PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 33974505-0 2021 Association of polymorphism of CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR with the concentration of cyclosporin a in allogeneic hematopoietic stem cell transplantation recipients. Cyclosporine 106-119 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 33991364-4 2021 Previous reports indicate increased systemic exposures of cyclosporine and sirolimus in patients receiving high-dose marine omega-3 FA supplements (3, 4) which could be related to reduced drug metabolism supported by the in vitro experimental observation of an inhibitory effect of omega-3 FAs on cytochrome P450 (CYP) 3A enzymes (5) expressed in the intestine and liver. Cyclosporine 58-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 297-321 34306041-9 2021 CYP3A4*22 was shown to significantly influence the pharmacokinetics of several drugs, with currently being most thoroughly investigated tacrolimus, cyclosporine, and statins. Cyclosporine 148-160 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 33974505-2 2021 In this study, we aimed to identify the association of CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR polymorphisms with CsA concentrations in patients with allogeneic hematopoietic cell transplantation (allo-HSCT) based on the route of administration.A total of 40 allo-HSCT recipients receiving CsA were genotyped for CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR polymorphisms. Cyclosporine 123-126 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 322-328 33974505-2 2021 In this study, we aimed to identify the association of CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR polymorphisms with CsA concentrations in patients with allogeneic hematopoietic cell transplantation (allo-HSCT) based on the route of administration.A total of 40 allo-HSCT recipients receiving CsA were genotyped for CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR polymorphisms. Cyclosporine 123-126 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 32967779-2 2020 Typical CYP3A4-substrates including erythromycin, cyclosporin A (ca.1200 Da), ivermectin B1a and taxanes were applied successfully and regioselective metabolisms of these ligands were reconstituted faithfully on Template. Cyclosporine 50-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 8-14 31248333-3 2020 We present a case of a 41-year-old woman with a stable living-related kidney transplant maintained on an immunosuppressive regimen of cyclosporine, mycophenolate mofetil, and prednisone, who was subsequently diagnosed with a metastatic lobular breast carcinoma and papillary thyroid cancer and started palbociclib, a time-dependent CYP3A inhibitor. Cyclosporine 134-146 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 332-337 32682934-10 2020 The saturated binding of ciclosporin to erythrocytes, auto-inhibition induced by the inhibitory effects of ciclosporin on cytochrome P450 3A4/P-glycoprotein may have contributed to the nonlinearity. Cyclosporine 25-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-141 32682934-10 2020 The saturated binding of ciclosporin to erythrocytes, auto-inhibition induced by the inhibitory effects of ciclosporin on cytochrome P450 3A4/P-glycoprotein may have contributed to the nonlinearity. Cyclosporine 107-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-141 30799725-11 2019 Conclusion: This study revealed the possible association of IL-17 G-197A with cyclosporine metabolism and transplant rejection after LT, which might be partly related to the upregulations of CYP3A4/5 dependent on PXR. Cyclosporine 78-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 191-199 32222391-13 2020 CONCLUSION: The study results suggest that in KTX metabolic transformations and transport, especially of cyclosporine, dependence on the genetic variability of CYP3A4, UGT1A9, and MDR1 may contribute to kidney damage. Cyclosporine 105-117 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 160-166 31261526-5 2019 The most commonly reported genotype was CYP3A53/3, which was strongly associated with cyclosporine A (CsA) and tacrolimus (FK506). Cyclosporine 86-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-49 31261526-5 2019 The most commonly reported genotype was CYP3A53/3, which was strongly associated with cyclosporine A (CsA) and tacrolimus (FK506). Cyclosporine 102-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-49 32162881-8 2020 Moreover, frequent TDM monitoring as well as CYP3A4/CYP3A5/MDR1 genotyping were given so as to tailor the oral dosage of cyclosporine individually and prevent the adverse reaction between cyclosporine and posaconazole. Cyclosporine 121-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 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. Cyclosporine 89-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 206-211 30912163-6 2019 RESULTS: Compared to baseline, ciclosporin increased rivaroxaban average exposure by 47% (90% confidence interval 28-68%), maximum concentration by 104% (70-146%), and decreased CYP3A4 activity by 34% (25-42%). Cyclosporine 31-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 178-184 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%). Cyclosporine 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 268-274 31156436-2 2019 Metabolized mainly by CYP3A and being a substrate of P-glycoprotein (P-gp), CsA is susceptible to drug-drug interactions. Cyclosporine 76-79 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-27 30799432-0 2019 Effect of Multidrug-Resistant 1 (MDR1) and CYP3A4*1B Polymorphisms on Cyclosporine-Based Immunosuppressive Therapy in Renal Transplant Patients. Cyclosporine 70-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 30799432-4 2019 The aim of this study was to determine the relationship between CYP3A4*1B and MDR1 polymorphisms and dose requirements to achieve the target therapeutic range for CsA. Cyclosporine 163-166 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-70 30799432-7 2019 RESULTS Patients with the CYP3A4*1/*1 genotype received the lowest mean dose of CsA compared to CYP3A4*1/*1B, and had a higher average drug concentration in the blood. Cyclosporine 80-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 31385766-0 2019 Association Between CYP3A4 and CYP3A5 Genotypes and Cyclosporine"s Blood Levels and Doses among Jordanian Kidney Transplanted Patients BACKGROUND: Cyclosporine is used as an immunosuppressive agent in kidney transplantation. Cyclosporine 52-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 30378493-12 2019 CYP3A families, especially CYP3A4 and CYP3A5, play an important role in the biotransformation of CsA. Cyclosporine 97-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 31385766-0 2019 Association Between CYP3A4 and CYP3A5 Genotypes and Cyclosporine"s Blood Levels and Doses among Jordanian Kidney Transplanted Patients BACKGROUND: Cyclosporine is used as an immunosuppressive agent in kidney transplantation. Cyclosporine 147-159 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 31385766-2 2019 Cyclosporine is predominantly metabolized by CYP3A4 and CYP3A5. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 31385766-3 2019 The most commonSingle Nucleotide Polymorphisms (SNPs) affecting cyclosporine metabolism (CYP3A4*1B, CYP3A4*1G,CYP3A4*22 and CYP3A5*3) were investigated among Jordanian kidney transplanted patients to find out the genotypesand allele frequencies of these SNPs. Cyclosporine 64-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 31385766-3 2019 The most commonSingle Nucleotide Polymorphisms (SNPs) affecting cyclosporine metabolism (CYP3A4*1B, CYP3A4*1G,CYP3A4*22 and CYP3A5*3) were investigated among Jordanian kidney transplanted patients to find out the genotypesand allele frequencies of these SNPs. Cyclosporine 64-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 31385766-3 2019 The most commonSingle Nucleotide Polymorphisms (SNPs) affecting cyclosporine metabolism (CYP3A4*1B, CYP3A4*1G,CYP3A4*22 and CYP3A5*3) were investigated among Jordanian kidney transplanted patients to find out the genotypesand allele frequencies of these SNPs. Cyclosporine 64-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 27519420-10 2016 The pharmacological interaction between vinflunine and cyclosporine, both metabolized by CYP 3A4, may explain the excellent result and the concomitant severe toxicity. Cyclosporine 55-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-96 29712725-3 2018 CsA is an inhibitor of organic anion transporting polypeptide (OATP)1B1 and CYP3A4, and GEM and its glucuronide (GEM-glu) inhibit OATP1B1 and CYP2C8. Cyclosporine 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 28479356-5 2017 The time profiles of RPG and the inhibitors were analyzed by PBPK models, considering the inhibition of OATP1B1 and CYP3A4 by CsA or OATP1B1 inhibition by GEM and its glucuronide and the mechanism-based inhibition of CYP2C8 by GEM glucuronide. Cyclosporine 126-129 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 116-122 28616429-2 2017 It can increase blood concentrations of other medications including cyclosporine A (CsA) which are substrates for cytochrome P450 3A4. Cyclosporine 68-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-133 28616429-2 2017 It can increase blood concentrations of other medications including cyclosporine A (CsA) which are substrates for cytochrome P450 3A4. Cyclosporine 84-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-133 30044899-0 2018 Amenamevir: Studies of Potential CYP3A-Mediated Pharmacokinetic Interactions With Midazolam, Cyclosporine, and Ritonavir in Healthy Volunteers. Cyclosporine 93-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-38 29678659-0 2018 Association of CYP3A4*1B genotype with Cyclosporin A pharmacokinetics in renal transplant recipients: A meta-analysis. Cyclosporine 39-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-21 29678659-2 2018 CYP3A4*1B is reported to be associated with CsA pharmacokinetics parameters, but the relevance is still in dispute. Cyclosporine 44-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 29678659-3 2018 Therefore, a meta-analysis was employed to evaluate the influence of CYP3A4*1B on CsA pharmacokinetics at different post-transplantation times in adult renal transplant recipients. Cyclosporine 82-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 29678659-11 2018 CONCLUSIONS: CYP3A4*1B is associated with CsA C0/Dose ratio in renal transplant recipients which indicates patients with CYP3A4*1B allele require lower dose of CsA to reach target blood concentration compared with the CYP3A4*1 carriers. Cyclosporine 42-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-19 29678659-11 2018 CONCLUSIONS: CYP3A4*1B is associated with CsA C0/Dose ratio in renal transplant recipients which indicates patients with CYP3A4*1B allele require lower dose of CsA to reach target blood concentration compared with the CYP3A4*1 carriers. Cyclosporine 42-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 29678659-11 2018 CONCLUSIONS: CYP3A4*1B is associated with CsA C0/Dose ratio in renal transplant recipients which indicates patients with CYP3A4*1B allele require lower dose of CsA to reach target blood concentration compared with the CYP3A4*1 carriers. Cyclosporine 42-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 29678659-11 2018 CONCLUSIONS: CYP3A4*1B is associated with CsA C0/Dose ratio in renal transplant recipients which indicates patients with CYP3A4*1B allele require lower dose of CsA to reach target blood concentration compared with the CYP3A4*1 carriers. Cyclosporine 160-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-19 29678659-11 2018 CONCLUSIONS: