PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 33826998-4 2021 In the present quantitative study, we investigated the inhibitory effects of three azole antifungals (ketoconazole, voriconazole, and fluconazole) on testosterone metabolism by recombinant CYP3A4 genetic variants (CYP3A4.1 (WT), CYP3A4.2, CYP3A4.7, CYP3A4.16, and CYP3A4.18) and compared them with those previously reported for itraconazole. Fluconazole 134-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 189-195 33826998-4 2021 In the present quantitative study, we investigated the inhibitory effects of three azole antifungals (ketoconazole, voriconazole, and fluconazole) on testosterone metabolism by recombinant CYP3A4 genetic variants (CYP3A4.1 (WT), CYP3A4.2, CYP3A4.7, CYP3A4.16, and CYP3A4.18) and compared them with those previously reported for itraconazole. Fluconazole 134-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 214-220 33826998-4 2021 In the present quantitative study, we investigated the inhibitory effects of three azole antifungals (ketoconazole, voriconazole, and fluconazole) on testosterone metabolism by recombinant CYP3A4 genetic variants (CYP3A4.1 (WT), CYP3A4.2, CYP3A4.7, CYP3A4.16, and CYP3A4.18) and compared them with those previously reported for itraconazole. Fluconazole 134-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 214-220 32691891-0 2021 Physiologically-Based Pharmacokinetic Modeling Characterizes the CYP3A-Mediated Drug-Drug Interaction Between Fluconazole and Sildenafil in Infants. Fluconazole 110-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-70 32691891-3 2021 To account for developmental changes in cytochrome P450 (CYP) 3A, we determined and incorporated fluconazole inhibition constants (KI ) for CYP3A4, CYP3A5, and CYP3A7 into a PBPK model developed for sildenafil and its active metabolite, N-desmethylsildenafil. Fluconazole 97-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-146 31475367-9 2019 Co-administration of fluconazole (n=4), a CYP3A inhibitor, resulted in an estimated 59% decrease in sildenafil clearance. Fluconazole 21-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-47 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. Fluconazole 32-43 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 291-297 30301385-6 2019 Co-administration of probenecid (an UGT2B7 inhibitor) or fluconazole (an UGT2B7 and CYP3A4 inhibitor) was predicted to increase area under the curve for mirabegron to 115% or 174%, respectively. Fluconazole 57-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 31090092-7 2019 5-HMT fractional clearance by CYP3A and CYP2D6 was verified from clinical DDI studies with a potent CYP3A4 inhibitor (ketoconazole) and inducer (rifampicin) in CYP2D6 extensive and poor metabolizers and with a moderate CYP3A inhibitor (fluconazole) in healthy volunteers. Fluconazole 236-247 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-35 31090092-7 2019 5-HMT fractional clearance by CYP3A and CYP2D6 was verified from clinical DDI studies with a potent CYP3A4 inhibitor (ketoconazole) and inducer (rifampicin) in CYP2D6 extensive and poor metabolizers and with a moderate CYP3A inhibitor (fluconazole) in healthy volunteers. Fluconazole 236-247 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 31145690-12 2019 The previous minimal PBPK model was supported by the FDA for the dose reduction strategy, halving the dose with the concomitant use of strong CYP3A4 inhibitors and dual inhibitors on CYP2C9 and CYP3A4, such as fluconazole at <=200 mg. Fluconazole simulation results were used as supportive evidence in discussions with the FDA and EMA about ruxolitinib dose adjustment when co-administering perpetrator drugs. Fluconazole 210-221 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 194-200 30912163-0 2019 Perpetrator effects of ciclosporin (P-glycoprotein inhibitor) and its combination with fluconazole (CYP3A inhibitor) on the pharmacokinetics of rivaroxaban in healthy volunteers. Fluconazole 87-98 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-105 30912163-2 2019 The aim of the present study was to investigate the effects of the potent P-gp inhibitor ciclosporin and its combination with the moderate CYP3A inhibitor fluconazole on rivaroxaban pharmacokinetics and on CYP3A activity. Fluconazole 155-166 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-144 30912163-7 2019 Ciclosporin combined with fluconazole increased rivaroxaban average exposure by 86% (58-119%) and maximum concentration by 115% (83-153%), which was considerably stronger than observed in historical controls receiving rivaroxaban with fluconazole alone, and decreased CYP3A4 activity by 79% (76-82%). Fluconazole 26-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 268-274 30676743-3 2019 Metyrapone and fluconazole are classic type II ligands that inhibit CYP3A4 with medium strength by ligating to the heme iron, whereas PMSF, lacking the heme-ligating moiety, acts as a weak type I ligand and inhibitor of CYP3A4. Fluconazole 15-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-74 30676743-3 2019 Metyrapone and fluconazole are classic type II ligands that inhibit CYP3A4 with medium strength by ligating to the heme iron, whereas PMSF, lacking the heme-ligating moiety, acts as a weak type I ligand and inhibitor of CYP3A4. Fluconazole 15-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 220-226 28249055-4 2017 The trigger for our patient"s statin-induced