZ as well as to improve its aqueous dispersibility and hence enhance its antifungal action. Itraconazole 120-123 progestagen associated endometrial protein Homo sapiens 39-42 23054991-1 2012 Cocrystals of itraconazole, an antifungal drug with poor bioavailability, and succinic acid, a water-soluble dicarboxylic acid, were formed by gas antisolvent (GAS) cocrystallization using pressurized CO(2) to improve itraconazole dissolution. Itraconazole 218-230 gastrin Homo sapiens 143-146 23054991-1 2012 Cocrystals of itraconazole, an antifungal drug with poor bioavailability, and succinic acid, a water-soluble dicarboxylic acid, were formed by gas antisolvent (GAS) cocrystallization using pressurized CO(2) to improve itraconazole dissolution. Itraconazole 218-230 gastrin Homo sapiens 160-163 23054991-6 2012 The dissolution profile of itraconazole was significantly enhanced through GAS cocrystallization with succinic acid, achieving over 90% dissolution in less than 2 h. The cocrystals appeared stable against thermal stress for up to 4 weeks under accelerated stability conditions, showing only moderate decreases in their degree of crystallinity but no change in their crystalline structure. Itraconazole 27-39 gastrin Homo sapiens 75-78 23054991-1 2012 Cocrystals of itraconazole, an antifungal drug with poor bioavailability, and succinic acid, a water-soluble dicarboxylic acid, were formed by gas antisolvent (GAS) cocrystallization using pressurized CO(2) to improve itraconazole dissolution. Itraconazole 14-26 gastrin Homo sapiens 160-163 21832990-4 2011 The pharmacokinetics of this cocktail was observed at baseline, after an oral dose of 600 mg rifampicin (an inhibitor of OATPs), and after an intravenous dose of 200 mg itraconazole (a CYP3A4 inhibitor). Itraconazole 169-181 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 185-191 23175341-6 2012 The purpose of the study is to evaluate the levels of selected inflammatory cytokines, IL-2, IL-4, IFN-gamma and TNF-alpha, in the serum after treatment with itraconazole. Itraconazole 158-170 interleukin 2 Homo sapiens 87-91 23175341-6 2012 The purpose of the study is to evaluate the levels of selected inflammatory cytokines, IL-2, IL-4, IFN-gamma and TNF-alpha, in the serum after treatment with itraconazole. Itraconazole 158-170 interleukin 4 Homo sapiens 93-97 23175341-6 2012 The purpose of the study is to evaluate the levels of selected inflammatory cytokines, IL-2, IL-4, IFN-gamma and TNF-alpha, in the serum after treatment with itraconazole. Itraconazole 158-170 interferon gamma Homo sapiens 99-108 23175341-6 2012 The purpose of the study is to evaluate the levels of selected inflammatory cytokines, IL-2, IL-4, IFN-gamma and TNF-alpha, in the serum after treatment with itraconazole. Itraconazole 158-170 tumor necrosis factor Homo sapiens 113-122 22564244-6 2012 We found that itraconazole inhibits angiogenesis markers such as VEGF, AAMP and e-NOS. Itraconazole 14-26 angio associated migratory cell protein Homo sapiens 71-75 22564244-6 2012 We found that itraconazole inhibits angiogenesis markers such as VEGF, AAMP and e-NOS. Itraconazole 14-26 nitric oxide synthase 3 Homo sapiens 80-85 22564244-7 2012 mTOR and ERK1/2 phosphorylation as well as the expression of Gli1, one of the main controllers of the Shh pathway, were also inhibited by itraconazole. Itraconazole 138-150 mechanistic target of rapamycin kinase Homo sapiens 0-4 22564244-7 2012 mTOR and ERK1/2 phosphorylation as well as the expression of Gli1, one of the main controllers of the Shh pathway, were also inhibited by itraconazole. Itraconazole 138-150 mitogen-activated protein kinase 3 Homo sapiens 9-15 22564244-7 2012 mTOR and ERK1/2 phosphorylation as well as the expression of Gli1, one of the main controllers of the Shh pathway, were also inhibited by itraconazole. Itraconazole 138-150 GLI family zinc finger 1 Homo sapiens 61-65 22564244-7 2012 mTOR and ERK1/2 phosphorylation as well as the expression of Gli1, one of the main controllers of the Shh pathway, were also inhibited by itraconazole. Itraconazole 138-150 sonic hedgehog signaling molecule Homo sapiens 102-105 22025615-0 2011 The antifungal drug itraconazole inhibits vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, trafficking, and signaling in endothelial cells. Itraconazole 20-32 kinase insert domain receptor Homo sapiens 42-87 22025615-0 2011 The antifungal drug itraconazole inhibits vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, trafficking, and signaling in endothelial cells. Itraconazole 20-32 kinase insert domain receptor Homo sapiens 89-95 22025615-4 2011 We report here that itraconazole significantly inhibited the binding of vascular endothelial growth factor (VEGF) to VEGF receptor 2 (VEGFR2) and that both VEGFR2 and an immediate downstream substrate, phospholipase C gamma1, failed to become activated after VEGF stimulation. Itraconazole 20-32 vascular endothelial growth factor A Homo sapiens 72-106 22025615-4 2011 We report here that itraconazole significantly inhibited the binding of vascular endothelial growth factor (VEGF) to VEGF receptor 2 (VEGFR2) and that both VEGFR2 and an immediate downstream substrate, phospholipase C gamma1, failed to become activated after VEGF stimulation. Itraconazole 20-32 vascular endothelial growth factor A Homo sapiens 108-112 22025615-4 2011 We report here that itraconazole significantly inhibited the binding of vascular endothelial growth factor (VEGF) to VEGF receptor 2 (VEGFR2) and that both VEGFR2 and an immediate downstream substrate, phospholipase C gamma1, failed to become activated after VEGF stimulation. Itraconazole 20-32 kinase insert domain receptor Homo sapiens 117-132 22025615-4 2011 We report here that itraconazole significantly inhibited the binding of vascular endothelial growth factor (VEGF) to VEGF receptor 2 (VEGFR2) and that both VEGFR2 and an immediate downstream substrate, phospholipase C gamma1, failed to become activated after VEGF stimulation. Itraconazole 20-32 kinase insert domain receptor Homo sapiens 134-140 22025615-4 2011 We report here that itraconazole significantly inhibited the binding of vascular endothelial growth factor (VEGF) to VEGF receptor 2 (VEGFR2) and that both VEGFR2 and an immediate downstream substrate, phospholipase C gamma1, failed to become activated after VEGF stimulation. Itraconazole 20-32 kinase insert domain receptor Homo sapiens 156-162 22025615-4 2011 We report here that itraconazole significantly inhibited the binding of vascular endothelial growth factor (VEGF) to VEGF receptor 2 (VEGFR2) and that both VEGFR2 and an immediate downstream substrate, phospholipase C gamma1, failed to become activated after VEGF stimulation. Itraconazole 20-32 phospholipase C gamma 1 Homo sapiens 202-224 22025615-4 2011 We report here that itraconazole significantly inhibited the binding of vascular endothelial growth factor (VEGF) to VEGF receptor 2 (VEGFR2) and that both VEGFR2 and an immediate downstream substrate, phospholipase C gamma1, failed to become activated after VEGF stimulation. Itraconazole 20-32 vascular endothelial growth factor A Homo sapiens 117-121 22025615-8 2011 Repletion of cellular cholesterol levels, which was known to rescue the effects of itraconazole on mTOR and cholesterol trafficking, was also able to restore VEGFR2 glycosylation and signaling. Itraconazole 83-95 mechanistic target of rapamycin kinase Homo sapiens 99-103 22025615-10 2011 We also demonstrated that itraconazole globally reduced poly-N-acetyllactosamine and tetra-antennary complex N-glycans in endothelial cells and induced hypoglycosylation of the epidermal growth factor receptor in a renal cell carcinoma line, suggesting that itraconazole"s effects extend beyond VEGFR2. Itraconazole 26-38 kinase insert domain receptor Homo sapiens 295-301 21896639-5 2011 In vivo, using primary xenograft models of human NSCLC, oral itraconazole showed single-agent growth-inhibitory activity associated with induction of tumor hypoxia-inducible factor 1 alpha expression and marked inhibition of tumor vascularity. Itraconazole 61-73 hypoxia inducible factor 1 subunit alpha Homo sapiens 156-188 21771587-1 2011 BACKGROUND: Itraconazole is a potent inhibitor of CYP3A4 and P-glycoprotein, but not CYP2C9. Itraconazole 12-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 21771587-1 2011 BACKGROUND: Itraconazole is a potent inhibitor of CYP3A4 and P-glycoprotein, but not CYP2C9. Itraconazole 12-24 ATP binding cassette subfamily B member 1 Homo sapiens 61-75 21771587-2 2011 Herein, we report a case study in which the plasma concentration of the CYP2C9 substrate (S)-warfarin, and not the CYP3A4 substrate (R)-warfarin, increased with itraconazole coadministration. Itraconazole 161-173 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 72-78 22088546-6 2011 Intravenous itraconazole was given at a dose of 200 mg bid (intravenous infusion every 12 hours) for the first two days, 200 mg qd for the subsequent 12 days. Itraconazole 12-24 BH3 interacting domain death agonist Homo sapiens 55-58 22088546-7 2011 Sequential oral itraconazole solution was given at a dose of 100 mg bid for 4 weeks. Itraconazole 16-28 BH3 interacting domain death agonist Homo sapiens 68-71 25787325-9 2012 Microemulsion-based itraconazole gel (MBGI) showed better penetration and retention in human skin as well as bovine hoof as compared to commercial preparation (market formulation, MFI). Itraconazole 20-32 MFI Bos taurus 180-183 22106171-0 2012 Stereospecific metabolism of itraconazole by CYP3A4: dioxolane ring scission of azole antifungals. Itraconazole 29-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 22106171-1 2012 Itraconazole (ITZ) is a mixture of four cis-stereoisomers that inhibit CYP3A4 potently and coordinate CYP3A4 heme via the triazole nitrogen. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 22106171-1 2012 Itraconazole (ITZ) is a mixture of four cis-stereoisomers that inhibit CYP3A4 potently and coordinate CYP3A4 heme via the triazole nitrogen. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 22106171-1 2012 Itraconazole (ITZ) is a mixture of four cis-stereoisomers that inhibit CYP3A4 potently and coordinate CYP3A4 heme via the triazole nitrogen. Itraconazole 14-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 22106171-1 2012 Itraconazole (ITZ) is a mixture of four cis-stereoisomers that inhibit CYP3A4 potently and coordinate CYP3A4 heme via the triazole nitrogen. Itraconazole 14-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 21838784-5 2012 Plasma concentrations of montelukast, gemfibrozil, itraconazole and their metabolites were measured up to 72 h. RESULTS: The CYP2C8 inhibitor gemfibrozil increased the AUC(0, ) of montelukast 4.3-fold and its t(1/2) 2.1-fold (P < 0.001). Itraconazole 51-63 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 125-131 21838784-7 2012 The CYP3A4 inhibitor itraconazole had no significant effect on the pharmacokinetic variables of montelukast or its M6 and M4 metabolites, but markedly reduced the AUC and C(max) of M5a and M5b (P < 0.05). Itraconazole 21-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-10 22589709-7 2012 In vitro assays confirmed that five old drugs, namely montelukast, diclofenac, simvastatin, ketoconazole, and itraconazole, showed polypharmacological features on estrogen receptors or dipeptidyl peptidase-IV with half maximal inhibitory or effective concentration ranged from 0.2 to 10 microM. Itraconazole 110-122 dipeptidyl peptidase 4 Homo sapiens 185-208 22119069-15 2011 Some causes have been recently described: familial hyponatraemia via X-linked recessive disease caused by an activating mutation of the vasopressin 2 receptor; and corticotropin insufficiency related to drug interference between some inhaled glucocorticoids and cytochrome p450 inhibitors, such as the antiretroviral drugs and itraconazole, etc. Itraconazole 327-339 arginine vasopressin Homo sapiens 136-147 21936514-0 2011 Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling. Itraconazole 0-12 kinase insert domain receptor Homo sapiens 125-170 21936514-0 2011 Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling. Itraconazole 0-12 kinase insert domain receptor Homo sapiens 172-178 21936514-3 2011 Through this analysis, we have identified analogues with increased potency for inhibiting endothelial cell proliferation and the Hh pathway, as well as VEGFR2 glycosylation that was recently found to be inhibited by itraconazole. Itraconazole 216-228 kinase insert domain receptor Homo sapiens 152-158 22090300-23 2011 Resistance rates for both fluconazole and itraconazole were higher in biofilm-producers (39.5% and 52.6%, respectively), than those of non-producers (10.6% and 29.8%, respectively), representing a statistical significance (p= 0.002 and p= 0.03, respectively) for Candida spp. Itraconazole 42-54 histocompatibility minor 13 Homo sapiens 271-274 22215390-3 2011 AIM: To evaluate the results of oral prophylaxis with high dose itraconazole, 400 mg bid, among patients with adult acute leukemia. Itraconazole 64-76 BH3 interacting domain death agonist Homo sapiens 85-88 21490593-7 2011 Given the significant decrease in CL(f) of 6beta-hydroxycortisone and 6beta-hydroxycortisol after 200-mg and 400-mg single doses of itraconazole, this endogenous probe can be used to detect moderate and potent CYP3A4 inhibition in vivo. Itraconazole 132-144 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 210-216 21716267-1 2011 This study examined drug-drug interactions of oral S-ketamine with the cytochrome P450 (CYP) 2B6 inhibitor ticlopidine and the CYP3A inhibitor itraconazole. Itraconazole 143-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-132 21484807-5 2011 The inhibition of P-gp-mediated efflux of these two fluorescent substrates by several drugs, including quinidine and itraconazole, was found to be substrate- and/or species-dependent. Itraconazole 117-129 ATP binding cassette subfamily B member 1 Homo sapiens 18-22 21420575-8 2011 Moreover, itraconazole and posaconazole are substrates and inhibitors of the transporter protein, P-glycoprotein. Itraconazole 10-22 ATP binding cassette subfamily B member 1 Homo sapiens 98-112 21360715-10 2011 CONCLUSION: Ciprofloxacin decreases the metabolism of itraconazole, most likely through inhibition of CYP3A4. Itraconazole 54-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 21212239-0 2011 Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants. Itraconazole 41-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-91 21212239-3 2011 In this study, we quantitatively investigated the inhibition kinetics of two typical inhibitors, itraconazole (ITCZ) and cimetidine (CMD), on CYP3A4 variants and evaluated whether the genetic variation leads to interindividual differences in the extent of CYP3A4-mediated drug interactions. Itraconazole 97-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 142-148 21212239-3 2011 In this study, we quantitatively investigated the inhibition kinetics of two typical inhibitors, itraconazole (ITCZ) and cimetidine (CMD), on CYP3A4 variants and evaluated whether the genetic variation leads to interindividual differences in the extent of CYP3A4-mediated drug interactions. Itraconazole 111-115 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 142-148 20875690-0 2011 The antimycotic drugs itraconazole and terbinafine hydrochloride induce the production of human beta-defensin-3 in human keratinocytes. Itraconazole 22-34 defensin beta 103B Homo sapiens 96-111 20875690-6 2011 Antimycotics itraconazole and terbinafine hydrochloride increased hBD-3 secretion and mRNA levels in parallel to the enhanced activity of activator protein-1, expression and phosphorylation of activator protein-1 component, c-Fos, but fluconazole was ineffective. Itraconazole 13-25 