CYP3A4*1B is associated with CsA C0/Dose ratio in renal transplant recipients which indicates patients with CYP3A4*1B allele require lower dose of CsA to reach target blood concentration compared with the CYP3A4*1 carriers. Cyclosporine 160-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 29678659-11 2018 CONCLUSIONS: CYP3A4*1B is associated with CsA C0/Dose ratio in renal transplant recipients which indicates patients with CYP3A4*1B allele require lower dose of CsA to reach target blood concentration compared with the CYP3A4*1 carriers. Cyclosporine 160-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 29801578-4 2018 For calcineurin inhibitors like cyclosporine and in particular tacrolimus however, cytochrome P450 3A4 and 3A5 variants were found to significantly affect the pharmacokinetics. Cyclosporine 32-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-102 29135906-1 2017 BACKGROUND: The interindividual variability of cyclosporin A (CsA) pharmacokinetics might be explained by heterogeneity in the cytochrome P450 3A (CYP3A) subfamily. Cyclosporine 47-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-145 29135906-1 2017 BACKGROUND: The interindividual variability of cyclosporin A (CsA) pharmacokinetics might be explained by heterogeneity in the cytochrome P450 3A (CYP3A) subfamily. Cyclosporine 47-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 147-152 29135906-1 2017 BACKGROUND: The interindividual variability of cyclosporin A (CsA) pharmacokinetics might be explained by heterogeneity in the cytochrome P450 3A (CYP3A) subfamily. Cyclosporine 62-65 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-145 29135906-1 2017 BACKGROUND: The interindividual variability of cyclosporin A (CsA) pharmacokinetics might be explained by heterogeneity in the cytochrome P450 3A (CYP3A) subfamily. Cyclosporine 62-65 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 147-152 29135906-3 2017 The aim of this study was to assess the impact of age, CYP3A5*3, CYP3A4*22, and POR*28 alleles on CsA pharmacokinetics in pediatric renal transplant recipients. Cyclosporine 98-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-71 28952408-0 2017 Influence of CYP3A and ABCB1 polymorphisms on cyclosporine concentrations in renal transplant recipients. Cyclosporine 46-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-18 28952408-1 2017 AIM: Cyclosporine is a substrate of CYP3A and ABCB1. Cyclosporine 5-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-41 28722255-3 2017 All of these agents are inhibitors of cytochrome P450 3A4, which plays a key role in metabolizing immunosuppressant drugs such as cyclosporine, tacrolimus, and sirolimus. Cyclosporine 130-142 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-57 27310200-8 2016 Cyclosporine predominantly inhibited CYP3A4 (half maximal inhibitory concentration = 0.71 microM) rather than CYP3A5 (>5 microM), whereas tacrolimus showed similar inhibition for CYP3A4 (0.29 microM) and CYP3A5 (0.41 microM). Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 26259716-5 2016 The interplay between hepatic uptake and CYP3A4 metabolism was verified by simulations with rifampicin, a potent CYP3A4 inducer and OATP1B1/3 inhibitor, and maintenance doses of cyclosporine. Cyclosporine 178-190 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 26950050-5 2016 The impact of phenotyping on the dose selection and pharmacokinetics of CYP3A substrates (docetaxel, irinotecan, tyrosine kinase inhibitors, ciclosporin, tacrolimus) are reviewed. Cyclosporine 141-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-77 26385839-5 2016 It performed well in recovering the observed effect of the CYP3A4 inhibitors ketoconazole and cyclosporine, and the CYP3A4 inducer rifampicin, as well as in predicting interactions with S-warfarin and sildenafil. Cyclosporine 94-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-65 26713664-7 2016 Moreover, CsA is highly metabolized by cytochrome P450 3A4 (CYP3A4), a polymorphic enzyme leading to variations of Cmax and AUC between 10-20% in patients using CsA. Cyclosporine 10-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-58 26713664-7 2016 Moreover, CsA is highly metabolized by cytochrome P450 3A4 (CYP3A4), a polymorphic enzyme leading to variations of Cmax and AUC between 10-20% in patients using CsA. Cyclosporine 10-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 26713664-7 2016 Moreover, CsA is highly metabolized by cytochrome P450 3A4 (CYP3A4), a polymorphic enzyme leading to variations of Cmax and AUC between 10-20% in patients using CsA. Cyclosporine 161-164 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-58 26713664-7 2016 Moreover, CsA is highly metabolized by cytochrome P450 3A4 (CYP3A4), a polymorphic enzyme leading to variations of Cmax and AUC between 10-20% in patients using CsA. Cyclosporine 161-164 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 26271661-2 2015 CYP3A5*3, CYP3A4*1B and CYP3A4*22 alleles of liver grafts may explain about one third of the inter-individual differences in pharmacokinetics of ciclosporin and tacrolimus in recipients. Cyclosporine 145-156 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-16 26353895-8 2016 Cyclosporine is an inhibitor of OATP1B1/3, BCRP and P-gp, and a mild inhibitor of CYP3A; cyclosporine causes a significant increase in simeprevir plasma concentrations, and coadministration is not recommended. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 82-87 26353895-8 2016 Cyclosporine is an inhibitor of OATP1B1/3, BCRP and P-gp, and a mild inhibitor of CYP3A; cyclosporine causes a significant increase in simeprevir plasma concentrations, and coadministration is not recommended. Cyclosporine 89-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 82-87 26912097-6 2016 Cyclosporine disposition is less susceptible to these interactions compared with tacrolimus, possibly because cyclosporine is itself a moderately strong CYP3A4- and strong P-gp inhibitor, blunting the effect of additional inhibitors. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 153-159 26912097-6 2016 Cyclosporine disposition is less susceptible to these interactions compared with tacrolimus, possibly because cyclosporine is itself a moderately strong CYP3A4- and strong P-gp inhibitor, blunting the effect of additional inhibitors. Cyclosporine 110-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 153-159 26271661-2 2015 CYP3A5*3, CYP3A4*1B and CYP3A4*22 alleles of liver grafts may explain about one third of the inter-individual differences in pharmacokinetics of ciclosporin and tacrolimus in recipients. Cyclosporine 145-156 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 26301745-4 2015 These changes could be blocked by the duel CYP3A4/P-glycoprotein inhibitor cyclosporine A, consequently, Papp values for CLA enantiomers in both directions were significantly greater than those obtained by using verapamil or ketoconazole, and their ERs were similar to those following (-) or (+)-isomer treatment alone. Cyclosporine 75-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 26817280-0 2015 A non-invasive CYP3A4 biomarker and body mass index predict cyclosporine dosage requirements in Chinese renal transplant recipients. Cyclosporine 60-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-21 26817280-1 2015 An endogenous CYP3A4 biomarker for in vivo metabolism of cyclosporine should be useful for optimizing individual dosage. Cyclosporine 57-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 26817280-7 2015 In summary, there is a significant relationship between endogenous CYP3A4 biomarker (assessed by urinary HOM) and in vivo metabolism of cyclosporine in renal transplant recipients. Cyclosporine 136-148 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 26150050-7 2015 Regarding the biopharmaceutical characteristics, the endogenous CYP3A biomarker explains 74.5% of variability in oral cyclosporine clearance between individuals. Cyclosporine 118-130 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 25976223-0 2015 CYP3A4*18B and CYP3A5*3 polymorphisms contribute to pharmacokinetic variability of cyclosporine among healthy Chinese subjects. Cyclosporine 83-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 25976223-8 2015 The Cmax of cyclosporine in CYP3A4*1/*1 was significantly greater than that in CYP3A4*1/*18B in the male group (P=0.023), but not the female group. Cyclosporine 12-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-34 25976223-10 2015 CONCLUSIONS: The results indicate that gender and polymorphism in CYP3A4*18B and CYP3A5*3 significantly affect cyclosporine pharmacokinetics in healthy subjects. Cyclosporine 111-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 25512016-5 2015 WHAT IS NEW AND CONCLUSION: Cyclosporine is a moderate inhibitor of the cytochrome P450 CYP3A4 isoenzyme, which is known to increase the serum level of atorvastatin. Cyclosporine 28-40 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 25644970-8 2015 There was a non-significant trend of lower cyclosporine dose requirement in CYP3A4*22 carriers. Cyclosporine 43-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 25280976-2 2014 Calcium channel blockers (CCBs) are considered to be the best treatment for CsA-induced hypertension, but they may alter the exposure and the effect of CsA by inhibiting the CYP3A4 pathway of CsA metabolism or P-gp. Cyclosporine 152-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 25240575-0 2015 Impact of CYP3A4 and MDR1 gene (G2677T) polymorphisms on dose requirement of the cyclosporine in renal transplant Egyptian recipients. Cyclosporine 81-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-16 25240575-6 2015 Interindividual heterogeneity in expression of ABCB1 and CYP3A4 has been suspected to be one of the factors resulting in cyclosporine (CsA) pharmacokinetic variation. Cyclosporine 121-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 25240575-6 2015 Interindividual heterogeneity in expression of ABCB1 and CYP3A4 has been suspected to be one of the factors resulting in cyclosporine (CsA) pharmacokinetic variation. Cyclosporine 135-138 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 25240575-7 2015 This study aimed to investigate the impact of inter-individual CYP3A4 rs4646437C>T and MDR1 G2677T/A polymorphisms on cyclosporine dose requirements among a sample of renal transplant Egyptian recipients. Cyclosporine 121-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 25240575-8 2015 Fifty adult Egyptian patients on CsA were genotyped for CYP3A4 rs4646437C>T and MDR1 G2677T/A and correlated with CsA dose requirement and dose-adjusted CsA (C0) blood levels at 3, 6, and 9 months post transplantation. Cyclosporine 117-120 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 25240575-8 2015 Fifty adult Egyptian patients on CsA were genotyped for CYP3A4 rs4646437C>T and MDR1 G2677T/A and correlated with CsA dose requirement and dose-adjusted CsA (C0) blood levels at 3, 6, and 9 months post transplantation. Cyclosporine 117-120 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 25240575-9 2015 CYP3A4 rs4646437C>T influenced significantly cyclosporine kinetics, the T carriers requiring higher cyclosporine dose. Cyclosporine 48-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 25240575-9 2015 CYP3A4 rs4646437C>T influenced significantly cyclosporine kinetics, the T carriers requiring higher cyclosporine dose. Cyclosporine 103-115 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 25240575-11 2015 Genotyping of both CYP3A4 and MDR1 SNPs may be helpful in providing pre-transplant pharmacogenetic information to individualize CsA dosing. Cyclosporine 128-131 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-25 