rhabdomyolysis was fluconazole, a known moderate inhibitor of CYP3A4, which is comparatively weaker than certain potent azoles like itraconazole or ketoconazole. Fluconazole 64-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-113 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. Fluconazole 117-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 170-176 27430348-0 2016 Rhabdomyolysis caused by the moderate CYP3A4 inhibitor fluconazole in a patient on stable atorvastatin therapy: a case report and literature review. Fluconazole 55-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 27430348-6 2016 WHAT IS NEW AND CONCLUSION: Our case demonstrates that in some subjects even a moderate CYP3A4 inhibitor such as fluconazole may lead to rhabdomyolysis in subjects receiving a statin. Fluconazole 113-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 26471025-4 2015 This case report describes an incident with QTc prolongation which was probably caused by an interaction induced by a combination of amiodarone, clarithromycin and the CYP3A4-inhibitor fluconazole. Fluconazole 185-196 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 168-174 25670523-3 2015 The model prospectively predicts that 100-200 mg daily dose of fluconazole, a dual inhibitor of CYP3A4 and 2C9, would increase ruxolitinib plasma concentration area under the curve by ~two-fold, and that as a perpetrator, ruxolitinib is highly unlikely to have any discernible effect on digoxin, a sensitive P-glycoprotein substrate. Fluconazole 63-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-110 27128233-3 2014 Two Phase 1, randomized, open-label, single sequence studies in 24 healthy subjects (12 per study) characterized the effects of fluconazole (moderate CYP3A4/potent CYP2C19 inhibitor) and ketoconazole (potent CYP3A4 inhibitor) on tofacitinib pharmacokinetics. Fluconazole 128-139 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-156 25429674-3 2014 Fluconazole, itraconazole, and voriconazole were relatively less potent inhibitors of CYP3A5 than of CYP3A4. Fluconazole 0-11 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. Fluconazole 26-37 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. Fluconazole 133-144 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. Fluconazole 133-144 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 216-222 22048224-0 2012 Evidence of CYP3A allosterism in vivo: analysis of interaction between fluconazole and midazolam. Fluconazole 71-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-17 22048224-1 2012 The allosteric effect of fluconazole (effector) on the formation of 1"-hydroxymidazolam (1"-OH-MDZ) and 4-hydroxymidazolam (4-OH-MDZ) from midazolam (MDZ), a substrate of CYP3A4/5--members of the cytochrome P450 superfamily of enzymes--was examined in healthy volunteers. Fluconazole 25-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 171-177 21545485-0 2011 Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Fluconazole 42-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 21545485-4 2011 AIMS: To assess the effects of fluconazole, a moderate CYP3A4 inhibitor, on the pharmacokinetics (PK) and safety/tolerability of fesoterodine. Fluconazole 31-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 19889796-3 2010 In addition, this approach was successfully extended to DDI predictions with the moderate competitive CYP3A inhibitor fluconazole for nine marketed drugs. Fluconazole 118-129 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-107 21712512-4 2011 Seven weeks after the initiation of inhaled fluticasone, she developed vaginal candidiasis and was prescribed fluconazole 100 mg/day, a CYP3A4 inhibitor. Fluconazole 110-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 136-142 24451503-13 2011 This suggests that in the presence of renal function alteration even low doses of fluconazole with an inhibition of only liver CYPA3A4 (without inhibition of intestinal CYP3A4 and P-gp) leads to an increase on tacrolimus concentration and occurrence of adverse effects related to tacrolimus toxicity. Fluconazole 82-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-175 18381488-3 2008 Whereas ketoconazole is often used to study the worst-case scenario for clinical pharmacokinetic drug-drug interactions (DDIs) for drugs that are primarily metabolized by CYP3A4, fluconazole is considered to be a moderate inhibitor of CYP3A4, providing assessment of the moderate-case scenario of CYP3A-based DDIs. Fluconazole 179-190 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 235-241 20175801-2 2009 Fluconazole, an antifungal agent and an inhibitor of CYP3A4 is an established part of the therapy in HIV patients, who in turn are prone to malaria in the tropics. Fluconazole 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 20175801-10 2009 CONCLUSION: The decreased plasma concentrations of the metabolite are presumably caused by metabolic inhibition of CYP3A4 by fluconazole. Fluconazole 125-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 18812562-14 2008 According to the different inhibitory potency of CYP3A4 activity, the reduction should be lower during fluconazole than during voriconazole cotreatment. Fluconazole 103-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-55 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. Fluconazole 57-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 17954524-3 2008 Fluconazole was a slightly more potent