defensin beta 103B Homo sapiens 66-71 20875690-6 2011 Antimycotics itraconazole and terbinafine hydrochloride increased hBD-3 secretion and mRNA levels in parallel to the enhanced activity of activator protein-1, expression and phosphorylation of activator protein-1 component, c-Fos, but fluconazole was ineffective. Itraconazole 13-25 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 138-157 20875690-6 2011 Antimycotics itraconazole and terbinafine hydrochloride increased hBD-3 secretion and mRNA levels in parallel to the enhanced activity of activator protein-1, expression and phosphorylation of activator protein-1 component, c-Fos, but fluconazole was ineffective. Itraconazole 13-25 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 193-212 20875690-6 2011 Antimycotics itraconazole and terbinafine hydrochloride increased hBD-3 secretion and mRNA levels in parallel to the enhanced activity of activator protein-1, expression and phosphorylation of activator protein-1 component, c-Fos, but fluconazole was ineffective. Itraconazole 13-25 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 224-229 20875690-9 2011 The conditioned medium from itraconazole or terbinafine hydrochloride-treated keratinocytes inhibited the growth of Candida albicans dependently on hBD-3. Itraconazole 28-40 defensin beta 103B Homo sapiens 148-153 20875690-10 2011 These results suggest that itraconazole and terbinafine hydrochloride may enhance c-Fos expression and phosphorylation, activator protein-1 activity and hBD-3 production by increasing prostaglandin D(2) release from keratinocytes. Itraconazole 27-39 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 82-87 20875690-10 2011 These results suggest that itraconazole and terbinafine hydrochloride may enhance c-Fos expression and phosphorylation, activator protein-1 activity and hBD-3 production by increasing prostaglandin D(2) release from keratinocytes. Itraconazole 27-39 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 120-139 20875690-10 2011 These results suggest that itraconazole and terbinafine hydrochloride may enhance c-Fos expression and phosphorylation, activator protein-1 activity and hBD-3 production by increasing prostaglandin D(2) release from keratinocytes. Itraconazole 27-39 defensin beta 103B Homo sapiens 153-158 20400651-0 2011 Itraconazole, a P-glycoprotein and CYP3A4 inhibitor, markedly raises the plasma concentrations and enhances the renin-inhibiting effect of aliskiren. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-41 20400651-0 2011 Itraconazole, a P-glycoprotein and CYP3A4 inhibitor, markedly raises the plasma concentrations and enhances the renin-inhibiting effect of aliskiren. Itraconazole 0-12 renin Homo sapiens 112-117 20400651-5 2011 Plasma renin activity 24 hours after aliskiren intake was 68% lower during the itraconazole phase than during the placebo phase (P = .011). Itraconazole 79-91 renin Homo sapiens 7-12 20400651-6 2011 In conclusion, itraconazole markedly raises the plasma concentrations and enhances the renin-inhibiting effect of aliskiren. Itraconazole 15-27 renin Homo sapiens 87-92 21219398-3 2011 Treatment of patients with strong inducers of CYP3A enzymes, e.g. anti-epileptic drugs, resulted in 10-fold increased concentrations of plasma 4beta-OHC, while treatment with CYP3A inhibitors such as ritonavir or itraconazole resulted in decreased plasma concentrations. Itraconazole 213-225 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-51 21147222-9 2011 Studies using itraconazole, a CYP3A4 inhibitor, established its role in curcumin metabolism. Itraconazole 14-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 21142269-3 2011 The aim of this study was to determine whether inhibition of CYP2D6 alone by paroxetine or inhibition of both CYP2D6 and CYP3A4 by a combination of paroxetine and itraconazole alters the pharmacokinetics of and pharmacological response to intravenous oxycodone. Itraconazole 163-175 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 110-116 21056966-0 2011 Itraconazole-induced cholestasis: involvement of the inhibition of bile canalicular phospholipid translocator MDR3/ABCB4. Itraconazole 0-12 ATP binding cassette subfamily B member 4 Homo sapiens 110-114 21056966-0 2011 Itraconazole-induced cholestasis: involvement of the inhibition of bile canalicular phospholipid translocator MDR3/ABCB4. Itraconazole 0-12 ATP binding cassette subfamily B member 4 Homo sapiens 115-120 21142269-3 2011 The aim of this study was to determine whether inhibition of CYP2D6 alone by paroxetine or inhibition of both CYP2D6 and CYP3A4 by a combination of paroxetine and itraconazole alters the pharmacokinetics of and pharmacological response to intravenous oxycodone. Itraconazole 163-175 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 20739919-0 2010 Accurate prediction of dose-dependent CYP3A4 inhibition by itraconazole and its metabolites from in vitro inhibition data. Itraconazole 59-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 21410294-3 2011 OBJECTIVE: The aim of this study was to investigate the effects of a potent CYP3A4 inducer, rifampicin (Study A), and a potent CYP3A4 inhibitor, itraconazole (Study B), on the pharmacokinetics of a single 300 mg dose of vandetanib in healthy subjects. Itraconazole 145-157 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-133 21410294-18 2011 Vandetanib exposure was increased by about 9% when it was taken in combination with the CYP3A4 inhibitor itraconazole. Itraconazole 105-117 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 21141064-6 2010 Following the administration of micafungin and itraconazole, the cavity lesion diminished in size, and his eosinophil and serum IgE levels decreased. Itraconazole 47-59 immunoglobulin heavy constant epsilon Homo sapiens 128-131 20860661-0 2010 Pharmacokinetic interaction between itraconazole and metformin in rats: competitive inhibition of metabolism of each drug by each other via hepatic and intestinal CYP3A1/2. Itraconazole 36-48 cytochrome P450, family 3, subfamily a, polypeptide 23-polypeptide 1 Rattus norvegicus 163-171 20860661-10 2010 The metabolism of itraconazole and metformin was significantly inhibited by each other via CYP3A1 and 3A2 in rat and 3A4 in human microsomes. Itraconazole 18-30 cytochrome P450, family 3, subfamily a, polypeptide 23-polypeptide 1 Rattus norvegicus 91-105 20739919-2 2010 The aim of this study was to determine the importance of inhibitory metabolites of itraconazole (ITZ) in in vivo cytochrome P450 (CYP) 3A4 inhibition. Itraconazole 83-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 113-138 20739919-2 2010 The aim of this study was to determine the importance of inhibitory metabolites of itraconazole (ITZ) in in vivo cytochrome P450 (CYP) 3A4 inhibition. Itraconazole 97-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 113-138 20739919-6 2010 The metabolites of ITZ were estimated to account for ~50% of the total CYP3A4 inhibition, with the relative contribution increasing with time after ITZ dosing. Itraconazole 19-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 20568249-0 2010 Effect of oral itraconazole on the pharmacokinetics of tacrolimus in a hematopoietic stem cell transplant recipient with CYP3A5*3/*3. Itraconazole 15-27 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 121-127 20952738-4 2010 Itraconazoles dose-dependently increased the production of prostaglandin E2 (PGE2) and tumor necrosis factor-alpha (TNF-alpha) without affecting the production of interleukin-1beta (IL-1beta) and nitric oxide (NO). Itraconazole 0-13 tumor necrosis factor Mus musculus 87-114 20952738-4 2010 Itraconazoles dose-dependently increased the production of prostaglandin E2 (PGE2) and tumor necrosis factor-alpha (TNF-alpha) without affecting the production of interleukin-1beta (IL-1beta) and nitric oxide (NO). Itraconazole 0-13 tumor necrosis factor Mus musculus 116-125 20952738-6 2010 The addition of itraconazoles to LPS-stimulated RAW264.7 cells significantly reduced the production of NO, but rather enhanced the production of PGE2, TNF-alpha and IL-1beta. Itraconazole 16-29 tumor necrosis factor Mus musculus 151-160 20952738-6 2010 The addition of itraconazoles to LPS-stimulated RAW264.7 cells significantly reduced the production of NO, but rather enhanced the production of PGE2, TNF-alpha and IL-1beta. Itraconazole 16-29 interleukin 1 beta Mus musculus 165-173 20621721-0 2010 TGF-beta plasma levels in chromoblastomycosis patients during itraconazole treatment. Itraconazole 62-74 transforming growth factor beta 1 Homo sapiens 0-8 20621721-4 2010 AIM: To quantify Transforming Growth Factor-beta (TGF-beta) plasma levels of CBM patients during itraconazole (ITZ) treatment. Itraconazole 97-109 transforming growth factor beta 1 Homo sapiens 17-48 20621721-4 2010 AIM: To quantify Transforming Growth Factor-beta (TGF-beta) plasma levels of CBM patients during itraconazole (ITZ) treatment. Itraconazole 97-109 transforming growth factor beta 1 Homo sapiens 50-58 20621721-4 2010 AIM: To quantify Transforming Growth Factor-beta (TGF-beta) plasma levels of CBM patients during itraconazole (ITZ) treatment. Itraconazole 111-114 transforming growth factor beta 1 Homo sapiens 17-48 20621721-4 2010 AIM: To quantify Transforming Growth Factor-beta (TGF-beta) plasma levels of CBM patients during itraconazole (ITZ) treatment. Itraconazole 111-114 transforming growth factor beta 1 Homo sapiens 50-58 20575631-10 2010 We further assessed whether a drug interaction between bortezomib and itraconazole and/or lansoprazole had occurred involving the CYP3A4 and/or the CYP2C19 pathways, respectively-resulting in increased severity of the bortezomib-induced peripheral neuropathy and thrombocytopenia-by using the Horn drug interaction probability scale. Itraconazole 70-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 130-136 20642550-5 2010 AIM: The aim of this study was to find out whether the inhibition of cytochrome P450 2D6 (CYP2D6) with paroxetine or concomitant inhibition of CYP2D6 and CYP3A4 with paroxetine and itraconazole, altered the pharmacokinetics and pharmacological response of orally administered oxycodone. Itraconazole 181-193 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 90-96 20642550-5 2010 AIM: The aim of this study was to find out whether the inhibition of cytochrome P450 2D6 (CYP2D6) with paroxetine or concomitant inhibition of CYP2D6 and CYP3A4 with paroxetine and itraconazole, altered the pharmacokinetics and pharmacological response of orally administered oxycodone. Itraconazole 181-193 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 143-149 20642550-5 2010 AIM: The aim of this study was to find out whether the inhibition of cytochrome P450 2D6 (CYP2D6) with paroxetine or concomitant inhibition of CYP2D6 and CYP3A4 with paroxetine and itraconazole, altered the pharmacokinetics and pharmacological response of orally administered oxycodone. Itraconazole 181-193 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 154-160 20575631-10 2010 We further assessed whether a drug interaction between bortezomib and itraconazole and/or lansoprazole had occurred involving the CYP3A4 and/or the CYP2C19 pathways, respectively-resulting in increased severity of the bortezomib-induced peripheral neuropathy and thrombocytopenia-by using the Horn drug interaction probability scale. Itraconazole 70-82 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 148-155 20304965-12 2010 In terms of UGT1A4 metabolism, itraconazole showed kinetic features characteristic of imidazole rather than triazole antifungals. Itraconazole 31-43 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 12-18 20460536-0 2010 Antifungal therapy with itraconazole impairs the anti-lymphoma effects of rituximab by inhibiting recruitment of CD20 to cell surface lipid rafts. Itraconazole 24-36 keratin 20 Homo sapiens 113-117 20460536-6 2010 At the molecular level, recruitment of CD20 to lipid rafts is inhibited in the presence of itraconazole. Itraconazole 91-103 keratin 20 Homo sapiens 39-43 20460536-9 2010 The finding that itraconazole also abolished the cytotoxic effects of other therapeutic antibodies directed against lipid raft-associated molecules (i.e., CD20 and CD52) but not those against the non-raft-associated molecule CD33 further supported our proposed mechanism of action. Itraconazole 17-29 keratin 20 Homo sapiens 155-159 20460536-9 2010 The finding that itraconazole also abolished the cytotoxic effects of other therapeutic antibodies directed against lipid raft-associated molecules (i.e., CD20 and CD52) but not those against the non-raft-associated molecule CD33 further supported our proposed mechanism of action. Itraconazole 17-29 CD52 molecule Homo sapiens 164-168 20497744-1 2010 OBJECTIVE: Itraconazole is a potent inhibitor of cytochrome P450 (CYP) 3A with an elimination half-life of more than 30 hours. Itraconazole 11-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-73 20497744-2 2010 Therefore, itraconazole may cause persistent CYP3A inhibition. Itraconazole 11-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-50 19818023-5 2009 Using gas chromatography, we showed that Sre1 and Stp1 are required for both normoxic and hypoxic ergosterol biosynthesis, and therefore cells lacking SRE1 or STP1 are defective for growth in the presence of low levels of the ergosterol biosynthesis inhibitors, itraconazole and 25-thialanosterol. Itraconazole 262-274 transition protein 1 Homo sapiens 50-54 20385363-3 2010 Mechanistically, itraconazole appears to act on the essential Hh pathway component Smoothened (SMO) by a mechanism distinct from that of cyclopamine and other known SMO antagonists, and prevents the ciliary accumulation of SMO normally caused by Hh stimulation. Itraconazole 17-29 smoothened, frizzled class receptor Homo sapiens 83-93 20385363-3 2010 Mechanistically, itraconazole appears to act on the essential Hh pathway component Smoothened (SMO) by a mechanism distinct from that of cyclopamine and other known SMO antagonists, and prevents the ciliary accumulation of SMO normally caused by Hh stimulation. Itraconazole 17-29 smoothened, frizzled class receptor Homo sapiens 95-98 20385363-3 2010 Mechanistically, itraconazole appears to act on the essential Hh pathway component Smoothened (SMO) by a mechanism distinct from that of cyclopamine and other known SMO antagonists, and prevents the ciliary accumulation of SMO normally caused by Hh stimulation. Itraconazole 17-29 smoothened, frizzled class receptor Homo sapiens 165-168 20385363-3 2010 Mechanistically, itraconazole appears to act on the essential Hh pathway component Smoothened (SMO) by a mechanism distinct from that of cyclopamine and other known SMO antagonists, and prevents the ciliary accumulation of SMO normally caused by Hh stimulation. Itraconazole 17-29 smoothened, frizzled class receptor Homo sapiens 165-168 20176935-3 2010 We report that blockade of cholesterol trafficking through lysosome by a newly identified inhibitor of angiogenesis, itraconazole, leads to inhibition of mTOR activity in endothelial cells. Itraconazole 117-129 mechanistic target of rapamycin kinase Homo sapiens 154-158 20176935-4 2010 Inhibition of mTOR by itraconazole but not rapamycin can be partially restored by extracellular cholesterol delivered by cyclodextrin. Itraconazole 22-34 mechanistic target of rapamycin kinase Homo sapiens 14-18 20176935-6 2010 In addition, both the accumulation of cholesterol in the lysosome and inhibition of mTOR caused by itraconazole can be reversed by thapsigarin. Itraconazole 99-111 mechanistic target of rapamycin kinase Homo sapiens 84-88 19954708-1 2009 OBJECTIVE: Itraconazole, a triazole antifungal agent, has been demonstrated to act as an inhibitor of the ligand induced pregnane X receptor-mediated