25280976-2 2014 Calcium channel blockers (CCBs) are considered to be the best treatment for CsA-induced hypertension, but they may alter the exposure and the effect of CsA by inhibiting the CYP3A4 pathway of CsA metabolism or P-gp. Cyclosporine 152-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 25561870-9 2014 Therefore, using Ferula asafetida with CYP3A4 drug substrates should be cautioned especially those with narrow therapeutic index such as cyclosporine, tacrolimus and carbamazepine. Cyclosporine 137-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 24739665-1 2014 BACKGROUND: Previous reports have suggested that imatinib may increase cyclosporine exposure by CYP3A4 inhibition. Cyclosporine 71-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102 24739669-3 2014 We thus assessed the role of genetic variation in CYP3A4, CYP3A5, POR, NR1I2, and ABCB1 acting jointly in immunosuppressive drug pathways in tacrolimus (TAC) and ciclosporin (CSA) dose requirement in HTx recipients. Cyclosporine 162-173 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 24522145-5 2014 CYP3A4*22 carriers showed a significant lower clearance for cyclosporine (-15%), and a trend was observed for everolimus (-7%) and tacrolimus (-16%). Cyclosporine 60-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 24691060-0 2014 Association of CYP3A4*18B and CYP3A5*3 polymorphism with cyclosporine-related liver injury in Chinese renal transplant recipients. Cyclosporine 57-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-21 24691060-1 2014 OBJECTIVE: The purpose of this study was to investigate the associations between CYP3A4*18B and CYP3A5*3 polymorphism and cyclosporine-related liver injuries in Chinese renal transplant recipients. Cyclosporine 122-134 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 24691060-4 2014 At 1 month after transplantation, the trough concentration of cyclosporine (C0) in the group with CYP3A4*1/*1(GG alleles) was significantly higher than in the group with CYP3A4*18B/*1 8B(AA alleles) (p < 0.05). Cyclosporine 62-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 24691060-4 2014 At 1 month after transplantation, the trough concentration of cyclosporine (C0) in the group with CYP3A4*1/*1(GG alleles) was significantly higher than in the group with CYP3A4*18B/*1 8B(AA alleles) (p < 0.05). Cyclosporine 62-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 170-176 24691060-10 2014 CONCLUSIONS: These results suggested that the wild type of CYP3A4*18B is a risk factor for the development of cyclosporine- related liver injuries in Chinese renal transplant recipients. Cyclosporine 110-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-65 25125033-2 2014 This particular characteristic makes it advantageous when combined with drugs metabolized by CYP3A4, such as cyclosporine. Cyclosporine 109-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 24658827-1 2014 PURPOSE: Tacrolimus (Tac) and cyclosporine (CsA) are mainly metabolized by CYP3A4 and CYP3A5. Cyclosporine 30-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 24658827-1 2014 PURPOSE: Tacrolimus (Tac) and cyclosporine (CsA) are mainly metabolized by CYP3A4 and CYP3A5. Cyclosporine 44-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 24658827-10 2014 CsA C2/D was 53 % higher among CYP3A4*22 carriers (P=0.03). Cyclosporine 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 24658827-12 2014 Furthermore, initial CsA dosing may be improved by pre-transplant CYP3A4*22 determination. Cyclosporine 21-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 24990333-9 2014 CONCLUSION: Combining agents that are mainly metabolized by CYP3A4 such as LPZ elevates the blood concentrations of TAC and CSA, which could leading to adverse events. Cyclosporine 124-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 24369269-3 2014 Before initiation of triple therapy, all patients switched from tacrolimus to cyclosporine, which has a lower inhibitory effect on CYP3A4 and CYP3A5 than tacrolimus. Cyclosporine 78-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-137 23557867-0 2013 CYP3A4/5 polymorphisms affect the blood level of cyclosporine and tacrolimus in Chinese renal transplant recipients. Cyclosporine 49-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 24527031-3 2014 Cytochrome P-450 isoenzymes CYP3A4 and CYP3A5 and protein P-glycoprotein (P-gp) are involved in CyA bioavailability. Cyclosporine 96-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-34 23557867-2 2013 We approached the effect of the CYP3A4*18B and CYP3A5*3 polymorphisms and haplotypes on the whole blood cyclosporine or tacrolimus concentration in Chinese renal transplant patients during the first month after transplantation. Cyclosporine 104-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 23557867-10 2013 CONCLUSIONS: Genetic polymorphisms of CYP3A5*3 and CYP3A4*18B may be partly responsible in large interindividual variability of cyclosporine and tacrolimus blood levels in Chinese renal transplant patients during the first month after transplantation. Cyclosporine 128-140 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-57 23085740-0 2012 Association of CYP3A polymorphisms with the pharmacokinetics of cyclosporine A in early post-renal transplant recipients in China. Cyclosporine 64-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-20 23252948-5 2013 A new CYP3A4 allele (CYP3A4*22; rs35599367 C>T in intron 6) with a frequency of 5-7% in the Caucasian population was recently discovered through its association with low hepatic CYP3A4 expression and CYP3A4 activity, and showing effects on statin, tacrolimus and cyclosporine metabolism. Cyclosporine 266-278 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 23252948-5 2013 A new CYP3A4 allele (CYP3A4*22; rs35599367 C>T in intron 6) with a frequency of 5-7% in the Caucasian population was recently discovered through its association with low hepatic CYP3A4 expression and CYP3A4 activity, and showing effects on statin, tacrolimus and cyclosporine metabolism. Cyclosporine 266-278 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 23252948-5 2013 A new CYP3A4 allele (CYP3A4*22; rs35599367 C>T in intron 6) with a frequency of 5-7% in the Caucasian population was recently discovered through its association with low hepatic CYP3A4 expression and CYP3A4 activity, and showing effects on statin, tacrolimus and cyclosporine metabolism. Cyclosporine 266-278 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 23252948-5 2013 A new CYP3A4 allele (CYP3A4*22; rs35599367 C>T in intron 6) with a frequency of 5-7% in the Caucasian population was recently discovered through its association with low hepatic CYP3A4 expression and CYP3A4 activity, and showing effects on statin, tacrolimus and cyclosporine metabolism. Cyclosporine 266-278 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 22886152-2 2013 We have investigated the effect of polymorphisms in the CYP3A and ABCB1 genes on CsA pharmacokinetics, acute rejection incidence and drug-related side effects in renal transplant recipients METHODS: The presence of CYP3A5*3, CYP3A4*1B and ABCB1 C1236T, G2677T/A and C3435T polymorphisms was assessed in 68 patients and retrospectively associated with pharmacokinetic and clinical parameters at 1 week and 1, 5 and 12 months after transplantation. Cyclosporine 81-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-61 23841924-3 2013 The metabolism and bioavailability of cyclosporin can be significantly and persistently influenced through induction of CYP3A4 caused by the concomitant use of rifampicin. Cyclosporine 38-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-126 23085740-1 2012 AIM: To evaluate retrospectively the association of cytochrome P450 3A (CYP3A) and ATP-binding cassette sub-family B member 1 (ABCB1) gene polymorphisms with the pharmacokinetics of cyclosporine A (CsA) in Chinese renal transplant patients. Cyclosporine 182-196 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-70 23085740-1 2012 AIM: To evaluate retrospectively the association of cytochrome P450 3A (CYP3A) and ATP-binding cassette sub-family B member 1 (ABCB1) gene polymorphisms with the pharmacokinetics of cyclosporine A (CsA) in Chinese renal transplant patients. Cyclosporine 182-196 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-77 23217392-1 2012 BACKGROUND: Cyclosporin A (CsA) is a substrate of both cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp), some of the single nucleotide polymorphisms (SNPs) in these genes are associated with interindividual variations in CsA pharmacokinetics. Cyclosporine 27-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-73 23217392-0 2012 CYP3A4 genetic polymorphisms predict cyclosporine-related clinical events in Chinese renal transplant recipients. Cyclosporine 37-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 23217392-1 2012 BACKGROUND: Cyclosporin A (CsA) is a substrate of both cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp), some of the single nucleotide polymorphisms (SNPs) in these genes are associated with interindividual variations in CsA pharmacokinetics. Cyclosporine 27-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-80 23217392-1 2012 BACKGROUND: Cyclosporin A (CsA) is a substrate of both cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp), some of the single nucleotide polymorphisms (SNPs) in these genes are associated with interindividual variations in CsA pharmacokinetics. Cyclosporine 225-228 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-73 23217392-1 2012 BACKGROUND: Cyclosporin A (CsA) is a substrate of both cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp), some of the single nucleotide polymorphisms (SNPs) in these genes are associated with interindividual variations in CsA pharmacokinetics. Cyclosporine 225-228 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-80 23217392-4 2012 Retrospective case control study was utilized to identify the association between CYP3A4 1G, CYP3A5 3, ABCB1 genetic polymorphisms and CsA-related outcomes. Cyclosporine 135-138 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 82-88 22476221-6 2012 Both protease inhibitors can modify the levels of drugs metabolized by the CYP3A/4 pathway, and in posttransplant patients, the protease inhibitors increase the levels of cyclosporine and tacrolimus, with the magnitude of the drug-drug interactions varying with protease inhibitor and type of calcineurin inhibitor (CNI). Cyclosporine 171-183 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-82 22576324-2 2012 Cyclosporine and tacrolimus are calcineurin inhibitor immunosuppressants used to prevent organ rejection after liver transplantation; both are substrates of CYP3A4. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 157-163 23018254-0 2012 Impact of CYP3A4*1B and CYP3A5*3 polymorphisms on the pharmacokinetics of cyclosporine and sirolimus in renal transplant recipients. Cyclosporine 74-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-16 23018254-7 2012 The mean cyclosporine dose in CYP3A4*1/*1B subjects was 455.04+-128.68 mg/day vs. 261.68+-64.72 mg/day in CYP3A4*1/*1 subjects (p<0.001). Cyclosporine 9-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 23018254-8 2012 The mean cyclosporine dose-adjusted trough blood concentrations (ng/ml per mg/kg body weight) in CYP3A4*1/*1B subjects were lower than in the CYP3A4*1/*1 group (37.06+-10.38 vs. 44.63+-13.99; p<0.218). Cyclosporine 9-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 23018254-11 2012 CONCLUSIONS: Genetic polymorphisms in CYP3A4 and CYP3A5 may underlie inter-individual differences in cyclosporine pharmacokinetics after renal transplantation. Cyclosporine 101-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 23018254-12 2012 Patients with at least 1 functional CYP3A5*1 or CYP3A4*1B allele require significantly higher doses of cyclosporine to reach target drug levels compared to patients with the CYP3A4*1 or CYP3A5*3 alleles. Cyclosporine 103-115 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54 23018254-12 2012 Patients with at least 1 functional CYP3A5*1 or CYP3A4*1B allele require significantly higher doses of cyclosporine to reach target drug levels compared to patients with the CYP3A4*1 or CYP3A5*3 alleles. Cyclosporine 103-115 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 22016125-8 2011 Calcineurin inhibitors (cyclosporine, tacrolimus) and mTOR inhibitors (sirolimus, everolimus) are particularly susceptible to the effects of substances that inhibit or induce cytochrome P450 (CYP) 3A4 and P-glycoprotein. Cyclosporine 24-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 175-200 22388796-0 2012 The new CYP3A4 intron 6 C>T polymorphism (CYP3A4*22) is associated with an increased risk of delayed graft function and worse renal function in cyclosporine-treated kidney transplant patients. Cyclosporine 147-159 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 8-14 22388796-0 2012 The new CYP3A4 intron 6 C>T polymorphism (CYP3A4*22) is associated with an increased risk of delayed graft function and worse renal function in cyclosporine-treated kidney transplant patients. Cyclosporine 147-159 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 22205779-0 2012 Cyclosporine A- and tacrolimus-mediated inhibition of CYP3A4 and CYP3A5 in vitro. Cyclosporine 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-60 22205779-3 2012 For CsA, in particular, inhibition of CYP3A has been suggested as the main mechanism of interactions seen clinically with various drugs. Cyclosporine 4-7 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 22205779-4 2012 The aim of this study was to investigate the inhibitory effect and inhibition characteristics of CsA and Tac on CYP3A4 and CYP3A5 in vitro and to evaluate its clinical relevance. Cyclosporine 97-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-118 22205779-5 2012 Inhibition by CsA and Tac was studied using midazolam as the probe substrate in coincubation and preincubation investigations using human liver microsomes (HLMs) as well as specific CYP3A4- and CYP3A5-expressing insect microsomes (Supersomes). Cyclosporine 14-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 182-188 22205779-8 2012 Experiments in Supersomes revealed that Tac inhibited both CYP3A4 and CYP3A5, whereas CsA only inhibited CYP3A4. Cyclosporine 86-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-111 20599501-4 2010 Since Cyclosporin is metabolized by cytochrome P450 CYP3A4, we examined whether interaction between Orlistat and Cyclosporin involves induction of CYP3A4. Cyclosporine 6-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 21902502-1 2011 AIMS: CYP3A4 is involved in the oxidative metabolism of many drugs and xenobiotics including the immunosuppressants tacrolimus (Tac) and cyclosporine (CsA). Cyclosporine 137-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 21902502-1 2011 AIMS: CYP3A4 is involved in the oxidative metabolism of many drugs and xenobiotics including the immunosuppressants tacrolimus (Tac) and cyclosporine (CsA). Cyclosporine 151-154 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 21902502-8 2011 CONCLUSION: The CYP3A4 intron 6 C>T polymorphism is associated with altered Tac and CsA metabolism. Cyclosporine 87-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-22 21857093-1 2011 The aim of this study was to retrospectively evaluate the effect of polymorphisms in the CYP3A4, CYP3A5 and ABCB1 genes on the dose-adjusted concentration and dose requirement of cyclosporine A(CsA) in Chinese recipients during the early period after bone marrow or hematopoietic stem cell transplantation. Cyclosporine 179-193 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 21857093-1 2011 The aim of this study was to retrospectively evaluate the effect of polymorphisms in the CYP3A4, CYP3A5 and ABCB1 genes on the dose-adjusted concentration and dose requirement of cyclosporine A(CsA) in Chinese recipients during the early period after bone marrow or hematopoietic stem cell transplantation. Cyclosporine 194-197 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 21753749-0 2011 In vivo CYP3A activity is significantly lower in cyclosporine-treated as compared with tacrolimus-treated renal allograft recipients. Cyclosporine 49-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 8-13 21753749-1 2011 In vitro studies have identified cyclosporine and tacrolimus as CYP3A inhibitors. Cyclosporine 33-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 21753749-5 2011 This implies that in vivo hepatic and first-pass CYP3A activities are significantly lower in patients receiving cyclosporine than in those receiving tacrolimus, indicating that, at the doses generally used in clinical practice, cyclosporine is the stronger of the two with respect to CYP3A inhibition. Cyclosporine 112-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-54 21753749-5 2011 This implies that in vivo hepatic and first-pass CYP3A activities are significantly lower in patients receiving cyclosporine than in those receiving tacrolimus, indicating that, at the doses generally used in clinical practice, cyclosporine is the stronger of the two with respect to CYP3A inhibition. Cyclosporine 112-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 284-289 21753749-5 2011 This implies that in vivo hepatic and first-pass CYP3A activities are significantly lower in patients receiving cyclosporine than in those receiving tacrolimus, indicating that, at the doses generally used in clinical practice, cyclosporine is the stronger of the two with respect to CYP3A inhibition. Cyclosporine 228-240 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-54 21753749-5 2011 This implies that in vivo hepatic and first-pass CYP3A activities are significantly lower in patients receiving cyclosporine than in those receiving tacrolimus, indicating that, at the doses generally used in clinical practice, cyclosporine is the stronger of the two with respect to CYP3A inhibition. Cyclosporine 228-240 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 284-289 21480191-2 2011 Seven separate drug-drug interaction (DDI) studies were performed to elucidate the in vivo effects of concomitant treatment with colchicine and known inhibitors of cytochrome P450 3A4 (CYP3A4)/P-glycoprotein (cyclosporine, ketoconazole, ritonavir, clarithromycin, azithromycin, verapamil ER [extended release]), and diltiazem ER) on the pharmacokinetics of colchicine. Cyclosporine 209-221 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 185-191 21466223-0 2011 Quercetin and rutin reduced the bioavailability of cyclosporine from Neoral, an immunosuppressant, through activating P-glycoprotein and CYP 3A4. Cyclosporine 51-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 137-144 21466223-2 2011 Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 119-139 21466223-2 2011 Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-147 21466223-2 2011 Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). Cyclosporine 14-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 119-139 21466223-2 2011 Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). Cyclosporine 14-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-147 21349923-5 2011 Three immunosuppressants (tacrolimus, sirolimus, and cyclosporine) were analyzed, because these CYP3A4 drug substrates are subject to long-term use and repeated concentration determinations. Cyclosporine 53-65 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102 19823813-2 2010 It has been reported that, in humans, CyA is metabolized by cytochrome P450 (CYP) 3A or excreted by P-glycoprotein/multidrug resistant protein (MRP) 2. Cyclosporine 38-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-84 20416375-8 2010 Using a PXR reporter gene assay, cyclosporin A - but not FK506 - was shown to be a direct PXR activator, and also to induce expression of the classic PXR-regulated CYP3A4 gene in human hepatocytes and in a cell line null for the FXR, a nuclear receptor with similar properties to the PXR. Cyclosporine 33-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 164-170 20170205-9 2010 CYP3A4 may play a more dominant role than CYP3A5 in the metabolism of ciclosporin. Cyclosporine 70-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 19729463-3 2009 Pharmacokinetic studies have demonstrated that cyclosporine increases statin drug levels, presumably via competitive inhibition of cytochrome P450 3A4. Cyclosporine 47-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-150 18192894-1 2008 OBJECTIVE: To evaluate whether variations in the ABCB1, ABCC2, SLCO1B1, CYP3A4, CYP3A5, or NR1I2 genes are associated with the pharmacokinetics of cyclosporine in pediatric renal transplant candidates, and whether the effects of these variants are related to age. Cyclosporine 147-159 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 19667964-8 2009 Cyclosporine A and Tac are metabolized by CYP3A4 and CYP3A5, and several single nucleotide polymorphisms in the two genes have been associated with differences in drug clearance. Cyclosporine 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-48 19343062-1 2009 AIM: To evaluate the potential drug-drug interactions between bifendate and cyclosporine, a substrate of CYP3A4, in relation to different CYP3A4*18B genotype groups. Cyclosporine 76-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-111 19343062-1 2009 AIM: To evaluate the potential drug-drug interactions between bifendate and cyclosporine, a substrate of CYP3A4, in relation to different CYP3A4*18B genotype groups. Cyclosporine 76-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 19343062-7 2009 The oral clearance of cyclosporine was altered in all the subjects, with substantial increases by 10.2%+/-4.4% (P=0.004) in CYP3A4*1/*1 subjects, 14.0%+/-12.0% (P=0.048) in CYP3A4*1/*18B subjects, and 32.4%+/-21.7% (P=0.013) in CYP3A4*18B/*18B subjects. Cyclosporine 22-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-130 19343062-7 2009 The oral clearance of cyclosporine was altered in all the subjects, with substantial increases by 10.2%+/-4.4% (P=0.004) in CYP3A4*1/*1 subjects, 14.0%+/-12.0% (P=0.048) in CYP3A4*1/*18B subjects, and 32.4%+/-21.7% (P=0.013) in CYP3A4*18B/*18B subjects. Cyclosporine 22-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 173-179 19343062-7 2009 The oral clearance of cyclosporine was altered in all the subjects, with substantial increases by 10.2%+/-4.4% (P=0.004) in CYP3A4*1/*1 subjects, 14.0%+/-12.0% (P=0.048) in CYP3A4*1/*18B subjects, and 32.4%+/-21.7% (P=0.013) in CYP3A4*18B/*18B subjects. Cyclosporine 22-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 173-179 19343062-8 2009 CONCLUSION: These results suggest that bifendate decreases the plasma concentration of cyclosporine in a CYP3A4 genotype-dependent manner. Cyclosporine 87-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-111 19183931-7 2009 CYP3A4 inducers can lower levels of cyclosporine or tacrolimus so much that transplant rejection occurs, and CYP3A4 inhibitors can increase their levels, leading to nephrotoxicity. Cyclosporine 36-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 18978522-1 2008 Cyclosporine is a substrate of cytochrome P450 (CYP) 3A and of the transporter ABCB1, for which polymorphisms have been described. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-55 18978522-6 2008 CYP3A4 rs4646437C>T influenced cyclosporine kinetics, the T carriers requiring higher cyclosporine dose. Cyclosporine 34-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 18978522-6 2008 CYP3A4 rs4646437C>T influenced cyclosporine kinetics, the T carriers requiring higher cyclosporine dose. Cyclosporine 89-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 18978522-8 2008 In conclusion, CYP3A4, CYP3A5, and CYP3A7 polymorphisms affect cyclosporine metabolism, and therefore, their genotyping could be useful, in association with therapeutic drug monitoring, to prospectively optimize cyclosporine prescription in transplant recipients. Cyclosporine 63-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-21 18978522-8 2008 In conclusion, CYP3A4, CYP3A5, and CYP3A7 polymorphisms affect cyclosporine metabolism, and therefore, their genotyping could be useful, in association with therapeutic drug monitoring, to prospectively optimize cyclosporine prescription in transplant recipients. Cyclosporine 212-224 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-21 18978522-9 2008 The administration of a CYP3A genotype-dependent cyclosporine starting dose should therefore be tested prospectively in a randomized controlled clinical trial to assess whether it leads to an improvement of the patients outcome after transplantation, with adequate immunosuppression and decreased toxicity. Cyclosporine 49-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-29 18636247-1 2008 OBJECTIVE: The objective of this study was to retrospectively evaluate the effects of MDR1, CYP3A4*18B, and CYP3A5*3 genetic polymorphisms on cyclosporine A (CsA) pharmacokinetics in Chinese renal transplant patients during the first month after transplantation. Cyclosporine 142-156 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 18636247-10 2008 Patients with CYP3A4*18B alleles may require higher doses of CsA to reach the target levels. Cyclosporine 61-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 18518855-7 2008 In adults, genetic polymorphisms in the genes encoding the cyclosporine-metabolizing enzymes CYP3A4 and CYP3A5, as well as the ABCB1 gene, which encodes the efflux-pump P-glycoprotein, seem to have a limited effect, if any, on cyclosporine pharmacokinetics. Cyclosporine 59-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 20038391-1 2009 OBJECTIVE: To determine how single nucleotide polymorphisms located on genes MDR1, CYP3A4 and CYP3A5 affect the absorption kinetics of cyclosporine in cardiac transplant patients. Cyclosporine 135-147 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 19728747-9 2009 Ciclosporin and tacrolimus have distinct pharmacokinetics, but both are metabolized by intestinal and hepatic CYP3A4/3A5 and transported across the cell membrane by P-glycoprotein. Cyclosporine 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 19005401-1 2008 BACKGROUND: Bioavailability of tacrolimus (Tac) and cyclosporine is determined by cytochrome P450IIIA and by P-glycoprotein encoded by the CYP3A4/CYP3A5 and ABCB1 genes. Cyclosporine 52-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 18608282-10 2008 Cyclosporine co-administration increases colchicine toxicity by a dual mechanism: cyclosporine inhibits P-glycoprotein resulting in increased intracellular colchicine concentrations and decreased hepatic and renal excretion of the drug and cyclosporine interacts with CYP3A4 to decreases the hepatic elimination of colchicine. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 268-274 18608282-10 2008 Cyclosporine co-administration increases colchicine toxicity by a dual mechanism: cyclosporine inhibits P-glycoprotein resulting in increased intracellular colchicine concentrations and decreased hepatic and renal excretion of the drug and cyclosporine interacts with CYP3A4 to decreases the hepatic elimination of colchicine. Cyclosporine 82-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 268-274 18076219-19 2008 Dosage adjustments may be required for drugs that are substrates of CYP3A4 (e.g. ciclosporin, triazolam) and CYP2C19 enzymes (e.g. diazepam, phenytoin) when administered with armodafinil. Cyclosporine 81-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-74 18223473-5 2008 A pharmacokinetic interaction between cyclosporine and everolimus has been described previously for healthy volunteers after single-dose application and presumably originates from a comparatively greater inhibition of hepatic CYP3A4 or P-glycoprotein efflux transporter with a low-dose cyclosporine regimen. Cyclosporine 38-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 226-232 17545536-1 2007 PURPOSE: Increased clearance of drugs, such as oral cyclosporine, that are CYP3A and/or ABCB1 (P-gp/MDR1) substrates was reported in African-American compared with Caucasian patients. Cyclosporine 52-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-80 18665658-8 2008 Several available statin medications are metabolized by cytochrome P450 (CYP) 3A4 and can therefore interact with commonly used medications such as amiodarone, macrolide antibacterials, calcium channel antagonists, fibric acid derivatives and ciclosporin. Cyclosporine 243-254 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-81 18721002-3 2008 Cinacalcet, as well as some immunosuppressants such as ciclosporin, tacrolimus and sirolimus, is partially metabolized by the cytochrome P450 3A enzymes (CYP3A). Cyclosporine 55-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 154-159 18240909-5 2007 The association between the CYP3A4 and CYP3A5 polymorphisms and cyclosporine pharmacokinetics is more questionable. Cyclosporine 64-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-34 17425754-2 2007 Ciclosporin is a substrate for P-gp and is metabolized by cytochrome P450 (CYP) 3A enzymes. Cyclosporine 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-82 17374625-8 2007 DATA SYNTHESIS: Elevated plasma concentrations and toxicities have been reported for a number of CYP3A substrates including amiodarone, carbamazepine, quinidine, tacrolimus, and cyclosporine when administered with metronidazole. Cyclosporine 178-190 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-102 17624028-0 2007 Association of CYP3A4*18B polymorphisms with the pharmacokinetics of cyclosporine in healthy subjects. Cyclosporine 69-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-21 17151193-10 2007 However, strong CYP 3A4 inhibition by cyclosporine could unveil the influence of this polymorphism. Cyclosporine 38-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-23 17624028-1 2007 The aim of this study is to evaluate the association of the CYP3A4*18B genotype with the cyclosporine metabolism in healthy subjects. Cyclosporine 89-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 17202802-3 2007 On the other hand, cyclosporine and tacrolimus competitively inhibited CYP3A4-mediated nifedipine oxidation activity, with inhibition constants (K(i)) of 1.42 and 0.36 muM, respectively. Cyclosporine 19-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 17624028-9 2007 The data suggest that the CYP3A4*18B genotype affects cyclosporine pharmacokinetics probably resulting from a higher enzymatic activity of this mutation in healthy subjects. Cyclosporine 54-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 17244767-9 2007 These results rationalize the use of a single high-dose cyclosporine as a probe inhibitor of P-glycoprotein for compound candidates whose elimination is less dependent on CYP3A4-mediated metabolism. Cyclosporine 56-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 171-177 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 19-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 16634729-2 2006 Possible causes, such as the inhibition of CYP3A4 induced by cyclosporine causing elevations of serum fentanyl, are discussed. Cyclosporine 61-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 16759707-5 2006 Both tacrolimus and cyclosporine are substrates of Pgp, CYP3A4 and CYP3A5, and therefore, these molecules are potential pharmacokinetic factors with which to establish personalized dosage regimens for these drugs. Cyclosporine 20-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 16911928-6 2006 RESULTS: The SNPs of CYP3A and P-gp are closely correlated to the large variations of cyclosporine and tacrolimus dosage between different patients, although conflicting results were obtained by some authors. Cyclosporine 86-98 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-26 16612333-0 2006 The influence of CYP3A gene polymorphisms on cyclosporine dose requirement in renal allograft recipients. Cyclosporine 45-57 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 17-22 16612333-1 2006 Cyclosporine is a substrate of cytochrome P-450 3A (CYP3A) subfamily of enzymes and characterized by a narrow therapeutic range with wide interindividual variation in pharmacokinetics. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-50 16612333-1 2006 Cyclosporine is a substrate of cytochrome P-450 3A (CYP3A) subfamily of enzymes and characterized by a narrow therapeutic range with wide interindividual variation in pharmacokinetics. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-57 16611021-0 2006 Evaluation of microsomal incubation conditions on CYP3A4-mediated metabolism of cyclosporine A by a statistical experimental design. Cyclosporine 80-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 16611021-7 2006 The present study showed that relatively small changes in the incubation matrix had a significant influence on the microsomal CYP3A4-mediated metabolism of CsA. Cyclosporine 156-159 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 126-132 17042920-0 2006 Effects of genetic polymorphisms of CYP3A4, CYP3A5 and MDR1 on cyclosporine pharmacokinetics after renal transplantation. Cyclosporine 63-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-42 17042920-7 2006 The aim of the present study was to evaluate retrospectively the effects of genetic polymorphisms of CYP3A4, CYP3A5 and MDR1 on cyclosporine dose adjusted trough blood concentration during the early period after renal transplantation in Chinese patients. Cyclosporine 128-140 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-107 16298597-3 2005 Some evidence points to a higher activity of some specific enzymes in women, such as CYP3A, that may influence differences in cyclosporine pharmacokinetics. Cyclosporine 126-138 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-90 16198658-15 2005 CONCLUSIONS: Cyclosporine raised the plasma concentrations of repaglinide, probably by inhibiting its CYP3A4-catalyzed biotransformation and OATP1B1-mediated hepatic uptake. Cyclosporine 13-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 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). Cyclosporine 272-284 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 134-140 16027407-1 2005 Cyclosporine is a marketed immunosuppressive agent and a known substrate for CYP3A. