PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 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 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 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 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 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 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 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 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 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 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 11465417-9 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 9695720-2 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 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 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 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 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 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 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 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 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 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 9390107-2 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 34426442-1 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 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 34267345-3 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 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 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 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 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 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 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 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 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 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 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 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 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 72-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-105 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 30171694-7 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 25429674-5 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 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 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 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 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 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 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 21838784-7 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 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 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 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 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 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 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 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 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 3 subfamily A member 4 Homo sapiens 121-127 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 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 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 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 3 subfamily A member 4 Homo sapiens 130-136 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 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 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 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 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 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 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 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 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 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-71 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 3 subfamily A member 4 Homo sapiens 115-121 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 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 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 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 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 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 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 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 15770075-2 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 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 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 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 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 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 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 4 Homo sapiens 322-328 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 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