transcriptional regulation of the CYP3A4 gene. Itraconazole 11-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 184-190 19954708-2 2009 Here, we study the potential endogenous serum marker of CYP3A4 activity, 4beta-hydroxycholesterol, during therapy with itraconazole. Itraconazole 119-131 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 19954708-11 2009 CONCLUSIONS: In conclusion, 4beta-hydroxycholesterol appears to be a sensitive endogenous surrogate marker in human serum for inhibition of CYP3A4 by itraconazole. Itraconazole 150-162 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-146 20076952-1 2010 BACKGROUND: The aim of this study was to investigate the effects of the cytochrome P450 3A4 (CYP34A) inhibitor itraconazole on the pharmacokinetics and pharmacodynamics of orally and intravenously administered oxycodone. Itraconazole 111-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-91 20000889-4 2010 OBJECTIVES: To accomplish a semi-mechanistic DDI model for a long-elimination-half-life drug substrate, tesofensine, and the cytochrome P450 (CYP) 3A4 inhibitor itraconazole, and to compare the results of the semi-mechanistic model with the results obtained from the standard NCA approach. Itraconazole 161-173 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-150 20000889-12 2010 Inhibition resulted in reduced clearances and prolonged elimination half-lives for tesofensine and itraconazole: using NCA, the actual study revealed an approximately 9% increase in exposure for the timeframe of the coadministration with itraconazole (the area under the plasma concentration-time curve (AUC) from 0 to 144 hours [AUC(144h)]), and the impact on exposure estimated to infinity (AUC(infinity)) was approximately 26%. Itraconazole 99-111 CEA cell adhesion molecule 4 Homo sapiens 119-122 20000889-12 2010 Inhibition resulted in reduced clearances and prolonged elimination half-lives for tesofensine and itraconazole: using NCA, the actual study revealed an approximately 9% increase in exposure for the timeframe of the coadministration with itraconazole (the area under the plasma concentration-time curve (AUC) from 0 to 144 hours [AUC(144h)]), and the impact on exposure estimated to infinity (AUC(infinity)) was approximately 26%. Itraconazole 238-250 CEA cell adhesion molecule 4 Homo sapiens 119-122 19947891-4 2010 Both in vitro and in vivo studies have demonstrated that both itraconazole and verapamil are potent P-glycoprotein inhibitors. Itraconazole 62-74 ATP binding cassette subfamily B member 1 Homo sapiens 100-114 19947891-7 2010 Co-administration of itraconazole and/or verapamil significantly increased the AUC(0 - 24) of both enantiomers; their influence on the P-glycoprotein-mediated transport of (S)-fexofenadine was greater than that of the (R)-enantiomer. Itraconazole 21-33 ATP binding cassette subfamily B member 1 Homo sapiens 135-149 19455959-1 2009 We report the case of a 75-year-old woman with mucoid impaction of the bronchi (MIB) due to Schizophyllum commune who improved with itraconazole (ITCZ) administration and relapsed after discontinuation of the drug. Itraconazole 132-144 MIB E3 ubiquitin protein ligase 1 Homo sapiens 80-83 19309762-3 2009 Since both itraconazole and hydroxyitraconazole are effective inhibitors of cytochrome P450 (CYP) 3A4 and p-glycoprotein (pgp)-mediated efflux transporters, they have the potential to elicit drug-drug interaction with a number of CYP3A4 and/or pgp substrates. Itraconazole 11-23 ATP binding cassette subfamily B member 1 Homo sapiens 106-120 19309762-3 2009 Since both itraconazole and hydroxyitraconazole are effective inhibitors of cytochrome P450 (CYP) 3A4 and p-glycoprotein (pgp)-mediated efflux transporters, they have the potential to elicit drug-drug interaction with a number of CYP3A4 and/or pgp substrates. Itraconazole 11-23 ATP binding cassette subfamily B member 1 Homo sapiens 122-125 19309762-3 2009 Since both itraconazole and hydroxyitraconazole are effective inhibitors of cytochrome P450 (CYP) 3A4 and p-glycoprotein (pgp)-mediated efflux transporters, they have the potential to elicit drug-drug interaction with a number of CYP3A4 and/or pgp substrates. Itraconazole 11-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 230-236 19309762-3 2009 Since both itraconazole and hydroxyitraconazole are effective inhibitors of cytochrome P450 (CYP) 3A4 and p-glycoprotein (pgp)-mediated efflux transporters, they have the potential to elicit drug-drug interaction with a number of CYP3A4 and/or pgp substrates. Itraconazole 11-23 ATP binding cassette subfamily B member 1 Homo sapiens 244-247 19414590-3 2009 We have found that incubation of macrophages with itraconazole (ICZ), an azole antifungal commonly used in humans, altered both the expression and glycosylation of CD14. Itraconazole 50-62 CD14 molecule Homo sapiens 164-168 19414590-3 2009 We have found that incubation of macrophages with itraconazole (ICZ), an azole antifungal commonly used in humans, altered both the expression and glycosylation of CD14. Itraconazole 64-67 CD14 molecule Homo sapiens 164-168 20209351-8 2009 The Cryptococcus gattii isolate from an HIV-positive patient showed resistance to fluconazole (MIC > or = 256 (1/4)g/ml) and itraconazole (MIC = 3 (1/4)microg/ml). Itraconazole 128-140 CD9 molecule Homo sapiens 142-149 20130764-7 2009 In vitro incubation of hepatocytes with itraconazole revealed significantly lower viability when compared to fluconazole as assessed by lactate dehydrogenase, aspartate aminotransferase and alanine aminotransferase activities. Itraconazole 40-52 glutamic-oxaloacetic transaminase 2 Rattus norvegicus 159-185 20230761-7 2009 A drug-drug interaction study with itraconazole confirmed in vitro metabolic results implicating CYP3A enzymes as the major contributors to in vivo oxidative metabolism. Itraconazole 35-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-102 19025521-0 2008 Itraconazole, a potent inhibitor of P-glycoprotein, moderately increases plasma concentrations of oral morphine. Itraconazole 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 36-50 18725258-2 2008 The distribution of P-gp substrates (rhodamine 123 and itraconazole) to the skin after administration from the epidermal side was lower in P-gp gene knockout (mdr1a/1b(-/-)) mice than that in wild-type mice. Itraconazole 55-67 phosphoglycolate phosphatase Mus musculus 20-24 18725258-2 2008 The distribution of P-gp substrates (rhodamine 123 and itraconazole) to the skin after administration from the epidermal side was lower in P-gp gene knockout (mdr1a/1b(-/-)) mice than that in wild-type mice. Itraconazole 55-67 phosphoglycolate phosphatase Mus musculus 139-143 18725258-2 2008 The distribution of P-gp substrates (rhodamine 123 and itraconazole) to the skin after administration from the epidermal side was lower in P-gp gene knockout (mdr1a/1b(-/-)) mice than that in wild-type mice. Itraconazole 55-67 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 159-164 18725258-3 2008 Coadministration of propranolol, a P-gp inhibitor, decreased the distribution of itraconazole to the skin in wild-type mice, but not in mdr1a/1b(-/-) mice. Itraconazole 81-93 phosphoglycolate phosphatase Mus musculus 35-39 18725258-6 2008 Distribution of itraconazole after intravenous administration, on the other hand, was higher in mdr1a/1b(-/-) mice than that in wild-type mice, suggesting that P-gp transports this drug from the skin to the circulation. Itraconazole 16-28 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 96-101 18725258-6 2008 Distribution of itraconazole after intravenous administration, on the other hand, was higher in mdr1a/1b(-/-) mice than that in wild-type mice, suggesting that P-gp transports this drug from the skin to the circulation. Itraconazole 16-28 phosphoglycolate phosphatase Mus musculus 160-164 19025521-4 2008 The aim of this study was to evaluate whether itraconazole, which is a potent inhibitor of P-glycoprotein and CYP3A4, would change the pharmacokinetics or the pharmacodynamics of oral morphine. Itraconazole 46-58 ATP binding cassette subfamily B member 1 Homo sapiens 91-105 19025521-4 2008 The aim of this study was to evaluate whether itraconazole, which is a potent inhibitor of P-glycoprotein and CYP3A4, would change the pharmacokinetics or the pharmacodynamics of oral morphine. Itraconazole 46-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 19025521-11 2008 CONCLUSIONS: Itraconazole moderately increases plasma concentrations of oral morphine, probably by enhancing its absorption by inhibiting intestinal wall P-glycoprotein. Itraconazole 13-25 ATP binding cassette subfamily B member 1 Homo sapiens 154-168 18755176-2 2008 DESIGN AND METHODS: A representative analyte (itraconazole) was extracted from plasma samples using small quantities of C18-modified ferromagnetic micro-particles. Itraconazole 46-58 Bardet-Biedl syndrome 9 Homo sapiens 120-123 19356088-2 2008 Itraconazole (ITZ) functions as an inhibitor of both the P-gp and CYP3A and is used as a fungistatic/fungicidal agent in human and veterinary medicine. Itraconazole 0-12 phosphoglycolate phosphatase Homo sapiens 57-61 18656535-7 2008 Due to the lower miscibility degree between the longer PEG types and HPMC 2910 E5, the ternary amorphous phase was further separated, leading to a more rapid decrease of the ternary amorphous phase glass transition as a function of PEG and itraconazole weight percentage and hence, itraconazole recrystallization. Itraconazole 240-252 progestagen associated endometrial protein Homo sapiens 55-58 18656535-7 2008 Due to the lower miscibility degree between the longer PEG types and HPMC 2910 E5, the ternary amorphous phase was further separated, leading to a more rapid decrease of the ternary amorphous phase glass transition as a function of PEG and itraconazole weight percentage and hence, itraconazole recrystallization. Itraconazole 240-252 progestagen associated endometrial protein Homo sapiens 232-235 18656535-7 2008 Due to the lower miscibility degree between the longer PEG types and HPMC 2910 E5, the ternary amorphous phase was further separated, leading to a more rapid decrease of the ternary amorphous phase glass transition as a function of PEG and itraconazole weight percentage and hence, itraconazole recrystallization. Itraconazole 282-294 progestagen associated endometrial protein Homo sapiens 55-58 18656535-7 2008 Due to the lower miscibility degree between the longer PEG types and HPMC 2910 E5, the ternary amorphous phase was further separated, leading to a more rapid decrease of the ternary amorphous phase glass transition as a function of PEG and itraconazole weight percentage and hence, itraconazole recrystallization. Itraconazole 282-294 progestagen associated endometrial protein Homo sapiens 232-235 18656535-8 2008 In terms of release, an advantage of the shorter chain length PEG types (2000, 6000) over the longer chain length PEG types (10,000, 20,000) was observed for the polymer blends with 5% of PEG with respect to the binary itraconazole/HPMC 2910 E5 solid dispersion. Itraconazole 219-231 progestagen associated endometrial protein Homo sapiens 62-65 18817631-1 2008 AIM: To evaluate the effects of cyclosporin A and itraconazole, which were used as inhibitors of P-glycoprotein (P-gp) and/or cytochrome P450 (CYP) 3A4 on the pharmacokinetics of atorvastatin in rats. Itraconazole 50-62 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 97-111 18817631-1 2008 AIM: To evaluate the effects of cyclosporin A and itraconazole, which were used as inhibitors of P-glycoprotein (P-gp) and/or cytochrome P450 (CYP) 3A4 on the pharmacokinetics of atorvastatin in rats. Itraconazole 50-62 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 113-117 18630936-8 2008 At a loading of 30 wt %, itraconazole exhibited intermolecular interactions inside the mesopores revealed by UV spectroscopy and endothermic events traced with DSC. Itraconazole 25-37 desmocollin 3 Homo sapiens 160-163 19356088-2 2008 Itraconazole (ITZ) functions as an inhibitor of both the P-gp and CYP3A and is used as a fungistatic/fungicidal agent in human and veterinary medicine. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-71 19356088-2 2008 Itraconazole (ITZ) functions as an inhibitor of both the P-gp and CYP3A and is used as a fungistatic/fungicidal agent in human and veterinary medicine. Itraconazole 14-17 phosphoglycolate phosphatase Homo sapiens 57-61 19356088-2 2008 Itraconazole (ITZ) functions as an inhibitor of both the P-gp and CYP3A and is used as a fungistatic/fungicidal agent in human and veterinary medicine. Itraconazole 14-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-71 18294330-2 2008 Although itraconazole co-administration is known to increase the bioavailability of a racemic mixture of fexofenadine, little is known about the stereoselective inhibition of P-gp activity by itraconazole. Itraconazole 192-204 ATP binding cassette subfamily B member 1 Homo sapiens 175-179 18520601-1 2008 An open-label, clinical pilot study was performed to study the effect of cyclosporine A (CsA) on single-dose pharmacokinetics of itraconazole in patients with a hematologic malignancy. Itraconazole 129-141 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 89-92 18520601-8 2008 In contrast, exposure to OH-itraconazole was significantly increased when itraconazole was coadministered with CsA (median increase of AUC[0-24h] 49%) with significant prolongation of T(max) and T1/2 (median increase of T(max) 37% and T1/2 176%). Itraconazole 28-40 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 111-114 18520601-9 2008 These differences may be the result of variability in affinity of itraconazole, OH-itraconazole, and CsA for the cytochrome P450 3A4 metabolic system and the occurrence of P-glycoprotein polymorphisms. Itraconazole 66-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 113-132 18339815-0 2008 Hydroxyitraconazole, formed during intestinal first-pass metabolism of itraconazole, controls the time course of hepatic CYP3A inhibition and the bioavailability of itraconazole in rats. Itraconazole 7-19 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 121-126 18339815-0 2008 Hydroxyitraconazole, formed during intestinal first-pass metabolism of itraconazole, controls the time course of hepatic CYP3A inhibition and the bioavailability of itraconazole in rats. Itraconazole 71-83 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 121-126 18339815-1 2008 Itraconazole (ITZ) is a substrate of CYP3A and both ITZ and hydroxyitraconazole (OH-ITZ), a major metabolite formed by CYP3A, are potent inhibitors of CYP3A. Itraconazole 0-12 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 37-42 18339815-1 2008 Itraconazole (ITZ) is a substrate of CYP3A and both ITZ and hydroxyitraconazole (OH-ITZ), a major metabolite formed by CYP3A, are potent inhibitors of CYP3A. Itraconazole 0-12 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 119-124 18339815-1 2008 Itraconazole (ITZ) is a substrate of CYP3A and both ITZ and hydroxyitraconazole (OH-ITZ), a major metabolite formed by CYP3A, are potent inhibitors of CYP3A. Itraconazole 0-12 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 119-124 18339815-1 2008 Itraconazole (ITZ) is a substrate of CYP3A and both ITZ and hydroxyitraconazole (OH-ITZ), a major metabolite formed by CYP3A, are potent inhibitors of CYP3A. Itraconazole 14-17 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 37-42 18339815-1 2008 Itraconazole (ITZ) is a substrate of CYP3A and both ITZ and hydroxyitraconazole (OH-ITZ), a major metabolite formed by CYP3A, are potent inhibitors of CYP3A. Itraconazole 14-17 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 119-124 18339815-1 2008 Itraconazole (ITZ) is a substrate of CYP3A and both ITZ and hydroxyitraconazole (OH-ITZ), a major metabolite formed by CYP3A, are potent inhibitors of CYP3A. Itraconazole 14-17 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 119-124 18520601-10 2008 In conclusion, exposure to OH-itraconazole, but not to itraconazole, is increased when itraconazole is coadministered with CsA. Itraconazole 30-42 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 123-126 18520601-11 2008 Although the interaction profile of itraconazole and CsA remains complex, these findings may be of importance in patients in whom monitoring of itraconazole serum levels is warranted, for example, in those with life-threatening fungal infections or in those who receive concurrent cytochrome inducers or inhibitors. Itraconazole 144-156 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 53-56 18294330-3 2008 WHAT THIS STUDY ADDS: This study indicates that the stereoselective pharmacokinetics of fexofenadine are due to P-gp-mediated transport and its stereoselectivity is altered by itraconazole, a an inhibitor of P-gp. Itraconazole 176-188 ATP binding cassette subfamily B member 1 Homo sapiens 112-116 18294330-4 2008 AIMS: The aim of this study was to determine the inhibitory effect of itraconazole, a P-glycoprotein (P-gp) inhibitor, on the stereoselective pharmacokinetics of fexofenadine. Itraconazole 70-82 ATP binding cassette subfamily B member 1 Homo sapiens 86-100 18294330-4 2008 AIMS: The aim of this study was to determine the inhibitory effect of itraconazole, a P-glycoprotein (P-gp) inhibitor, on the stereoselective pharmacokinetics of fexofenadine. Itraconazole 70-82 ATP binding cassette subfamily B member 1 Homo sapiens 102-106 18294330-11 2008 CONCLUSIONS: This study indicates that the stereoselective pharmacokinetics of fexofenadine are due to P-gp-mediated transport and its stereoselectivity is altered by itraconazole, a P-gp inhibitor. Itraconazole 167-179 ATP binding cassette subfamily B member 1 Homo sapiens 103-107 17998298-3 2008 In the present study, we examined effects of azole antimycotics clotrimazole, ketoconazole, econazole, oxiconazole, miconazole, fluconazole, and itraconazole on PXR-mediated expression of CYP3A4. Itraconazole 145-157 nuclear receptor subfamily 1 group I member 2 Homo sapiens 161-164 18218784-8 2008 In conclusion, itraconazole increases the plasma concentrations of imidafenacin by inhibiting CYP3A4. Itraconazole 15-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 94-100 18783297-10 2008 The CRCYP3A4 was calculated for 22 substrates on the basis of the previously reported method from inhibitory DDI studies using a potent CYP3A4 inhibitor such as itraconazole or ketoconazole. Itraconazole 161-173 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 18033783-7 2008 Exposure to fluconazole led to significant increases in GFP-SAP4 and -SAP6 fluorescence in the filaments; itraconazole exposure also significantly increased GFP-SAP4 fluorescence, whereas flucytosine had no effect on any of the constructs. Itraconazole 106-118 Sap4p Saccharomyces cerevisiae S288C 161-165 17495874-0 2008 Contribution of itraconazole metabolites to inhibition of CYP3A4 in vivo. Itraconazole 16-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-64 17495874-6 2008 A 3.9-fold decrease in the hepatic intrinsic clearance of a CYP3A4 substrate was predicted using the average unbound steady-state concentrations (C(ss,ave,u)) and liver microsomal inhibition constants for ITZ, OH-ITZ, keto-ITZ, and ND-ITZ. Itraconazole 212-216 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 17495874-7 2008 Accounting for circulating metabolites of ITZ significantly improved the in vitro to in vivo extrapolation of CYP3A4 inhibition compared to a consideration of ITZ exposure alone. Itraconazole 42-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 17283379-0 2007 Induction of cytochrome P450 1A1 by ketoconazole and itraconazole but not fluconazole in murine and human hepatoma cell lines. Itraconazole 53-65 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 13-32 17923278-0 2007 Induction of the NAD(P)H:quinone oxidoreductase 1 by ketoconazole and itraconazole: a mechanism of cancer chemoprotection. Itraconazole 70-82 NAD(P)H dehydrogenase, quinone 1 Mus musculus 17-49 17923278-3 2007 Therefore, we examined the ability of three structurally different antifungal drugs, ketoconazole (KTZ), itraconazole (ITZ), and fluconazole (FLZ) to induce the expression of NAD(P)H:quinone oxidoreductase 1 (Nqo1), an enzyme known to play an important role in xenobiotic and carcinogen detoxifications. Itraconazole 105-117 NAD(P)H dehydrogenase, quinone 1 Mus musculus 175-207 17923278-3 2007 Therefore, we examined the ability of three structurally different antifungal drugs, ketoconazole (KTZ), itraconazole (ITZ), and fluconazole (FLZ) to induce the expression of NAD(P)H:quinone oxidoreductase 1 (Nqo1), an enzyme known to play an important role in xenobiotic and carcinogen detoxifications. Itraconazole 119-122 NAD(P)H dehydrogenase, quinone 1 Mus musculus 175-207 17518356-11 2007 These results suggest that BCRP could play a significant role in the pharmacokinetic interactions of ketoconazole or itraconazole with BCRP substrate drugs. Itraconazole 117-129 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 27-31 17518356-11 2007 These results suggest that BCRP could play a significant role in the pharmacokinetic interactions of ketoconazole or itraconazole with BCRP substrate drugs. Itraconazole 117-129 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 135-139 17518356-2 2007 The goal of this study was to investigate the interactions of azole antifungal agents, ketoconazole, itraconazole, fluconazole, and voriconazole, with BCRP. Itraconazole 101-113 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 151-155 17518356-4 2007 We found that keotoconazole and itraconazole significantly inhibited BCRP-mediated efflux of PhA at low microM concentrations. Itraconazole 32-44 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 69-73 17518356-4 2007 We found that keotoconazole and itraconazole significantly inhibited BCRP-mediated efflux of PhA at low microM concentrations. Itraconazole 32-44 lamin B receptor Homo sapiens 93-96 17518356-7 2007 Ketoconazole and itraconazole also effectively reversed BCRP-mediated resistance of HEK cells to topotecan. Itraconazole 17-29 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 56-60 17518356-10 2007 Taken together, ketoconazole and itraconazole are BCRP inhibitors, but fluconazole and voriconazole are not. Itraconazole 33-45 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 50-54 17517842-4 2007 Consistent with the role of CYP3A4 in the biotransformation of itraconazole, a substantial degree of variability was observed in the pharmacokinetics of this drug after IV administration. Itraconazole 63-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-34 17725244-7 2007 RESULTS: During itraconazole treatment total cholesterol and LDL-C decreased on average by 12% (p < 0.001) and 17% (p < 0.001), respectively, whereas HDL-C increased by 21% (p < 0.001). Itraconazole 16-28 component of oligomeric golgi complex 2 Homo sapiens 61-66 17725244-9 2007 Incubation of Caco-2 cells in the presence of itraconazole and hydroxyitraconazole for 3 hours resulted in a significant increase in apoA-I concentration in the medium (913 and 412%, respectively) compared with control. Itraconazole 46-58 apolipoprotein A1 Homo sapiens 133-139 17725244-10 2007 CONCLUSION: In addition to its inhibitory effect on cholesterol synthesis, high-dose itraconazole (400 mg/d) causes a significant decrease in serum LDL-C and, in contrast to ketoconazole, a significant increase in HDL-C. Itraconazole 85-97 component of oligomeric golgi complex 2 Homo sapiens 148-153 17472656-2 2007 The comparative effect of the itraconazole (ITZ)-mediated modulation of P-glycoprotein (P-gp) activity on the in vivo kinetic behaviour of ivermectin (IVM) administered by the intravenous (i.v.) Itraconazole 30-42 multidrug resistance protein 1 Ovis aries 72-86 17472656-2 2007 The comparative effect of the itraconazole (ITZ)-mediated modulation of P-glycoprotein (P-gp) activity on the in vivo kinetic behaviour of ivermectin (IVM) administered by the intravenous (i.v.) Itraconazole 30-42 multidrug resistance protein 1 Ovis aries 88-92 17472656-2 2007 The comparative effect of the itraconazole (ITZ)-mediated modulation of P-glycoprotein (P-gp) activity on the in vivo kinetic behaviour of ivermectin (IVM) administered by the intravenous (i.v.) Itraconazole 44-47 multidrug resistance protein 1 Ovis aries 72-86 17472656-2 2007 The comparative effect of the itraconazole (ITZ)-mediated modulation of P-glycoprotein (P-gp) activity on the in vivo kinetic behaviour of ivermectin (IVM) administered by the intravenous (i.v.) Itraconazole 44-47 multidrug resistance protein 1 Ovis aries 88-92 17472656-15 2007 An ITZ-induced reduction on the P-gp efflux activity at the intestinal lining may have accounted for the greater absorption and enhanced systemic availability observed for IVM in the intraruminally treated animals. Itraconazole 3-6 multidrug resistance protein 1 Ovis aries 32-36 17283379-2 2007 Therefore, we examined here the ability of three structurally different antifungal drugs, ketoconazole (KTZ), itraconazole (ITZ), and fluconazole (FLZ) to induce the CYP1A1, an enzyme known to play an important role in chemical activation of xenobiotics to toxic metabolites. Itraconazole 110-122 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 166-172 17283379-2 2007 Therefore, we examined here the ability of three structurally different antifungal drugs, ketoconazole (KTZ), itraconazole (ITZ), and fluconazole (FLZ) to induce the CYP1A1, an enzyme known to play an important role in chemical activation of xenobiotics to toxic metabolites. Itraconazole 124-127 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 166-172 17283379-6 2007 Inhibition studies showed that KTZ and ITZ, in addition to being CYP1A1 inducers, are substrates and competitive inhibitors. Itraconazole 39-42 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 65-71 17432820-5 2007 In attempts to delineate the mechanism of action of itraconazole, we found that human lanosterol 14alpha-demethylase (14DM) is essential for endothelial cell proliferation and may partially mediate the inhibition of endothelial cells by itraconazole. Itraconazole 52-64 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 86-116 17432820-5 2007 In attempts to delineate the mechanism of action of itraconazole, we found that human lanosterol 14alpha-demethylase (14DM) is essential for endothelial cell proliferation and may partially mediate the inhibition of endothelial cells by itraconazole. Itraconazole 237-249 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 86-116 17304149-3 2007 The aim of this study was to examine the effects of itraconazole, a P-glycoprotein inhibitor, on the pharmacokinetics of paroxetine. Itraconazole 52-64 ATP binding cassette subfamily B member 1 Homo sapiens 68-82 17386084-0 2007 Dynamically simulating the interaction of midazolam and the CYP3A4 inhibitor itraconazole using individual coupled whole-body physiologically-based pharmacokinetic (WB-PBPK) models. Itraconazole 77-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 17304149-9 2007 The present study demonstrated that the bioavailability of paroxetine was increased by itraconazole, suggesting a possible involvement of P-glycoprotein in the pharmacokinetics of paroxetine. Itraconazole 87-99 ATP binding cassette subfamily B member 1 Homo sapiens 138-152 17178259-4 2006 Simvastatin, lovastatin, and atorvastatin are metabolized by cytochrome P450 (CYP) 3A4 (simvastatin acid is also metabolized by CYP2C8); their plasma concentrations and risk of myotoxicity are greatly increased by strong inhibitors of CYP3A4 (eg, itraconazole and ritonavir). Itraconazole 247-259 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-86 17484517-5 2007 Clinically established CYP3A4 inhibitors including itraconazole, ketoconazole, erythromycin and clarithromycin inhibited the elimination of IM in HLM. Itraconazole 51-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 23-29 17003527-11 2007 CONCLUSIONS: Itraconazole comedication substantially increases systemic levels of inhaled fluticasone, most likely by inhibiting the cytochrome P450 3A4 enzyme system and thus the clearance of fluticasone. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 133-152 17178259-4 2006 Simvastatin, lovastatin, and atorvastatin are metabolized by cytochrome P450 (CYP) 3A4 (simvastatin acid is also metabolized by CYP2C8); their plasma concentrations and risk of myotoxicity are greatly increased by strong inhibitors of CYP3A4 (eg, itraconazole and ritonavir). Itraconazole 247-259 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 128-134 17022761-0 2006 Fluconazole and itraconazole susceptibilities of Candida spp. Itraconazole 16-28 histocompatibility minor 13 Homo sapiens 57-60 16989930-10 2006 For the inhibition of hCYP51, IC(50) values split into two classes: the newer drugs fluconazole and itraconazole showed little inhibition (> or = 30 microM) while the older drugs were even more potent than the agricultural fungicides, with miconazole being the most potent (0.057 microM). Itraconazole 100-112 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 22-28 17022761-2 2006 This study examined the in vitro susceptibilities to fluconazole and itraconazole of isolates of Candida spp. Itraconazole 69-81 histocompatibility minor 13 Homo sapiens 105-108 16872551-5 2006 The sex-related influence on the itraconazole (ITZ) modulation of P-gp-mediated IVM intestinal transport was also assessed. Itraconazole 33-45 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 66-70 16872551-5 2006 The sex-related influence on the itraconazole (ITZ) modulation of P-gp-mediated IVM intestinal transport was also assessed. Itraconazole 47-50 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 66-70 16556082-7 2006 The systemic azoles, such as ketoconazole, itraconazole, fluconazole and voriconazole, are inhibitors of CYP isoenzymes, such as CYP3A4, CYP2C9 and CYP2C19, to varying degrees. Itraconazole 43-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 16700545-3 2006 However, CYP3A4 also slowly oxidizes the antifungal itraconazole (ITZ) at a site that is approximately 25 A from the triazole nitrogens, suggesting that large antifungal azoles can adopt multiple orientations within the CYP3A4 active site. Itraconazole 52-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 9-15 16700545-3 2006 However, CYP3A4 also slowly oxidizes the antifungal itraconazole (ITZ) at a site that is approximately 25 A from the triazole nitrogens, suggesting that large antifungal azoles can adopt multiple orientations within the CYP3A4 active site. Itraconazole 52-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 220-226 16700545-3 2006 However, CYP3A4 also slowly oxidizes the antifungal itraconazole (ITZ) at a site that is approximately 25 A from the triazole nitrogens, suggesting that large antifungal azoles can adopt multiple orientations within the CYP3A4 active site. Itraconazole 66-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 9-15 16700545-3 2006 However, CYP3A4 also slowly oxidizes the antifungal itraconazole (ITZ) at a site that is approximately 25 A from the triazole nitrogens, suggesting that large antifungal azoles can adopt multiple orientations within the CYP3A4 active site. Itraconazole 66-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 220-226 16556082-7 2006 The systemic azoles, such as ketoconazole, itraconazole, fluconazole and voriconazole, are inhibitors of CYP isoenzymes, such as CYP3A4, CYP2C9 and CYP2C19, to varying degrees. Itraconazole 