inhibitor of CYP3A activity in CYP3A5-HLM than in CYP3A5+ HLM with midazolam (K(i) of 15 and 25 microM, respectively) but not with erythromycin (IC(50) of 70 and 54 microM, respectively). Fluconazole 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-57 11932962-3 2002 Fluconazole is a potent competitive inhibitor of CYP2C19 and a weak inhibitor of CYP3A4. Fluconazole 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 15843491-8 2005 Fluconazole (CYP2C9/19 and CYP3A4 inhibitor at clinical concentrations) inhibited hydroxylamine formation, with one-enzyme model K(i) estimates ranging from 9 to 40 microM. Fluconazole 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 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. Fluconazole 234-245 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-42 16205037-3 2005 Fluconazole, micafungin, and voriconazole have lower inhibitory effects on CYP3A4 activities than itraconazole and miconazole, and IC(50) and/or K(i) values against CYP2C9 and CYP2C19 activities are the lowest for miconazole, followed by voriconazole and fluconazole. Fluconazole 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 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). Fluconazole 157-168 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). Fluconazole 157-168 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). Fluconazole 157-168 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 286-292 15963096-1 2005 AIMS: Our objective was to study in vivo the role of CYP2C and CYP3A4 in the disposition of 3-keto-desogestrel after administration of desogestrel, by using the selective inhibitors fluconazole (CYP2C) and itraconazole (CYP3A4). Fluconazole 182-193 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 8520811-1 1995 Fluconazole, an azole antifungal agent, moderately inhibits the CYP3A-mediated metabolism of midazolam in vitro. Fluconazole 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 12405865-14 2002 Inhibitors of CYP3A4, such as fluconazole, and of CYP2D6, such as paroxetine, increase methadone blood concentrations. Fluconazole 30-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 10923859-11 2000 Rifalazil-32-hydroxylation in microsomes was completely inhibited by CYP3A4-specific inhibitors (fluconazole, ketoconazole, miconazole, troleandomycin) and drugs metabolized by CYP3A4 such as cyclosporin A and clarithromycin, indicating that the enzyme responsible for the rifalazil-32-hydroxylation is CYP3A4. Fluconazole 97-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 10709776-9 2000 The potency of fluconazole as a CYP3A4 inhibitor is much lower. Fluconazole 15-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 10709776-10 2000 Thus, clinical interactions of CYP3A substrates with this azole derivative are of lesser magnitude, and are generally observed only with fluconazole dosages of > or =200 mg/day. Fluconazole 137-148 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-36 10730911-4 1999 For example, itraconazole, and to a lesser extent fluconazole (in high doses) are inhibitors of CYP3A4. Fluconazole 50-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102 10456482-6 1999 As an example, prediction and validation studies of CYP3A4 inhibition by ketoconazole and fluconazole will be discussed. Fluconazole 90-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 10341997-2 1999 The antimycotic fluconazole is often used in these patients as well and has been shown to inhibit CYP3A4-mediated drug metabolism. Fluconazole 16-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 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. Fluconazole 43-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 10466905-9 1999 Fluconazole is renally excreted but has been noted to inhibit CYP3A4. Fluconazole 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 10466905-11 1999 CONCLUSIONS: Fluconazole may cause carbamazepine toxicity presumably by inhibiting the cytochrome P450 3A4 isoenzyme. Fluconazole 13-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-106 9929500-8 1999 For liver and intestinal microsomes that contained only CYP3A4, the average ketoconazole Ki was found to be 14.9 +/- 6.7 nM and 17.0 +/- 7.9 nM, respectively, whereas fluconazole yielded mean respective Ki values of 10.7 +/- 4.2 microM and 10.4 +/- 2.9 microM. Fluconazole 167-178 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 9929500-9 1999 Liver and intestinal microsomes that contained an equal or greater amount of CYP3A5, in addition to CYP3A4, were less susceptible to inhibition by both ketoconazole and fluconazole. Fluconazole 169-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 34851444-4 2022 We evaluated the pharmacokinetics and tolerability of fuzuloparib by fluconazole, which is a broad antifungal agent and a moderate inhibitor of CYP3A4. Fluconazole 69-80 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 144-150 35165925-14 2022 CONCLUSION: Our results demonstrated the impact of fluconazole and isavuconazole on the pharmacokinetics of acalabrutinib and ACP-5862 and suggests no dose adjustment is needed for concomitant administration with moderate CYP3A inhibitors. Fluconazole 51-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 222-227 35238961-10 2022 Both fluconazole and rifampicin altered CYP3A4 activity whereas no change of CYP2D6 activity was observed at all. Fluconazole 5-16 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-46