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-82 16095503-8 2005 Concomitantly, a profound decrease of hepatic and intestinal PGP and an increase of intestinal CYP3A4 were noted with CsA, whereas no effect was seen after atorvastatin therapy with or without Tac. Cyclosporine 118-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 15845749-0 2005 Midazolam and cyclosporin a metabolism in transgenic mice with liver-specific expression of human CYP3A4. Cyclosporine 14-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 15845749-8 2005 Similarly, following intravenous administration of cyclosporin A (20 mg/kg), CYP3A4 transgenic mice displayed a reduced plasma AUC compared with wild-type (24.3 +/- 0.66 versus 35.8 +/- 0.53 microg . Cyclosporine 51-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-83 15845749-10 2005 Thus, midazolam and cyclosporin A, compounds with markedly different clearance rates and half-lives, both demonstrated clearly accelerated kinetics in the CYP3A4 transgenic mice. Cyclosporine 20-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 155-161 15592326-10 2004 CONCLUSION: Patients carrying a CYP3A4*1B variant allele have a significantly higher oral cyclosporine clearance compared with patients homozygous for CYP3A4*1 . Cyclosporine 90-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 15723604-5 2005 The association between the CYP3A4 and CYP3A5 polymorphisms and cyclosporine pharmacokinetics is more questionable. Cyclosporine 64-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-34 16541750-3 2005 Since cyclosporine is a substrate and inhibitor of CYP3A4, researchers suspect that the immunosuppressant inhibits CYP3A4-mediated metabolism of statins, leading to an increase in statin plasma concentration and infrequently resulting in rhabdomyolysis. Cyclosporine 6-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-57 16541750-3 2005 Since cyclosporine is a substrate and inhibitor of CYP3A4, researchers suspect that the immunosuppressant inhibits CYP3A4-mediated metabolism of statins, leading to an increase in statin plasma concentration and infrequently resulting in rhabdomyolysis. Cyclosporine 6-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 16541750-8 2005 Furthermore, in the Japanese package inserts, it is either stated that cyclosporine inhibits CYP3A4-mediated metabolism or no comment is made on the mechanism. Cyclosporine 71-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 15592326-1 2004 OBJECTIVE: Our objective was to determine the relationship between single nucleotide polymorphisms (SNPs) in the multidrug resistance 1 (MDR-1) gene and the cytochrome P450 (CYP) genes CYP3A4 and CYP3A5 and the pharmacokinetics of cyclosporine (INN, ciclosporin). Cyclosporine 231-243 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 185-191 15592326-1 2004 OBJECTIVE: Our objective was to determine the relationship between single nucleotide polymorphisms (SNPs) in the multidrug resistance 1 (MDR-1) gene and the cytochrome P450 (CYP) genes CYP3A4 and CYP3A5 and the pharmacokinetics of cyclosporine (INN, ciclosporin). Cyclosporine 250-261 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 185-191 15450954-1 2004 The objectives of this study were to characterize and compare the metabolic profile of cyclosporine A (CsA) catalyzed by CYP3A4, CYP3A5 and human kidney and liver microsomes, and to evaluate the impact of the CYP3A5 polymorphism on product formation from parent drug and its primary metabolites. Cyclosporine 103-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 15450954-2 2004 Three primary CsA metabolites (AM1, AM9 and AM4N) were produced by heterologously expressed CYP3A4. Cyclosporine 14-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 15450954-9 2004 AM19 and AM1c9, two of the major secondary metabolites of CsA, were produced by CsA, AM1 and AM1c when incubated with CYP3A4, CYP3A5, kidney microsomes from CYP3A5*1/*3 donors and all liver microsomes. Cyclosporine 58-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 15450954-9 2004 AM19 and AM1c9, two of the major secondary metabolites of CsA, were produced by CsA, AM1 and AM1c when incubated with CYP3A4, CYP3A5, kidney microsomes from CYP3A5*1/*3 donors and all liver microsomes. Cyclosporine 80-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 15369802-2 2004 We found a significant inhibition of human CYP3A4-dependent transformation of cyclosporine by resveratrol, with IC50 = 4.5 microM. Cyclosporine 78-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 15197524-1 2004 OBJECTIVE: The aim of this study was to (a) quantify the gene expression of some cytochromes P(450) (CYP), especially CYP3A4, in serial biopsies from liver grafts the first year after orthoptic liver transplantation (OLT) and (b) study the relationship between hepatic CYP3A4 gene expression and plasma levels of cyclosporine and tacrolimus. Cyclosporine 313-325 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 15454731-1 2004 OBJECTIVE: Cyclosporine is extensively metabolized by cytochrome-P450 3A (CYP3A) enzymes in the liver and intestine including the CYP3A5 isoenzyme. Cyclosporine 11-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-72 15454731-1 2004 OBJECTIVE: Cyclosporine is extensively metabolized by cytochrome-P450 3A (CYP3A) enzymes in the liver and intestine including the CYP3A5 isoenzyme. Cyclosporine 11-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 74-79 15307840-0 2004 CYP3A4 and P-glycoprotein activity in healthy controls and transplant patients on cyclosporin vs. tacrolimus vs. sirolimus. Cyclosporine 82-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 15197524-7 2004 The gene expression of CYP3A4 was related to the plasma concentration of cyclosporine and tacrolimus, i.e. low mRNA concentrations corresponded to high serum concentration levels and vice versa. Cyclosporine 73-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 23-29 15197524-11 2004 Low CYP3A4 gene expression was related to high plasma levels of cyclosporine and tacrolimus and vice versa. Cyclosporine 64-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-10 15350151-5 2004 Drugs most prominently affected and contraindicated for concomitant use with St John"s wort are metabolised via both CYP3A4 and P-glycoprotein pathways, including HIV protease inhibitors, HIV non-nucleoside reverse transcriptase inhibitors (only CYP3A4), the immunosuppressants ciclosporin and tacrolimus, and the antineoplastic agents irinotecan and imatinib mesylate. Cyclosporine 278-289 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-123 14617681-10 2004 It is, however, clear that inhibition of CYP3A4-mediated metabolism by cyclosporin A alone is insufficient to explain the increased bosentan concentrations and that inhibition of hepatocellular uptake offers an attractive mechanistic alternative also in human. Cyclosporine 71-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 15307840-1 2004 This study aimed to determine the impact of maintenance immunosuppressive therapy with cyclosporin A (CsA), tacrolimus (FK506) and sirolimus (Rapa) on the in vivo activity of both intestinal and hepatic cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (PGP) in renal transplant patients. Cyclosporine 87-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 203-222 15307840-1 2004 This study aimed to determine the impact of maintenance immunosuppressive therapy with cyclosporin A (CsA), tacrolimus (FK506) and sirolimus (Rapa) on the in vivo activity of both intestinal and hepatic cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (PGP) in renal transplant patients. Cyclosporine 102-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 203-222 15307840-1 2004 This study aimed to determine the impact of maintenance immunosuppressive therapy with cyclosporin A (CsA), tacrolimus (FK506) and sirolimus (Rapa) on the in vivo activity of both intestinal and hepatic cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (PGP) in renal transplant patients. Cyclosporine 102-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 224-230 15307840-5 2004 A significant increase in intestinal CYP3A4 activity and a significant decrease in hepatic and intestinal PGP activity was seen in patients on CsA in comparison with those on FK506 or Rapa (p < 0.01). Cyclosporine 143-146 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 15116055-1 2004 BACKGROUND: The immunosuppressive drug cyclosporine (INN, ciclosporin), whose pharmacokinetic characteristics vary greatly among individuals, is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Cyclosporine 39-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-185 15116055-1 2004 BACKGROUND: The immunosuppressive drug cyclosporine (INN, ciclosporin), whose pharmacokinetic characteristics vary greatly among individuals, is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Cyclosporine 58-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-185 12562644-1 2003 BACKGROUND: Pharmacokinetic study has shown that co-administration of cyclosporin A (CsA), which acts as a P-glycoprotein (P-gp) and CYP-3A blocker, resulted in an 8-fold increase in the systemic exposure of oral paclitaxel. Cyclosporine 70-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 133-139 12966368-0 2003 Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR-1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus. Cyclosporine 112-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 12966368-3 2003 OBJECTIVE: Our objective was to determine the role of genetic polymorphisms in CYP3A4, CYP3A5, and MDR-1 with respect to interindividual variability in cyclosporine and tacrolimus pharmacokinetics. Cyclosporine 152-164 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 79-85 12817518-1 2003 Variability in CYP3A (CYP3A4/5) and P-glycoprotein (human MDR1 gene product) activity underlies interindividual differences in oral cyclosporine (CsA) bioavailability. Cyclosporine 132-144 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-20 12817518-1 2003 Variability in CYP3A (CYP3A4/5) and P-glycoprotein (human MDR1 gene product) activity underlies interindividual differences in oral cyclosporine (CsA) bioavailability. Cyclosporine 132-144 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-30 12817518-1 2003 Variability in CYP3A (CYP3A4/5) and P-glycoprotein (human MDR1 gene product) activity underlies interindividual differences in oral cyclosporine (CsA) bioavailability. Cyclosporine 146-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-20 12817518-1 2003 Variability in CYP3A (CYP3A4/5) and P-glycoprotein (human MDR1 gene product) activity underlies interindividual differences in oral cyclosporine (CsA) bioavailability. Cyclosporine 146-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-30 12766558-0 2003 Association of the CYP3A4*1B 5"-flanking region polymorphism with cyclosporine pharmacokinetics in healthy subjects. Cyclosporine 66-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-25 12562644-1 2003 BACKGROUND: Pharmacokinetic study has shown that co-administration of cyclosporin A (CsA), which acts as a P-glycoprotein (P-gp) and CYP-3A blocker, resulted in an 8-fold increase in the systemic exposure of oral paclitaxel. Cyclosporine 85-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 133-139 12673034-3 2003 In this study, we demonstrated the inductive effects of phenobarbital, rifampicin, carbamazepine, phenytoin, prednisolone, ciclosporin and clotrimazole on CYP3A4, CYP3A5 and CYP3A7 mRNA expression, and established the relationship between the expression of human glucocorticoid receptor alpha (hGR) mRNA and the induction of CYP3A4 mRNA in cultured HepG2 cells by reverse transcription polymerase chain reaction (RT-PCR). Cyclosporine 123-134 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 155-161 12673034-3 2003 In this study, we demonstrated the inductive effects of phenobarbital, rifampicin, carbamazepine, phenytoin, prednisolone, ciclosporin and clotrimazole on CYP3A4, CYP3A5 and CYP3A7 mRNA expression, and established the relationship between the expression of human glucocorticoid receptor alpha (hGR) mRNA and the induction of CYP3A4 mRNA in cultured HepG2 cells by reverse transcription polymerase chain reaction (RT-PCR). Cyclosporine 123-134 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 325-331 12673034-6 2003 The induction of CYP3A4 mRNA expression by clotrimazole and ciclosporin was negligible. Cyclosporine 60-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 17-23 