43-55 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 137-143 16556082-7 2006 The systemic azoles, such as ketoconazole, itraconazole, fluconazole and voriconazole, are inhibitors of CYP isoenzymes, such as CYP3A4, CYP2C9 and CYP2C19, to varying degrees. Itraconazole 43-55 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 148-155 16633141-7 2006 In the presence of itraconazole, subjects with CYP2D6*10/*10 showed 3-fold higher AUC of haloperidol compared to that of placebo pretreated subjects with CYP2D6*1/*1 genotype (21.7 +/- 11.3 vs 66.7 +/- 62.1 ng h/mL; P < 0.05). Itraconazole 19-31 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 47-53 16633141-10 2006 Barnes Akathisia Rating Scale (BARS) of subjects with CYP2D6*10/*10 in the presence of itraconazole pretreatment was significantly higher than that of subjects with CYP2D6*1/*1 genotype in the period of placebo pretreatment. Itraconazole 87-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 54-60 16633141-12 2006 The moderate effect of CYP2D6*10 genotype on the pharmacokinetics and pharmacodynamics of haloperidol seems to be augmented by the presence of itraconazole pretreatment. Itraconazole 143-155 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 23-29 18360572-6 2005 Itraconazole works by inhibiting ergosterol synthesis via cytochrome P-450 (CYP450)-dependent demethylation step. Itraconazole 0-12 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 58-74 16418697-3 2006 In this study, the authors investigated the effects of itraconazole, which is a specific inhibitor of CYP3A4, or tandospirone, which is mainly metabolized by CYP3A4 and is expected to competitively inhibit the activity of this enzyme, on single oral dose pharmacokinetics of perospirone. Itraconazole 55-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 16418697-3 2006 In this study, the authors investigated the effects of itraconazole, which is a specific inhibitor of CYP3A4, or tandospirone, which is mainly metabolized by CYP3A4 and is expected to competitively inhibit the activity of this enzyme, on single oral dose pharmacokinetics of perospirone. Itraconazole 55-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 158-164 18360572-6 2005 Itraconazole works by inhibiting ergosterol synthesis via cytochrome P-450 (CYP450)-dependent demethylation step. Itraconazole 0-12 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 76-82 16141569-1 2005 The effects of five antifungal drugs, fluconazole, itraconazole, micafungin, miconazole, and voriconazole, on cytochrome P450 (CYP) 1A2-mediated 7-ethoxyresorufin O-deethylation, CYP2D6-mediated debrisoquine 4-hydroxylation, and CYP2E1-mediated chlorzoxazone 6-hydroxylation activities in human liver microsomes were compared. Itraconazole 51-63 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 110-135 16321618-2 2005 The aim of this study was to evaluate the effect of itraconazole, a CYP3A inhibitor, on the plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients in relation to CYP2D6 genotype. Itraconazole 52-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-73 16321618-2 2005 The aim of this study was to evaluate the effect of itraconazole, a CYP3A inhibitor, on the plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients in relation to CYP2D6 genotype. Itraconazole 52-64 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 195-201 16321618-7 2005 Itraconazole increased the concentrations of risperidone by 69% (P < .001) and 75% (P < .01) in CYP2D6 extensive and poor metabolizers, respectively. Itraconazole 0-12 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 102-108 16321618-8 2005 In addition, the active moiety (risperidone plus 9-hydroxyrisperidone) also increased similarly, by 71% (P < .001) and 73% (P < .05), respectively, with itraconazole, without a significant difference between CYP2D6 genotypes. Itraconazole 159-171 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 214-220 16321618-11 2005 In addition to CYP2D6, treatment with CYP3A inhibitor(s) including itraconazole may influence clinical symptoms and risperidone side effects. Itraconazole 67-79 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 16205037-4 2005 In in vivo pharmacokinetic studies, it is well known that itraconazole is a potent clinically important inhibitor of the clearance of CYP3A4 substrates, and fluconazole and voriconazole are reported to increase the blood or plasma concentrations of not only midazolam and cyclosporine (CYP3A4 substrates) but also of phenytoin (CYP2C9 substrate) and/or omeprazole (CYP2C19/CYP3A4 substrate). Itraconazole 58-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 134-140 16205037-4 2005 In in vivo pharmacokinetic studies, it is well known that itraconazole is a potent clinically important inhibitor of the clearance of CYP3A4 substrates, and fluconazole and voriconazole are reported to increase the blood or plasma concentrations of not only midazolam and cyclosporine (CYP3A4 substrates) but also of phenytoin (CYP2C9 substrate) and/or omeprazole (CYP2C19/CYP3A4 substrate). Itraconazole 58-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 286-292 16205037-4 2005 In in vivo pharmacokinetic studies, it is well known that itraconazole is a potent clinically important inhibitor of the clearance of CYP3A4 substrates, and fluconazole and voriconazole are reported to increase the blood or plasma concentrations of not only midazolam and cyclosporine (CYP3A4 substrates) but also of phenytoin (CYP2C9 substrate) and/or omeprazole (CYP2C19/CYP3A4 substrate). Itraconazole 58-70 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 328-334 16205037-4 2005 In in vivo pharmacokinetic studies, it is well known that itraconazole is a potent clinically important inhibitor of the clearance of CYP3A4 substrates, and fluconazole and voriconazole are reported to increase the blood or plasma concentrations of not only midazolam and cyclosporine (CYP3A4 substrates) but also of phenytoin (CYP2C9 substrate) and/or omeprazole (CYP2C19/CYP3A4 substrate). Itraconazole 58-70 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 365-372 16205037-4 2005 In in vivo pharmacokinetic studies, it is well known that itraconazole is a potent clinically important inhibitor of the clearance of CYP3A4 substrates, and fluconazole and voriconazole are reported to increase the blood or plasma concentrations of not only midazolam and cyclosporine (CYP3A4 substrates) but also of phenytoin (CYP2C9 substrate) and/or omeprazole (CYP2C19/CYP3A4 substrate). Itraconazole 58-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 286-292 16042675-0 2005 Coadministration of gemfibrozil and itraconazole has only a minor effect on the pharmacokinetics of the CYP2C9 and CYP3A4 substrate nateglinide. Itraconazole 36-48 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 104-110 16042675-0 2005 Coadministration of gemfibrozil and itraconazole has only a minor effect on the pharmacokinetics of the CYP2C9 and CYP3A4 substrate nateglinide. Itraconazole 36-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 16042675-1 2005 BACKGROUND AND AIMS: Gemfibrozil, and particularly its combination with itraconazole, greatly increases the area under the plasma concentration-time curve [AUC(0, infinity)] and response to the cytochrome P450 (CYP) 2C8 and 3A4 substrate repaglinide. Itraconazole 72-84 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 194-219 16042675-3 2005 Our aim was to investigate the effects of the gemfibrozil-itraconazole combination on the pharmacokinetics and pharmacodynamics of another meglitinide analogue, nateglinide, which is metabolized by CYP2C9 and CYP3A4. Itraconazole 58-70 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 198-204 16042675-3 2005 Our aim was to investigate the effects of the gemfibrozil-itraconazole combination on the pharmacokinetics and pharmacodynamics of another meglitinide analogue, nateglinide, which is metabolized by CYP2C9 and CYP3A4. Itraconazole 58-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 209-215 16012077-4 2005 The formation of 4-hydroxyestazolam from estazolam in pooled human liver microsomes was significantly inhibited by itraconazole and erythromycin, specific CYP3A4 inhibitors, in a dose-dependent manner, with IC50 values of 1.1 and 12.8 microM, respectively. Itraconazole 115-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 155-161 15969931-3 2005 An inhibitory effect on CYP3A4 activity was found for ketoconazole, itraconazole and miconazole, with 50% inhibitory concentrations of 11.7, 32.6 and 74.2 nM, respectively. Itraconazole 68-80 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 15900215-2 2005 Some patients who take atorvastatin along with concomitant medications known to inhibit CYP3A enzyme activity (e.g. itraconazole) develop rhabdomyolysis secondary to a severe drug-induced myopathy. Itraconazole 116-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-93 15829804-10 2005 In keratitis due to Fusarium spp, 19 (79%) of 24 patients showed a favorable response to natamycin, which was significantly greater than the 8 (44%) of 18 patients who showed a favorable response to itraconazole (P < 0.02). Itraconazole 199-211 histocompatibility minor 13 Homo sapiens 29-32 15829804-13 2005 CONCLUSIONS: Topical natamycin should continue to be considered as the treatment of choice for filamentous fungal keratitis; when natamycin is unavailable, topical itraconazole therapy could be used, particularly if the infections are due to Aspergillus or Curvularia spp. Itraconazole 164-176 histocompatibility minor 13 Homo sapiens 268-271 15969931-5 2005 The MDR1-mediated transport of [3H]digoxin was inhibited by ketoconazole and itraconazole, and slightly by miconazole. Itraconazole 77-89 ATP binding cassette subfamily B member 1 Homo sapiens 4-8 15905803-11 2005 Drug interactions can occur with itraconazole because it is both an inhibitor and substrate of the cytochrome P450 3A4 (CYP3A4) enzyme and P-glycoprotein transporter systems. Itraconazole 33-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 99-118 15905803-11 2005 Drug interactions can occur with itraconazole because it is both an inhibitor and substrate of the cytochrome P450 3A4 (CYP3A4) enzyme and P-glycoprotein transporter systems. Itraconazole 33-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-126 15770075-2 2005 The objective of the present study was to investigate the influence of itraconazole (hereafter referred to as ITZ) co-administration (CYP3A4 inhibition) on the pharmacokinetics of ARIPIPRAZOLE administered to 24 healthy adult male volunteers in a fasting condition. Itraconazole 71-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 134-140 15684493-3 2005 This might be because concomitant drugs such as itraconazole inhibit cytochrome P450 3A4 (CYP3A4), the enzyme responsible for the degradation of terfenadine and astemizole, and thus the blood concentrations of the drugs are abnormally increased. Itraconazole 48-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-88 15684493-3 2005 This might be because concomitant drugs such as itraconazole inhibit cytochrome P450 3A4 (CYP3A4), the enzyme responsible for the degradation of terfenadine and astemizole, and thus the blood concentrations of the drugs are abnormally increased. Itraconazole 48-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 15770075-12 2005 The urinary 6beta-hydroxycortisol/cortisol concentration ratio following ITZ administration for 7 consecutive days was about half of that before the start of ITZ administration, indicating that CYP3A4 metabolic activity was inhibited by administration of ITZ. Itraconazole 73-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 194-200 15770075-12 2005 The urinary 6beta-hydroxycortisol/cortisol concentration ratio following ITZ administration for 7 consecutive days was about half of that before the start of ITZ administration, indicating that CYP3A4 metabolic activity was inhibited by administration of ITZ. Itraconazole 158-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 194-200 15770075-12 2005 The urinary 6beta-hydroxycortisol/cortisol concentration ratio following ITZ administration for 7 consecutive days was about half of that before the start of ITZ administration, indicating that CYP3A4 metabolic activity was inhibited by administration of ITZ. Itraconazole 158-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 194-200 16122280-16 2005 Inhibition of CYP3A4 by potent inhibitors such as itraconazole and ketoconazole results in a 54% and 95% increase in telithromycin area under the plasma concentration-time curve, respectively. Itraconazole 50-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 15726880-1 2005 OBJECTIVE: The present study evaluates the acute effect of a single-dose itraconazole administration on CYP3A phenotype, as measured by cortisol MR ratio in urine. Itraconazole 73-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 104-109 15447735-3 2004 We have studied the effect of a potent CYP3A4 inhibitor, itraconazole, on the pharmacokinetics of inhaled lidocaine in ten healthy volunteers using a randomized, two-phase cross-over study design. Itraconazole 57-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 15865259-2 2005 Itraconazole is an inhibitor of CYP3A4, a metabolic enzyme of sildenafil. Itraconazole 0-12 cytochrome P450 3A12 Canis lupus familiaris 32-38 15521894-7 2004 CONCLUSIONS: Itraconazole increases plasma concentrations of brotizolam probably via its inhibitory effect on CYP3A4 brotizolam metabolism. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 15242978-0 2004 Role of itraconazole metabolites in CYP3A4 inhibition. Itraconazole 8-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-42 15242978-1 2004 Itraconazole (ITZ) is a potent inhibitor of CYP3A in vivo. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-49 15242978-1 2004 Itraconazole (ITZ) is a potent inhibitor of CYP3A in vivo. Itraconazole 14-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-49 15242978-10 2004 Both ITZ and OH-ITZ were competitive inhibitors of CYP3A4, with unbound Ki (1.3 nM for ITZ and 14.4 nM for OH-ITZ) close to their respective Km. Itraconazole 5-8 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-57 15242978-10 2004 Both ITZ and OH-ITZ were competitive inhibitors of CYP3A4, with unbound Ki (1.3 nM for ITZ and 14.4 nM for OH-ITZ) close to their respective Km. Itraconazole 16-19 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-57 15552648-9 2004 However, itraconazole which targets Erg11p (lanosterol demethylase) increased ERG27 expression 10-fold and zaragozic acid A which targets the Erg9p (squalene synthase) increased ERG27 expression fivefold. Itraconazole 9-21 3-keto-steroid reductase Saccharomyces cerevisiae S288C 78-83 15289787-10 2004 However, during cytochrome P450 (CYP) 3A inhibition by itraconazole, individuals carrying the CYP3A5*1 allele were found to be less susceptible to changes in systemic clearance and showed higher 1"-hydroxymidazolam-to-midazolam area under the plasma concentration-time curve ratios, probably resulting from the relatively CYP3A4-specific inhibition caused by itraconazole. Itraconazole 55-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-40 15289787-10 2004 However, during cytochrome P450 (CYP) 3A inhibition by itraconazole, individuals carrying the CYP3A5*1 allele were found to be less susceptible to changes in systemic clearance and showed higher 1"-hydroxymidazolam-to-midazolam area under the plasma concentration-time curve ratios, probably resulting from the relatively CYP3A4-specific inhibition caused by itraconazole. Itraconazole 55-67 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 94-100 15289787-10 2004 However, during cytochrome P450 (CYP) 3A inhibition by itraconazole, individuals carrying the CYP3A5*1 allele were found to be less susceptible to changes in systemic clearance and showed higher 1"-hydroxymidazolam-to-midazolam area under the plasma concentration-time curve ratios, probably resulting from the relatively CYP3A4-specific inhibition caused by itraconazole. Itraconazole 359-371 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 94-100 15289787-10 2004 However, during cytochrome P450 (CYP) 3A inhibition by itraconazole, individuals carrying the CYP3A5*1 allele were found to be less susceptible to changes in systemic clearance and showed higher 1"-hydroxymidazolam-to-midazolam area under the plasma concentration-time curve ratios, probably resulting from the relatively CYP3A4-specific inhibition caused by itraconazole. Itraconazole 55-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 322-328 15204103-0 2004 In vitro evaluation of cytochrome P450-mediated drug interactions between cytarabine, idarubicin, itraconazole and caspofungin. Itraconazole 98-110 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 23-38 15232663-2 2004 METHODS: The effects of itraconazole, a potent and specific inhibitor of CYP3A4, on the single oral dose pharmacokinetics and pharmacodynamics of etizolam were examined. Itraconazole 24-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-79 15232663-9 2004 CONCLUSION: The present study suggests that itraconazole inhibits the metabolism of etizolam, providing evidence that CYP3A4 is at least partly involved in etizolam metabolism. Itraconazole 44-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 15286096-2 2004 The purpose of this study was to evaluate the effect of itraconazole, a known P-gp inhibitor, on the renal tubular secretion of cimetidine in healthy volunteers who received intravenous cimetidine alone and following 3 days of oral itraconazole (400 mg/day) administration. Itraconazole 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 78-82 15286096-10 2004 The increased systemic exposure of cimetidine during coadministration with itraconazole was likely due to inhibition of P-gp-mediated renal tubular secretion. Itraconazole 75-87 ATP binding cassette subfamily B member 1 Homo sapiens 120-124 15286096-11 2004 Further evaluation of renal P-gp-modulating drugs such as itraconazole that may alter the renal excretion of coadministered drugs is warranted. Itraconazole 58-70 ATP binding cassette subfamily B member 1 Homo sapiens 28-32 15204103-3 2004 In vitro assays were performed to assess whether cytochrome P450 (CYP450) enzymes were affected by combinations of cytarabine or idarubicin with itraconazole or caspofungin. Itraconazole 145-157 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 49-64 15204103-3 2004 In vitro assays were performed to assess whether cytochrome P450 (CYP450) enzymes were affected by combinations of cytarabine or idarubicin with itraconazole or caspofungin. Itraconazole 145-157 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 66-72 15204103-4 2004 METHODS: The high throughput microtiter assay was used to determine whether cytarabine, idarubicin and itraconazole or caspofungin were CYP450 isoenzyme substrates, inhibitors of CYP450 isoenzymes, and to determine potential CYP450 metabolism interactions between these agents. Itraconazole 103-115 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 136-142 15204103-4 2004 METHODS: The high throughput microtiter assay was used to determine whether cytarabine, idarubicin and itraconazole or caspofungin were CYP450 isoenzyme substrates, inhibitors of CYP450 isoenzymes, and to determine potential CYP450 metabolism interactions between these agents. Itraconazole 103-115 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 179-185 15204103-4 2004 METHODS: The high throughput microtiter assay was used to determine whether cytarabine, idarubicin and itraconazole or caspofungin were CYP450 isoenzyme substrates, inhibitors of CYP450 isoenzymes, and to determine potential CYP450 metabolism interactions between these agents. Itraconazole 103-115 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 179-185 15133245-3 2004 This might be because concomitant drugs such as itraconazole inhibit cytochrome P450 3A4 (CYP3A4), the enzyme responsible for degradation of terfenadine and astemizole, and thus the blood concentrations of the drugs are abnormally increased. Itraconazole 48-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-88 15133245-3 2004 This might be because concomitant drugs such as itraconazole inhibit cytochrome P450 3A4 (CYP3A4), the enzyme responsible for degradation of terfenadine and astemizole, and thus the blood concentrations of the drugs are abnormally increased. Itraconazole 48-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 14517708-3 2003 The purpose of this study was to examine whether the inhibition of CYP3A4 produced by itraconazole alters the pharmacokinetics and pharmacodynamics of bromazepam. Itraconazole 86-98 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 15370674-0 2004 Modulation of the human interleukin-12p40 response by a triazole antifungal derivative, itraconazole. Itraconazole 88-100 interleukin 12B Homo sapiens 24-41 15370674-2 2004 We investigated whether itraconazole (ITCZ) can modulate the serum cytokine levels (tumor necrosis factor (TNF-alpha, interleukin (IL)-10, IL-12p40) in both patients and healthy subjects. Itraconazole 24-36 tumor necrosis factor Homo sapiens 84-105 15370674-2 2004 We investigated whether itraconazole (ITCZ) can modulate the serum cytokine levels (tumor necrosis factor (TNF-alpha, interleukin (IL)-10, IL-12p40) in both patients and healthy subjects. Itraconazole 38-42 tumor necrosis factor Homo sapiens 84-105 15284827-4 2004 Azole derivatives, ketoconazole, itraconazole, miconazole and non-azole terbinafine hydrochloride and tolnaftate reduced IL-4 and IL-5 secretion without altering that of IFN-gamma and IL-2 in anti-CD3/CD28-stimulated T cells from both AD patients and normal donors. Itraconazole 33-45 interleukin 4 Homo sapiens 121-125 15284827-4 2004 Azole derivatives, ketoconazole, itraconazole, miconazole and non-azole terbinafine hydrochloride and tolnaftate reduced IL-4 and IL-5 secretion without altering that of IFN-gamma and IL-2 in anti-CD3/CD28-stimulated T cells from both AD patients and normal donors. Itraconazole 33-45 interleukin 5 Homo sapiens 130-134 12684380-7 2003 Dap1p also directs resistance to itraconazole and fluconazole, inhibitors of sterol synthesis. Itraconazole 33-45 death associated protein Homo sapiens 0-5 12883232-1 2003 The effects of itraconazole, a potent inhibitor of cytochrome P450 (CYP) 3A4, on the plasma kinetics of quazepam and its two active metabolites after a single oral dose of the drug were studied. Itraconazole 15-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-76 12743557-8 2003 Itraconazole reduced systemic immune activation, leading to a decrease in serum IgE levels (310 IU/mL) compared with levels seen in the placebo group (increase of 18 IU/mL, P <.01) and a decrease in IgG levels to A fumigatu s (15.4 IU/mL) compared with levels seen in the placebo group (increase of 3.7 IU/mL, P =.03). Itraconazole 0-12 immunoglobulin heavy constant epsilon Homo sapiens 80-83 12709722-2 2003 Itraconazole, an inhibitor of cytochrome P450 (CYP) 3A4 and the transport protein P-glycoprotein, is known to interact with other HMG-CoA reductase inhibitors. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-55 12709722-2 2003 Itraconazole, an inhibitor of cytochrome P450 (CYP) 3A4 and the transport protein P-glycoprotein, is known to interact with other HMG-CoA reductase inhibitors. Itraconazole 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 82-96 12595750-0 2003 Effect of interleukin 6 on the hepatic metabolism of itraconazole and its metabolite hydroxyitraconazole using primary human hepatocytes. Itraconazole 53-65 interleukin 6 Homo sapiens 10-23 12654681-0 2003 In vitro synergy of caspofungin and itraconazole against Aspergillus spp. Itraconazole 36-48 histocompatibility minor 13 Homo sapiens 69-72 12166560-2 2002 Itraconazole can inhibit CYP3A, thus interfering with synthesis of gluco- and mineralocorticoids, androgens and oestradiol as well as the metabolism of budesonide. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 25-30 12619051-5 2003 Itraconazole was reported to be metabolized via CYP3A4 to several metabolites, including hydroxyitraconazole, in human subjects. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54 12388057-6 2003 We found that in high endothelial venular cells (SVEC4-10), multiple inhibitors of CYP450 monooxygenases (SKF-525a, ketoconazole, troleandomycin, itraconazole) attenuated TNF-alpha induction of MAdCAM-1, whereas NADPH oxidase inhibition (PR-39) did not. Itraconazole 146-158 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 83-89 12949438-6 2003 Serious cases by coadministration of CYP3A inhibitors resulting in acute hepatitis, hypotension, rhabdomyolyis, torsade de pointes, sedation, or ergotism are presented: interactions with azole antifungals (ketoconazole, itraconazole, fluconazole), HIV protease inhibitors (ritonavir, indinavir, saquinavir, nelfinavir), macrolide antibiotics (clarithromycin, erythromycin), and grapefruit juice. Itraconazole 220-232 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-42 12237270-0 2002 P-glycoprotein as the mediator of itraconazole-digoxin interaction. Itraconazole 34-46 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 12069997-3 2002 The in vitro MICs of posaconazole and itraconazole for the strains of Mucor spp. Itraconazole 38-50 sphingosine-1-phosphate phosphatase 1 Mus musculus 76-79 12412882-8 2002 CONCLUSION: This observation suggests that the metabolic clearance of buDesonide was compromised by itraconazole"s inhibition of cytochrome P450 enzymes, especially the CYP3A isoforms, causing an elevation in systemic budesonide concentration. Itraconazole 100-112 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-174 12134942-5 2002 RESULTS: Amiodarone (10 microM) inhibited slightly the transcellular transport of digoxin in LLC-GA5-COL150 monolayers, whereas itraconazole (10 microM), a potent Pgp inhibitor, markedly blocked the transport. Itraconazole 128-140 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 163-166 11740718-8 2002 Primary prophylaxis with oral itraconazole is well tolerated and prevents cryptococcosis and penicilliosis marneffei in patients with advanced HIV infection, especially those with CD4+ lymphocyte counts of <100 cells/microL. Itraconazole 30-42 CD4 molecule Homo sapiens 180-183 15618678-8 2002 Correspondingly, the content of CYP3A2 was significantly altered by single or repeated itraconazole administration. Itraconazole 87-99 cytochrome P450, family 3, subfamily a, polypeptide 2 Rattus norvegicus 32-38 11751127-6 2002 In a cell line presenting an overexpressed amount of the human P-gp transporter, itraconazole and ketoconazole inhibited P-gp function with 50% inhibitory concentrations (IC(50)s) of approximately 2 and approximately 6 microM, respectively. Itraconazole 81-93 ATP binding cassette subfamily B member 1 Homo sapiens 63-67 11751127-6 2002 In a cell line presenting an overexpressed amount of the human P-gp transporter, itraconazole and ketoconazole inhibited P-gp function with 50% inhibitory concentrations (IC(50)s) of approximately 2 and approximately 6 microM, respectively. Itraconazole 81-93 ATP binding cassette subfamily B member 1 Homo sapiens 121-125 11836874-6 2001 The concomitant use of statins with drugs that inhibit CYP3A4 (cyclosporin, erythromycin, clarithromycin, itraconazole, and ketoconazole), may result in increased plasma concentrations of HMG-CoA reductase inhibitors leading occasionally to myotoxicity. Itraconazole 106-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 11808341-6 2002 The ATP-driven efflux pump P-glycoprotein appeared to be an interaction site between digoxin and clarithromycin or itraconazole in the kidney. Itraconazole 115-127 ATP binding cassette subfamily B member 1 Homo sapiens 27-41 11886533-4 2001 Azole derivatives, ketoconazole, itraconazole, miconazole, and nonazole terbinafine hydrochloride, and tolnaftate reduced interleukin-4 and interleukin-5 secretion without altering that of interferon-gamma and interleukin-2 in anti-CD3/CD28-stimulated T cells from both atopic dermatitis patients and normal donors. Itraconazole 33-45 interleukin 4 Homo sapiens 122-135 11886533-4 2001 Azole derivatives, ketoconazole, itraconazole, miconazole, and nonazole terbinafine hydrochloride, and tolnaftate reduced interleukin-4 and interleukin-5 secretion without altering that of interferon-gamma and interleukin-2 in anti-CD3/CD28-stimulated T cells from both atopic dermatitis patients and normal donors. Itraconazole 33-45 interleukin 5 Homo sapiens 140-153 11516940-4 2001 The activities of posaconazole for all the fungal species far surpassed those of fluconazole and were even superior to those of itraconazole for Aspergillus spp. Itraconazole 128-140 histocompatibility minor 13 Homo sapiens 157-160 11531835-9 2001 With itraconazole 200 mg d(-1) or 400 mg d(-1) for 1 week each month for 3-4 months, EP1 was 37% at 18 months, and 53% at 2 years; EP2 was 76% at 4 years. Itraconazole 5-17 prostaglandin E receptor 1 Homo sapiens 85-88 11531835-11 2001 In the only study planned to compare the long-term efficacy of terbinafine and itraconazole, EP1 at 18 months was significantly higher with continuous terbinafine than with intermittent itraconazole (66% vs. 37%, P < 0.001). Itraconazole 79-91 prostaglandin E receptor 1 Homo sapiens 93-96 11531835-11 2001 In the only study planned to compare the long-term efficacy of terbinafine and itraconazole, EP1 at 18 months was significantly higher with continuous terbinafine than with intermittent itraconazole (66% vs. 37%, P < 0.001). Itraconazole 186-198 prostaglandin E receptor 1 Homo sapiens 93-96 11558564-6 2001 Itraconazole was found to have potent reversal effect on the resistance to VLB and TXL, but the others had no such effect. Itraconazole 0-12 thioredoxin like 1 Homo sapiens 83-86 11737382-2 2001 METHODS: HIV-1 infected patients with CD4 counts < 300 cells/microL were treated with itraconazole (200 mg per day) or matching placebo and followed for 2 years. Itraconazole 89-101 CD4 molecule Homo sapiens 38-41 11408375-4 2001 Therefore, the sex difference in the inhibition of simvastatin metabolism by itraconazole seems to be caused by a difference in the P450 isozymes responsible for the metabolism of simvastatin in male and female rats and the different ability of itraconazole to inhibit CYP3A and CYP2C11. Itraconazole 77-89 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 269-274 11408375-4 2001 Therefore, the sex difference in the inhibition of simvastatin metabolism by itraconazole seems to be caused by a difference in the P450 isozymes responsible for the metabolism of simvastatin in male and female rats and the different ability of itraconazole to inhibit CYP3A and CYP2C11. Itraconazole 77-89 cytochrome P450, subfamily 2, polypeptide 11 Rattus norvegicus 279-286 11422002-1 2001 AIMS: Itraconazole is a potent inhibitor of CYP3A4 activity and is often used in combination with corticosteroids. Itraconazole 6-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-50 11422002-9 2001 The pharmacokinetic interaction between methylprednisolone and itraconazole is probably related to inhibition of hepatic CYP3A4 activity by itraconazole. Itraconazole 63-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 11422002-9 2001 The pharmacokinetic interaction between methylprednisolone and itraconazole is probably related to inhibition of hepatic CYP3A4 activity by itraconazole. Itraconazole 140-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 11465417-4 2001 RESULTS: Itraconazole competitively inhibited the metabolism of simvastatin to M-1 and M-2 with Ki values in the nM range. Itraconazole 9-21 cholinergic receptor muscarinic 1 Homo sapiens 79-82 11465417-9 2001 CONCLUSIONS: It was demonstrated that the competitive inhibition of CYP3A4-mediated simvastatin metabolism by itraconazole is the main cause of the drug interaction and that a Ki value corrected for drug adsorption to microsomes is the key factor in quantitatively predicting the maximum in vivo drug interactions. Itraconazole 110-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-74 11372588-1 2001 OBJECTIVE: To characterise the effects of itraconazole, a potent inhibitor of CYP3A4, on the pharmacokinetics of selegiline in healthy volunteers. Itraconazole 42-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 11799844-3 2001 The present study was carried out to determine whether oxatomide and terfenadine have effects on QT interval as a single drug or in combination with itraconazole (CAS 84625-61-6), an antifungal agent with a CYP3A4 inhibitory effect, in conscious dogs. Itraconazole 149-161 cytochrome P450 3A12 Canis lupus familiaris 207-213 11322176-7 2001 Both clarithromycin and itraconazole inhibit the CYP3A4 mediated formation of (S)-2",6"-pipecoloxylidide from ropivacaine. Itraconazole 24-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-55 11061579-5 2000 OBJECTIVE: To determine the comparative effect of itraconazole, a potent CYP3A4 inhibitor, on the pharmacokinetics of cerivastatin, atorvastatin, and pravastatin. Itraconazole 50-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-79 11687098-16 2001 REVIEWER"S CONCLUSIONS: Itraconazole modifies the immunologic activation associated with ABPA and improves clinical outcome in ABPA at least over the period of 16 weeks. Itraconazole 24-36 filamin C Homo sapiens 89-93 11687098-16 2001 REVIEWER"S CONCLUSIONS: Itraconazole modifies the immunologic activation associated with ABPA and improves clinical outcome in ABPA at least over the period of 16 weeks. Itraconazole 24-36 filamin C Homo sapiens 127-131 11103751-0 2000 The cytochrome P450 3A4 inhibitor itraconazole markedly increases the plasma concentrations of dexamethasone and enhances its adrenal-suppressant effect. Itraconazole 34-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-23 11103751-10 2000 A careful follow-up is recommended when itraconazole or other potent inhibitors of the cytochrome P450 3A4 are added to the drug regimen of patients receiving dexamethasone. Itraconazole 40-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-106 10926350-9 2000 Similarly, azole antifungal agents such as fluconazole, itraconazole and ketoconazole are CYP3A4 inhibitors and their concomitant use with cisapride should be avoided. Itraconazole 56-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 11007866-0 2000 Tacrolimus/itraconazole interactions: a case report of ABO-incompatible living-related renal transplantation. Itraconazole 11-23 ABO, alpha 1-3-N-acetylgalactosaminyltransferase and alpha 1-3-galactosyltransferase Homo sapiens 55-58 10786463-7 2000 Three weeks into the puerperium, she developed generalised seizures and investigations indicated systemic fungal infection with positive cultures for Aureobasidium spp which responded to appropriate antifungal therapy of flucytosine and itraconazole. Itraconazole 237-249 histocompatibility minor 13 Homo sapiens 164-167 10731517-2 2000 IC(50) values for ketoconazole and itraconazole CYP3A4 inhibition were 0.25 and 0. Itraconazole 35-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54 10722490-14 2000 The higher level of distribution of SYN-2869 into lung tissue was considered to contribute to the potent efficacy in respiratory tract infection models compared with the potency of itraconazole. Itraconazole 181-193 joined toes Mus musculus 36-39 10853878-8 2000 The susceptibility of prednisolone to interact with CYP3A4 inhibitors is considerably smaller than that of methylprednisolone, and itraconazole and probably also other inhibitors of CYP3A4 can be used concomitantly with prednisolone without marked changes in the effects of this corticosteroid. Itraconazole 131-143 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 182-188 10885336-7 2000 He responded to fluconazole, and was given itraconazole as secondary prophylaxis because of persistent low CD4 counts. Itraconazole 43-55 CD4 molecule Homo sapiens 107-110 10746169-1 1999 The reversal effect of itraconazole on P-glycoprotein (P-gp)-mediated resistance of vinblastine, daunorubicin and doxorubicin was analyzed from a cellular pharmacokinetic point of view, namely by [3H]azidopine photoaffinity labeling, intracellular accumulation and transcellular transport experiments. Itraconazole 23-35 phosphoglycolate phosphatase Homo sapiens 55-59 10709776-6 2000 Ketoconazole and itraconazole are potent inhibitors of the major drug-metabolising CYP isoform in humans, CYP3A4. Itraconazole 17-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-112 10668858-6 2000 Clinically important CYP3A4 inhibitors include itraconazole, ketoconazole, clarithromycin, erythromycin, nefazodone, ritonavir and grapefruit juice. Itraconazole 47-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 10746169-4 1999 [3H]Azidopine photoaffinity labeling demonstrated that itraconazole, vinblastine, daunorubicin and doxorubicin showed higher binding ability for P-gp compared with digoxin, suggesting the following results were via P-gp. Itraconazole 55-67 phosphoglycolate phosphatase Homo sapiens 145-149 10746169-4 1999 [3H]Azidopine photoaffinity labeling demonstrated that itraconazole, vinblastine, daunorubicin and doxorubicin showed higher binding ability for P-gp compared with digoxin, suggesting the following results were via P-gp. Itraconazole 55-67 phosphoglycolate phosphatase Homo sapiens 215-219 10746169-7 1999 However, their basal-to-apical transport was hardly affected by itraconazole, and this was explained by the fact that itraconazole inhibited P-gp, and subsequently increased their intracellular concentration and then the non-P-gp mediated transport from the intracellular space to apical side. Itraconazole 118-130 phosphoglycolate phosphatase Homo sapiens 141-145 10746169-7 1999 However, their basal-to-apical transport was hardly affected by itraconazole, and this was explained by the fact that itraconazole inhibited P-gp, and subsequently increased their intracellular concentration and then the non-P-gp mediated transport from the intracellular space to apical side. Itraconazole 118-130 phosphoglycolate phosphatase Homo sapiens 225-229 10746169-8 1999 The apical-to-basal transport of [3H]vinblastine, [3H]daunorubicin and [14C]doxorubicin was increased by itraconazole, and this was reasonably explained by the inhibition of P-gp, and partly also by the increase of their intracellular concentration via the inhibition of P-gp. Itraconazole 105-117 phosphoglycolate phosphatase Homo sapiens 174-178 10746169-8 1999 The apical-to-basal transport of [3H]vinblastine, [3H]daunorubicin and [14C]doxorubicin was increased by itraconazole, and this was reasonably explained by the inhibition of P-gp, and partly also by the increase of their intracellular concentration via the inhibition of P-gp. Itraconazole 105-117 phosphoglycolate phosphatase Homo sapiens 271-275 10426160-1 1999 A possible interaction of itraconazole, a potent inhibitor of CYP3A4, with intravenously administered methylprednisolone, was examined. Itraconazole 26-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 10730911-4 1999 For example, itraconazole, and to a lesser extent fluconazole (in high doses) are inhibitors of CYP3A4. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102 10544287-10 1999 The lanosterol demethylase activity of the reconstituted system of CYP51m was inhibited by ketoconazole, itraconazole and fluconazole with apparent IC(50) values of 0.2, 0.7, and 160 microM, respectively. Itraconazole 105-117 cytochrome P450, family 51 Rattus norvegicus 67-72 10463320-2 1999 OBJECTIVE: We investigated pharmacokinetic interaction between bromperidol and itraconazole, a potent inhibitor of CYP3A4, to clarify the involvement of CYP3A4 in the metabolism of bromperidol and its reduced metabolite. Itraconazole 79-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 10600094-5 1999 The time course suggested a possible interaction between clarithromycin and itraconazole, presumably through itraconazole"s effects on cytochrome P450 3A4 activity. Itraconazole 76-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 135-154 10600094-5 1999 The time course suggested a possible interaction between clarithromycin and itraconazole, presumably through itraconazole"s effects on cytochrome P450 3A4 activity. Itraconazole 109-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 135-154 10471571-4 1999 While both BMS-207147 and itraconazole displayed a stepwise decrease in activity against isolates for which the fluconazole MICs were elevated, BMS-207147 had two- to fourfold greater activity than itraconazole both against Candida spp. Itraconazole 26-38 histocompatibility minor 13 Homo sapiens 232-235 10426160-11 1999 Care should be taken when itraconazole or other potent inhibitors of CYP3A4 are used concomitantly with methylprednisolone. Itraconazole 26-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 10546485-4 1999 In these patients the itraconazole trough concentrations exceeded 500 ng ml-1 (measured by high performance liquid chromatography) significantly less often (median 48%, interquartile range 0-100%) than in another group of 150 leukaemia patients without invasive fungal infections who received 287 courses of prophylaxis with itraconazole at our institution (median 100%, interquartile range 38-100%, P = 0.039). Itraconazole 22-34 interleukin 17F Homo sapiens 73-77 10211916-1 1999 The effects of itraconazole, a potent inhibitor of cytochrome P450 (CYP) 3A4, on the steady-state plasma concentrations of haloperidol and reduced haloperidol were examined in schizophrenic patients. Itraconazole 15-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-76 10027433-1 1999 STUDY OBJECTIVES: (1) To determine the relationship between IgE levels and the prevalence of allergic bronchopulmonary aspergillosis (ABPA) in cystic fibrosis (CF) patients, (2) to establish the usefulness of assessing atopy as an identifying risk factor for ABPA, (3) to evaluate the clinical course of patients receiving and not receiving itraconazole as reflected in oral steroid dose requirements and number of acute episodes of ABPA, and (4) to determine the role of acute episodes of ABPA in pulmonary exacerbations of CF. Itraconazole 341-353 immunoglobulin heavy constant epsilon Homo sapiens 60-63 10546485-6 1999 Patients with fatal invasive fungal infections had lower median itraconazole concentrations immediately before occurrence of the infection than patients with non-fatal infections: 120 (0-478) ng ml-1 versus 690 (305-1908) ng ml-1 (P = 0.039). Itraconazole 64-76 interleukin 17F Homo sapiens 225-229 10546485-7 1999 In conclusion, this analysis of breakthrough invasive fungal infections during prophylaxis with itraconazole demonstrates that patients with itraconazole trough concentrations below 500 ng ml-1 were significantly more likely to develop fungal infections and that the last itraconazole trough concentration before occurrence of the infection was significantly lower in patients with fatal invasive fungal infections. Itraconazole 141-153 interleukin 17F Homo sapiens 189-193 10546485-7 1999 In conclusion, this analysis of breakthrough invasive fungal infections during prophylaxis with itraconazole demonstrates that patients with itraconazole trough concentrations below 500 ng ml-1 were significantly more likely to develop fungal infections and that the last itraconazole trough concentration before occurrence of the infection was significantly lower in patients with fatal invasive fungal infections. Itraconazole 141-153 interleukin 17F Homo sapiens 189-193 11252341-1 1999 The protein binding of itraconazole and fluconazole in the serum of patients with insulin-dependent (IDDM) and non-insulin-dependent (NIDDM) diabetes mellitus was investigated in vitro. Itraconazole 23-35 insulin Homo sapiens 82-89 10449937-3 1999 Itraconazole can inhibit the metabolism of drugs by CYP 3A4 and therefore might affect the efficacy of antidiabetic agents. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-59 10027660-1 1999 OBJECTIVE: To determine the effects of itraconazole, a potent inhibitor of CYP3A4, on the pharmacokinetics of cerivastatin, a competitive 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor. Itraconazole 39-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 10027660-1 1999 OBJECTIVE: To determine the effects of itraconazole, a potent inhibitor of CYP3A4, on the pharmacokinetics of cerivastatin, a competitive 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor. Itraconazole 39-51 3-hydroxy-3-methylglutaryl-CoA reductase Homo sapiens 138-195 10067059-7 1999 RFP induces cytochrome P450 3A in the liver to decrease the activities of many drugs, such as cyclosporin A, tacrolimus, protease inhibitor, itraconazole, and clarithromycin. Itraconazole 141-153 tripartite motif containing 27 Homo sapiens 0-3 10546485-6 1999 Patients with fatal invasive fungal infections had lower median itraconazole concentrations immediately before occurrence of the infection than patients with non-fatal infections: 120 (0-478) ng ml-1 versus 690 (305-1908) ng ml-1 (P = 0.039). Itraconazole 64-76 interleukin 17F Homo sapiens 195-199 10680434-1 1999 We have previously shown that a trough concentration of at least 500 ng ml-1 itraconazole is necessary for an effective antifungal prophylaxis in neutropenic patients. Itraconazole 77-89 interleukin 17F Homo sapiens 72-76 9726699-1 1998 Itraconazole is a potent inhibitor of CYP3A4 isoenzyme and it can cause clinically significant interactions with some other drugs. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 10680434-4 1999 After the first week, patients taking 800 mg day-1 or 400 mg day-1 (s/c1200) itraconazole solution achieved significantly higher trough concentrations (high-performance liquid chromatography) than patients in other groups (P < 0.05) and 87 and 100%, respectively, of these had concentrations > 500 ng ml-1. Itraconazole 77-89 interleukin 17F Homo sapiens 307-311 11362022-9 1998 In patients with CD4 counts of < or = 150/microL, itraconazole is effective primary prophylaxis. Itraconazole 53-65 CD4 molecule Homo sapiens 17-20 9784084-1 1998 To assess the effect of itraconazole, a potent inhibitor of cytochrome P450 (CYP) 3A4, on the single oral dose pharmacokinetics and pharmacodynamics of alprazolam, the study was conducted in a double-blind randomized crossover manner with two phases of treatment with itraconazole-placebo or placebo-itraconazole. Itraconazole 24-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-85 9784084-6 1998 It is suggested that itraconazole, a potent CYP3A4 inhibitor, increases plasma concentration of alprazolam via its inhibitory effects on alprazolam metabolism. Itraconazole 21-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-50 9832299-1 1998 OBJECTIVE: We have studied the possible interaction of erythromycin and itraconazole, both inhibitors of cytochrome P450 3A4 isoenzyme (CYP3A4), with intravenous lignocaine in nine healthy volunteers using a randomized cross-over study design. Itraconazole 72-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-134 9832299-1 1998 OBJECTIVE: We have studied the possible interaction of erythromycin and itraconazole, both inhibitors of cytochrome P450 3A4 isoenzyme (CYP3A4), with intravenous lignocaine in nine healthy volunteers using a randomized cross-over study design. Itraconazole 72-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 136-142 9884817-14 1998 Itraconazole is a potent inhibitor of cytochrome P450 (CYP) 3A4 and, thus, can also considerably change the pharmacokinetics of other drugs. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-63 9855331-3 1998 All the substrates and inhibitors of CYP3A4 such as the azole antifungals (itraconazole, ketoconazole), cyclosporine, isoniazid, and nifedipine have very high propensity to interfere with vincristine metabolism. Itraconazole 75-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 9797792-2 1998 In this study, a possible interaction of itraconazole, a potent inhibitor of CYP3A4, with orally administered methylprednisolone was examined. Itraconazole 41-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-83 9797792-9 1998 CONCLUSIONS: Itraconazole considerably increases plasma concentrations and effects of oral methylprednisolone, probably by inhibiting its CYP3A4-mediated metabolism. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 9797792-10 1998 Care should be taken if itraconazole or other potent inhibitors of CYP3A4 are used concomitantly with oral methylprednisolone, particularly during long-term use. Itraconazole 24-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 9661014-8 1998 Moreover, the uptake of vincristine or vinblastine, both of which are substrates of the P glycoprotein (P-gp), into mouse brain capillary endothelial cells was also significantly increased by ITZ or verapamil. Itraconazole 192-195 phosphoglycolate phosphatase Mus musculus 88-102 9695720-1 1998 BACKGROUND: Itraconazole, a potent inhibitor of CYP3A4, increases the risk of skeletal muscle toxicity of some 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors by increasing their serum concentrations. Itraconazole 12-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54 9695720-1 1998 BACKGROUND: Itraconazole, a potent inhibitor of CYP3A4, increases the risk of skeletal muscle toxicity of some 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors by increasing their serum concentrations. Itraconazole 12-24 3-hydroxy-3-methylglutaryl-CoA reductase Homo sapiens 111-168 9695720-2 1998 The aim of this study was to characterize the effect of itraconazole on the pharmacokinetics of atorvastatin, a new HMG-CoA reductase inhibitor that is metabolized at least in part by CYP3A4. Itraconazole 56-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 184-190 9695720-12 1998 The mechanism of increased serum concentrations of atorvastatin and HMG-CoA reductase inhibitors is inhibition of CYP3A4-mediated metabolism of atorvastatin and its metabolites by itraconazole. Itraconazole 180-192 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-120 9695720-13 1998 Concomitant use of itraconazole and other potent inhibitors of CYP3A4 with atorvastatin should be avoided or the dose of atorvastatin should be reduced accordingly. Itraconazole 19-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 9661014-8 1998 Moreover, the uptake of vincristine or vinblastine, both of which are substrates of the P glycoprotein (P-gp), into mouse brain capillary endothelial cells was also significantly increased by ITZ or verapamil. Itraconazole 192-195 phosphoglycolate phosphatase Mus musculus 104-108 9626923-1 1998 OBJECTIVE: We studied a possible pharmacokinetic interaction between clozapine and itraconazole, a potent CYP3A4 inhibitor. Itraconazole 83-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-112 9594936-11 1998 Itraconazole has an affinity for mammalian cytochrome P-450 enzymes as well as for fungal P-450-dependent enzyme, and thus has the potential for clinically important interactions (e.g., astemizole, terfenadine, rifampin, oral contraceptives, H2 receptor antagonists, warfarin, cyclosporine). Itraconazole 0-12 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 43-59 9626922-2 1998 Itraconazole strongly interacts with many substrates of CYP3A4 such as midazolam and triazolam. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 9584328-5 1998 Ketoconazole inhibited oxybutynin N-deethylation by the recombinant CYP3A4 and CYP3A5 almost completely, whereas itraconazole inhibited the activity of CYP3A4 more potently than that of CYP3A5. Itraconazole 113-125 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 152-158 9390107-2 1997 Itraconazole interacts with some but not all of the substrates of CYP3A4; it is therefore important to study the possible interaction of itraconazole with quinidine. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 9551703-2 1998 Itraconazole is an inhibitor of CYP3A4, whereas fluconazole affects CYP2C9 more than CYP3A4. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 9542477-0 1998 Simvastatin but not pravastatin is very susceptible to interaction with the CYP3A4 inhibitor itraconazole. Itraconazole 93-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 9542477-1 1998 BACKGROUND: Itraconazole increases the risk of skeletal muscle toxicity of some 3-hydroxy-3-methylglutaryl coenzyme A" (HMG-CoA) reductase inhibitors by increasing their serum concentrations. Itraconazole 12-24 3-hydroxy-3-methylglutaryl-CoA reductase Homo sapiens 80-138 9542477-14 1998 CONCLUSIONS: Itraconazole greatly increased serum concentrations of simvastatin, simvastatin acid, and HMG CoA reductase inhibitors, probably by inhibiting CYP3A-mediated metabolism, but it had only a minor effect on pravastatin. Itraconazole 13-25 3-hydroxy-3-methylglutaryl-CoA reductase Homo sapiens 103-120 9421099-1 1997 Itraconazole strongly interacts with some drugs metabolized by cytochrome P450 3A4, for example, felodipine and lovastatin, by inhibiting their metabolism. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-82 9390107-12 1997 CONCLUSIONS: Itraconazole increases plasma concentrations of oral quinidine, probably by inhibiting the CYP3A4 isozyme during the first-pass and elimination phases of quinidine. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 104-110 9321523-11 1997 SV was > 30-fold less potent than ketoconazole and itraconazole as an inhibitor of CYP3A. Itraconazole 54-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-91 9326581-9 1997 Azole antibiotics (clotrimazole, ketoconazole, and itraconazole) widely used to combat fungal infections are known to do so by inhibiting the ERG11 gene product, the 14alpha-demethylase. Itraconazole 51-63 sterol 14-demethylase Saccharomyces cerevisiae S288C 142-147 9333111-2 1997 Erythromycin and itraconazole are potent inhibitors of CYP3A4, and they increase plasma concentrations and effects of certain drugs, for example, oral midazolam and triazolam. Itraconazole 17-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 9386354-8 1997 160 ng/g-4, 010 ng/g of itraconazole was detected in aspergilloma in 4 measurable cases. Itraconazole 24-36 chromosome 6 open reading frame 47 Homo sapiens 7-10 9333111-14 1997 CONCLUSIONS: Both erythromycin and itraconazole greatly increased plasma buspirone concentrations, obviously by inhibiting its CYP3A4-mediated first-pass metabolism. Itraconazole 35-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-133 8936563-11 1996 The mechanism of the itraconazole-digoxin interaction is unclear but may be related to CYP3A4-mediated changes in the pharmacokinetics of digoxin. Itraconazole 21-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-93 16854169-14 1997 Not only fluconazole, ketoconazole and itraconazole are substrates for CDR1, terbinafine and amorolfine have also been established as substrates, BEN(r) overexpression only accounts for fluconazole resistance. Itraconazole 39-51 cerebellar degeneration related protein 1 Homo sapiens 71-75 9129558-2 1997 Itraconazole strongly interacts with some of the substrates of CYP3A4 (e.g., terfenadine, triazolam and lovastatin); hence it is important to uncover the possible interaction of itraconazole with felodipine. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 9129558-2 1997 Itraconazole strongly interacts with some of the substrates of CYP3A4 (e.g., terfenadine, triazolam and lovastatin); hence it is important to uncover the possible interaction of itraconazole with felodipine. Itraconazole 178-190 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 9375500-5 1997 The concentration of itraconazole, ketoconazole or miconazole needed to inhibit iNOS activity by 50% in RAW 264.7 cells, MPM and DLD-1 cells was > or = 10 mumol l-1. Itraconazole 21-33 nitric oxide synthase 2, inducible Mus musculus 80-84 9272412-3 1997 Because itraconazole, a widely used mycotic, is a potent inhibitor of CYP3A4, we wanted to study a possible interaction between oxybutynin and itraconazole. Itraconazole 8-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 70-76 9272412-10 1997 CONCLUSIONS: Itraconazole moderately increases serum concentrations of oxybutynin, probably by inhibiting the CYP3A-mediated metabolism. Itraconazole 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-115 8689812-13 1996 Inhibition of CYP3A4-mediated metabolism probably explains the increased toxicity of lovastatin caused not only by itraconazole but also by cyclosporine, erythromycin, and other inhibitors of CYP3A4. Itraconazole 115-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 8689812-4 1996 Because itraconazole is a potent inhibitor of CYP3A4, we wanted to study a possible interaction between these drugs. Itraconazole 8-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-52 8712747-10 1996 Itraconazole and its analogues are inhibitors of both cytochrome P450 and lipoxygenase and since itraconazole can modulate BU pharmacokinetics, oxidative catabolism is probably a determinant of BU metabolism. Itraconazole 0-12 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 54-86 7995001-2 1994 Ketoconazole and itraconazole may seriously interact with some of the substrates of CYP3A4 (e.g., terfenadine); hence their possible interaction with triazolam in humans is important to uncover. Itraconazole 17-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 8873882-3 1996 Burdens of Histoplasma capsulatum in the liver and spleen of survivors showed that D0870 given QD or QOD and itraconazole given BID caused dose-responsive reduction of infectious burden. Itraconazole 109-121 BH3 interacting domain death agonist Mus musculus 128-131 18611706-1 1996 Itraconazole is an orally active, broad-spectrum, triazole antifungal agent which has a higher affinity for fungal cytochrome P-450 than ketoconazole but a low affinity for mammalian cytochrome P-450. Itraconazole 0-12 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 115-131 18611706-1 1996 Itraconazole is an orally active, broad-spectrum, triazole antifungal agent which has a higher affinity for fungal cytochrome P-450 than ketoconazole but a low affinity for mammalian cytochrome P-450. Itraconazole 0-12 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 183-199 8605275-6 1996 These results suggested the involvement of itraconazole in the mdr gene and/or mrp gene product-associated resistance. Itraconazole 43-55 ATP binding cassette subfamily C member 1 Homo sapiens 79-82 8846621-6 1995 The azole antifungal agents ketoconazole and itraconazole are potent inhibitors of human CYP3A isoforms. Itraconazole 45-57 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-94 10684424-3 1996 Itraconazole, an oral antifungal agent, is an inhibitor of cytochrome P450 (CYP3A4) metabolism and may elevate serum drug levels of compounds metabolized by this pathway. Itraconazole 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 7884727-1 1994 Eight cats with histoplasmosis were treated with itraconazole at 5 mg/kg per dose PO bid. Itraconazole 49-61 BH3 interacting domain death agonist Felis catus 85-88 1319312-7 1992 Over the past 8 years, itraconazole has been used in clinical trials for all 3 mycoses. Itraconazole 23-35 paired box 5 Homo sapiens 73-78 8064660-2 1994 Two horses with Aspergillus spp nasal granulomas and 1 horse with Conidiobolus coronatus nasal infection were treated with itraconazole (3 mg/kg PO bid). Itraconazole 123-135 BH3 interacting domain death agonist Equus caballus 148-151 8064660-7 1994 Itraconazole (3 mg/kg PO bid) appears to be effective in the treatment of nasal Aspergillus spp infections in horses because the fungal infection was eliminated in both horses. Itraconazole 0-12 BH3 interacting domain death agonist Equus caballus 25-28 1330944-5 1992 Similar observations were made in experiments using IL-2-stimulated CTLL-2 cells: the growth inhibition in the presence of 10 microM ketoconazole or 1 microM itraconazole could be counteracted by increased serum supplementation. Itraconazole 158-170 interleukin 2 Mus musculus 52-56 7518966-2 1994 Nonspecific inhibitors of cytochrome P-450, such as ketoconazole, itraconazole, fluconazole and SKF 525 A, and most of the cytochrome P-450 IIIA specific substrates used in this study significantly inhibited FK 506 metabolism. Itraconazole 66-78 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 26-42 7518966-2 1994 Nonspecific inhibitors of cytochrome P-450, such as ketoconazole, itraconazole, fluconazole and SKF 525 A, and most of the cytochrome P-450 IIIA specific substrates used in this study significantly inhibited FK 506 metabolism. Itraconazole 66-78 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 123-139 33771716-4 2021 In this study, we aimed to estimate the effect of itraconazole (a strong inhibitor of CYP3A4) on the pharmacokinetics of alflutinib. Itraconazole 50-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-92 1951574-9 1991 The triazole antifungals, terconazole and itraconazole, combine a high affinity for Candida P-45014DM with an exceptionally low effect on mammalian cytochrome P-450. Itraconazole 42-54 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 92-101 1951574-9 1991 The triazole antifungals, terconazole and itraconazole, combine a high affinity for Candida P-45014DM with an exceptionally low effect on mammalian cytochrome P-450. Itraconazole 42-54 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 148-164 2128178-3 1990 The effects of the new antimycotic drugs, itraconazole and fluconazole, on the 5-lipoxygenase pathway in human polymorphonuclear leukocytes (PMNL), on the eicosanoid metabolism in platelets, platelet aggregation and on cyclooxygenase activity were investigated and compared with miconazole and ketoconazole. Itraconazole 42-54 arachidonate 5-lipoxygenase Homo sapiens 79-93 2091733-9 1990 Of all the azoles tested, itraconazole shows the highest affinity for the cytochrome P450 involved. Itraconazole 26-38 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 85-89 2091733-11 1990 Itraconazole"s high affinity for the fungal P450 originates from its triazole group as well as from the nonligating lipophilic tail. Itraconazole 0-12 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 44-48 2128178-4 1990 Itraconazole inhibited the formation of 5-lipoxygenase metabolites in human PMNL (IC50 = 2 x 10(-6) mol/l), while it had no effect on cyclooxygenase and platelet aggregation at concentrations up to 10(-4) mol/l and 10(-5) mol/l, respectively. Itraconazole 0-12 arachidonate 5-lipoxygenase Homo sapiens 40-54 33235852-0 2020 Topical Itraconazole Formulations: Unscrupulous Pharmaceutical Companies and Lax Indian Drug Regulators Endangering a Precious Drug. Itraconazole 8-20 lymphocyte transmembrane adaptor 1 Homo sapiens 77-80 34417912-4 2022 Clinical studies investigated the effect of a strong CYP3A4 inhibitor (itraconazole) and inducer (rifampin) on single-dose entrectinib pharmacokinetics. Itraconazole 71-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59