12673034-12 2003 Furthermore, we studied the associations between the expression of hGRalpha mRNA and the induced level of CYP3A4 mRNA by prednisolone and ciclosporin. Cyclosporine 138-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-112 12673034-13 2003 Treatment with both prednisolone and ciclosporin showed synergistic effects on induction of CYP3A4 mRNA and, following treatment with both drugs, the expression level of CYP3A4 mRNA was 2-fold greater compared with prednisolone alone after the fifth day. Cyclosporine 37-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 12673034-13 2003 Treatment with both prednisolone and ciclosporin showed synergistic effects on induction of CYP3A4 mRNA and, following treatment with both drugs, the expression level of CYP3A4 mRNA was 2-fold greater compared with prednisolone alone after the fifth day. Cyclosporine 37-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 170-176 12558459-7 2003 Cyclosporin-treated patients on the other hand show several-fold higher systemic exposure of all statins, both those that are metabolised by CYP3A4 and fluvastatin (metabolised by CYP2C9). Cyclosporine 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-147 12563178-1 2003 Intestinal cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp) both play a vital role in the metabolism of oral cyclosporine (CsA). Cyclosporine 115-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 12563178-1 2003 Intestinal cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp) both play a vital role in the metabolism of oral cyclosporine (CsA). Cyclosporine 129-132 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 12523495-2 2002 The CYPs activities were assessed by measuring the rate of acetanilide 4-hydroxylation (CYP1A2) and cyclosporine A oxidation (CYP3A4) after treatment with TCDD (a CYP1A subfamily inducer) or rifampicin (mainly a CYP3A4 inducer). Cyclosporine 100-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 126-132 12698985-3 2002 MATERIALS AND METHODS: We chose 3 model drugs that are metabolized by distinct cytochrome P450 (CYP) isoforms (theophylline, phenytoin and cyclosporine for CYPIA2, CYP2C9/2C19 and CYP3A4, respectively). Cyclosporine 139-151 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 180-186 11849198-5 2002 As indinavir and cyclosporin are substrates for both CYP3A4 and the multi drug transporter P-glycoprotein we hypothesized that modulation of P-glycoprotein expression and function by SJW may contribute to the development of potentially harmful drug-drug interactions. Cyclosporine 17-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 12160480-8 2002 The combined up-regulation in intestinal P-glycoprotein and hepatic and intestinal CYP3A4 impairs the absorption and stimulates the metabolism of cyclosporine, leading to subtherapeutic plasma levels. Cyclosporine 146-158 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 11978159-5 2002 Since the interaction between cyclosporine and HMG-CoA reductase inhibitors involves the CYP3A4 enzyme system, the possibility of amplifying this interaction exists when other drugs affecting the same enzyme system are coprescribed. Cyclosporine 30-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 11888457-8 2002 The mechanism of interaction between St John"s wort and cyclosporine has been recently elucidated and involves both P-glycoprotein and cytochrome P 450 3A4 expression. Cyclosporine 56-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 135-155 11914905-7 2002 The inhibitory concentrations of paclitaxel, tamoxifen and cyclosporine on MMDx metabolism were in the range of those observed in patients upon administration of these drugs, which are known to be CYP3A4 substrates. Cyclosporine 59-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 197-203 12036392-14 2002 Thus, rhabdomyolysis has occurred following the coadministration of cyclosporin, a potent CYP3A4 and P-glycoprotein inhibitor, and lovastatin. Cyclosporine 68-79 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 12497749-1 2002 AIM: Hepatic metabolism of sildenafil uses the same metabolic pathway as the calcineurin inhibitors (cyclosporine/tacrolimus), through the CYP3A4 isoenzyme. Cyclosporine 101-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 11408558-9 2001 Inhibition of Pgp in CYP3A4-expressing Caco-2 cells by UIC2 and 1 microM CsA resulted in a significant decrease in the apical secretion of M6, M5, and OH-indinavir and an increase in the amount of the metabolites secreted in the basolateral compartment and retained in the cytosol. Cyclosporine 73-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 11719731-1 2001 BACKGROUND: Interindividual variation in the pharmacokinetics of the immunosuppressive agents cyclosporine (INN, ciclosporin) and tacrolimus may result from differences in the activity of cytochrome P4503A (CYP3A). Cyclosporine 94-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 188-194 11719731-1 2001 BACKGROUND: Interindividual variation in the pharmacokinetics of the immunosuppressive agents cyclosporine (INN, ciclosporin) and tacrolimus may result from differences in the activity of cytochrome P4503A (CYP3A). Cyclosporine 94-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 207-212 11719731-1 2001 BACKGROUND: Interindividual variation in the pharmacokinetics of the immunosuppressive agents cyclosporine (INN, ciclosporin) and tacrolimus may result from differences in the activity of cytochrome P4503A (CYP3A). Cyclosporine 113-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 188-194 11719731-1 2001 BACKGROUND: Interindividual variation in the pharmacokinetics of the immunosuppressive agents cyclosporine (INN, ciclosporin) and tacrolimus may result from differences in the activity of cytochrome P4503A (CYP3A). Cyclosporine 113-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 207-212 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. Cyclosporine 63-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 11549208-7 2001 In addition, the higher levels of CsA with docetaxel than with paclitaxel co-administration may be explained by the fact that docetaxel is almost exclusively metabolised by CYP 3A4, whereas paclitaxel is predominantly metabolised by CYP 2C8 and to a lesser extent by CYP 3A4. Cyclosporine 34-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 173-180 11549208-7 2001 In addition, the higher levels of CsA with docetaxel than with paclitaxel co-administration may be explained by the fact that docetaxel is almost exclusively metabolised by CYP 3A4, whereas paclitaxel is predominantly metabolised by CYP 2C8 and to a lesser extent by CYP 3A4. Cyclosporine 34-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 267-274 11180020-2 2000 Previous reports have described reductions in concentrations of CYP3A4 substrates indinavir and cyclosporine (INN, ciclosporin) associated with St John"s Wort. Cyclosporine 115-126 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-70 11375290-1 2001 BACKGROUND: A substantial proportion of the variability in the absorption and clearance of cyclosporin A (CsA) after oral administration has been attributed to variability in liver cytochrome P-450 3A4 (CYP3A4) activity and intestinal P-glycoprotein (P-gp) concentration. Cyclosporine 106-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 181-201 11375290-1 2001 BACKGROUND: A substantial proportion of the variability in the absorption and clearance of cyclosporin A (CsA) after oral administration has been attributed to variability in liver cytochrome P-450 3A4 (CYP3A4) activity and intestinal P-glycoprotein (P-gp) concentration. Cyclosporine 106-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 203-209 11871046-6 2001 St John"s wort may induce cytochrome P-450 3A4 activity and/or P-glycoprotein expression, which are both involved in the metabolism and absorption of cyclosporine. Cyclosporine 150-162 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-46 11181682-3 2001 The purpose of this study was to enhance the systemic exposure to oral docetaxel on coadministration of cyclosporine (CsA), an efficacious inhibitor of P-gp and substrate for CYP 3A4. Cyclosporine 104-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 175-182 11181682-3 2001 The purpose of this study was to enhance the systemic exposure to oral docetaxel on coadministration of cyclosporine (CsA), an efficacious inhibitor of P-gp and substrate for CYP 3A4. Cyclosporine 118-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 175-182 11239516-1 2001 OBJECTIVES: Little is known about the effect of ischemia/reperfusion with xenogenic blood on function and gene expression of CYP3A4, the enzyme largely responsible for the metabolism of the immunosuppressants Cyclosporin A (CsA) and Tacrolimus. Cyclosporine 209-222 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 11239516-1 2001 OBJECTIVES: Little is known about the effect of ischemia/reperfusion with xenogenic blood on function and gene expression of CYP3A4, the enzyme largely responsible for the metabolism of the immunosuppressants Cyclosporin A (CsA) and Tacrolimus. Cyclosporine 224-227 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 11121733-2 2000 Because cytochrome P450 (CYP) 3A-mediated first-pass metabolism contributes to this unpredictable bioavailability, an in vivo oral CYP3A phenotyping probe could be a valuable tool in optimizing cyclosporine therapy. Cyclosporine 194-206 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-136 11498403-6 2000 A wealth of recent experimental data shows that many of the previously tested P-glycoprotein inhibitors, including verapamil, cyclosporin A, and valspodar (SDZ PSC 833), are substrates and/or potent inhibitors of cytochrome P450 3A4 (CYP3A4). Cyclosporine 126-139 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 213-232 11498403-6 2000 A wealth of recent experimental data shows that many of the previously tested P-glycoprotein inhibitors, including verapamil, cyclosporin A, and valspodar (SDZ PSC 833), are substrates and/or potent inhibitors of cytochrome P450 3A4 (CYP3A4). Cyclosporine 126-139 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 234-240 11067738-5 2000 The inhibitory effects of ketoconazole, cyclosporin A, and cimetidine toward the 2-hydroxylation of E2 catalyzed by CYP3A4 were obtained, and their IC(50) values were 7 nM, 64 nM, and 290 microM, respectively. Cyclosporine 40-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 116-122 11038163-11 2000 All three K11777 metabolites were formed by isolated CYP3A and their formation by human liver microsomes was inhibited by the CYP3A inhibitor cyclosporine (50 microM, 54-62% inhibition) and antibodies against human CYP3A4/5 (100 microg of antibodies/100 microg microsomal protein, 55-68% inhibition). Cyclosporine 142-154 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-58 11038163-11 2000 All three K11777 metabolites were formed by isolated CYP3A and their formation by human liver microsomes was inhibited by the CYP3A inhibitor cyclosporine (50 microM, 54-62% inhibition) and antibodies against human CYP3A4/5 (100 microg of antibodies/100 microg microsomal protein, 55-68% inhibition). Cyclosporine 142-154 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 126-131 11038163-11 2000 All three K11777 metabolites were formed by isolated CYP3A and their formation by human liver microsomes was inhibited by the CYP3A inhibitor cyclosporine (50 microM, 54-62% inhibition) and antibodies against human CYP3A4/5 (100 microg of antibodies/100 microg microsomal protein, 55-68% inhibition). Cyclosporine 142-154 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 215-223 11151744-1 2000 OBJECTIVE: Case reports have described elevated concentrations of CYP3A4 substrates (e.g. cyclosporin) during metronidazole treatment. Cyclosporine 90-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 10741627-0 2000 Prediction of cyclosporine clearance in liver transplant recipients by the use of midazolam as a cytochrome P450 3A probe. Cyclosporine 14-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-115 10981246-7 2000 Cyclosporine exhibits a relatively small therapeutic window and is sensitive to medications that can modulate the CYP3A4 isoenzyme and P-gp in both the liver and small intestines. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-120 11009048-8 2000 The median cyclosporin pseudo-clearance of transplant patients with wild-type CYP3A4 was 0.90 l/h/kg (range: 0.35-3.8 l/h/kg; n = 86), whereas the corresponding value for the five patients heterozygotic for the CYP3A4-G variant was 0.71 l/h/kg (range 0.35-0.91 l/h/kg). Cyclosporine 11-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 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. Cyclosporine 192-205 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 10786743-4 2000 CYP3A4 is responsible for the metabolism of numerous other therapeutic agents, including those administered concurrently with fentanyl (e.g., nifedipine, lidocaine, erythromycin and cyclosporine). Cyclosporine 182-194 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 10898107-10 2000 The point estimates of rGC for composite (hepatic + intestinal) CYP3A4 activity measured after oral administration of cyclosporine, ethinylestradiol, ethylmorphine, nifedipine and nitrendipine, ranged from 0.66-0.98 (median: 0.83) (P < 0.05). Cyclosporine 118-130 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-70 10898107-11 2000 Cyclosporine data suggested a higher genetic control of CYP3A4 at night than during the day. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 10741627-1 2000 BACKGROUND: Interindividual differences in the kinetics of cyclosporine (INN, ciclosporin) result in part from variations in the activity of cytochrome P450 3A (CYP3A). Cyclosporine 59-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-159 10741627-1 2000 BACKGROUND: Interindividual differences in the kinetics of cyclosporine (INN, ciclosporin) result in part from variations in the activity of cytochrome P450 3A (CYP3A). Cyclosporine 59-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-166 10741627-1 2000 BACKGROUND: Interindividual differences in the kinetics of cyclosporine (INN, ciclosporin) result in part from variations in the activity of cytochrome P450 3A (CYP3A). Cyclosporine 78-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-159 10741627-1 2000 BACKGROUND: Interindividual differences in the kinetics of cyclosporine (INN, ciclosporin) result in part from variations in the activity of cytochrome P450 3A (CYP3A). Cyclosporine 78-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-166 10741627-3 2000 The objective of this study was to examine the usefulness of midazolam as a CYP3A probe to predict cyclosporine clearance. Cyclosporine 99-111 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-81 10741627-12 2000 CONCLUSION: Heterogeneity in CYP3A activity contributes to interpatient differences in cyclosporine dosage requirements after liver transplantation. Cyclosporine 87-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-34 10752642-3 2000 During clinical investigations of drug-drug interactions with therapeutics (terfenadine and cyclosporine) known to be metabolized by CYP3A4, pharmacokinetic interactions were noted upon troglitazone multiple-dose treatments. Cyclosporine 92-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 133-139 10385214-12 1999 Diltiazem, erythromycin, nifedipine and cyclosporin (CYP 3A substrates) inhibited halofantrine metabolism. Cyclosporine 40-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 10503812-15 1999 Polypharmacy may have specific relevance for elderly patients treated with cyclosporin since this agent is a substrate of both CYP3A and P-glycoprotein, both of which are important in the elimination of many commonly used drugs. Cyclosporine 75-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-132 10503812-3 1999 Cyclosporin is primarily eliminated via biotransformation by cytochrome P450 (CYP)3A in the gut wall and liver. Cyclosporine 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 10496299-12 1999 Troglitazone may enhance the activities of cytochrome P450 (CYP) 3A and/or transporter(s) thereby reducing the plasma concentrations of terfenadine, cyclosporin, atorvastatin and fexofenadine. Cyclosporine 149-160 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-67 10411567-3 1999 Sulfoxide formation was determined to be cytochrome P-450 (CYP) 3A4-dependent by correlation with CYP3A4-marker nifedipine oxidase activity, inhibition by cyclosporin A and troleandomycin, and inhibition of R- (70%) and S- (64%) sulfoxide formation by anti-3A antibody. Cyclosporine 155-168 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-67 10668858-13 2000 Administration of a CYP3A4 inhibitor with cyclosporin may allow reduction of the dosage and cost of the immunosuppressant. Cyclosporine 42-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 10513779-13 1999 Potent CYP3A4 inhibitors, especially cyclosporine, significantly increase the risk. Cyclosporine 37-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 7-13 10215697-1 1999 Cytochrome P-450 (CYP) 3A4 accounts for approximately 50% of all P-450s found in the small intestine (Paine et al., 1997) and contributes to the extensive and variable first-pass extraction of drugs such as cyclosporine and saquinavir. Cyclosporine 207-219 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-26 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. Cyclosporine 104-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 10092957-15 1999 Nevertheless, care should be taken with the use of known CYP3A4 inhibitors such as erythromycin, ketoconazole and cyclosporin. Cyclosporine 114-125 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 9402948-6 1997 Moreover, the oxidative metabolism of cyclosporin A, a monoxygenase activity depending on CYP3A4, has been monitored directly on the cultured cells by HPLC analysis of extracellular medium. Cyclosporine 38-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 9698296-16 1998 Conversely, PSC inhibited only reactions catalyzed by CYP3A, including cyclosporine A metabolism (IC50 = 6.5 microM) and p-hydroxyphenyl-C3"-paclitaxel formation (Ki = 1.2 microM). Cyclosporine 71-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-59 9749227-10 1998 Cyclosporine is metabolised in the liver by cytochrome P450 3A4 dependant enzymes. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-63 9469504-4 1998 Because cyclosporine is metabolized predominantly by CYP3A3/4 isoenzymes, inhibition of this system can lead to the buildup of toxic levels. Cyclosporine 8-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 9400033-2 1997 For some of these (e.g., cyclosporine, verapamil, midazolam), CYP3A in the intestinal mucosa contributes to their extensive and variable first-pass extraction. Cyclosporine 25-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-67 8855178-3 1996 It has been shown that such prehepatic metabolism contributes substantially to total clearance of CYP3A4 substrates (e.g., cyclosporine) before and even more pronounced during enzyme induction. Cyclosporine 123-135 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 10837554-13 1997 It is also clear that some of the substrates for CYP3A4 (e.g., cyclosporine, midazolam, nifedipine, verapamil and saquinavir) undergo significant metabolic extraction by the gut wall. Cyclosporine 63-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-55 10837558-2 1997 Cyclosporine and tacrolimus are metabolized primarily by cytochrome P450 3A4 (CYP3A4) in the liver and small intestine. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-76 10837558-2 1997 Cyclosporine and tacrolimus are metabolized primarily by cytochrome P450 3A4 (CYP3A4) in the liver and small intestine. Cyclosporine 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 10837558-14 1997 It seems that compounds that alter (either induce or inhibit) CYP3A4 and/or p-glycoprotein will alter the oral pharmacokinetics of cyclosporine and tacrolimus. Cyclosporine 131-143 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 9333100-1 1997 Interpatient differences in the oral clearance of cyclosporine (INN, ciclosporin) have been partially attributed to variation in the activity of a single liver enzyme termed CYP3A4. Cyclosporine 50-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 9333100-1 1997 Interpatient differences in the oral clearance of cyclosporine (INN, ciclosporin) have been partially attributed to variation in the activity of a single liver enzyme termed CYP3A4. Cyclosporine 69-80 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 9333100-2 1997 Recently it has been shown that small bowel also contains CYP3A4, as well as P-glycoprotein, a protein able to transport cyclosporine. Cyclosporine 121-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-64 9333100-8 1997 Drug interactions with cyclosporine previously ascribed to intestinal CYP3A4 may instead be mediated by interactions with intestinal P-glycoprotein. Cyclosporine 23-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 70-76 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. Cyclosporine 140-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 8885130-3 1996 This elevation in cyclosporine level is possibly due to an interaction between the two drugs resulting from an inhibition of CYP3A4-mediated metabolism of cyclosporine by glibenclamide. Cyclosporine 18-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 8885130-3 1996 This elevation in cyclosporine level is possibly due to an interaction between the two drugs resulting from an inhibition of CYP3A4-mediated metabolism of cyclosporine by glibenclamide. Cyclosporine 155-167 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 8857552-2 1996 Interpatient differences in liver CYP3A4 activity, as measured by the ERMBT, seem to account, for the most part, for interindividual differences in the kinetics of cyclosporin A and FK506. Cyclosporine 164-177 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 7473140-8 1995 Inhibitor experiments suggest that typical CYP3A substrates/inhibitors (e.g., cyclosporin, epipodophyllotoxins) may significantly interact with paclitaxel in vivo. Cyclosporine 78-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-48 8549033-1 1996 INTRODUCTION: Cytochrome P4503A (CYP3A) is primarily responsible for the metabolism of cyclosporine and that of many other drugs. Cyclosporine 87-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 8549033-1 1996 INTRODUCTION: Cytochrome P4503A (CYP3A) is primarily responsible for the metabolism of cyclosporine and that of many other drugs. Cyclosporine 87-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-38 8549033-3 1996 One such measure of CYP3A activity is the 14C erythromycin breath test, which has been applied to the prediction of cyclosporine disposition. Cyclosporine 116-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-25 8849485-6 1996 Using specific antibodies and inhibitors, we showed that, as in the liver, cytochrome P450 3A (CYP 3A) enzymes are responsible for ciclosporin metabolism in the human small intestine. Cyclosporine 131-142 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-93 8849485-6 1996 Using specific antibodies and inhibitors, we showed that, as in the liver, cytochrome P450 3A (CYP 3A) enzymes are responsible for ciclosporin metabolism in the human small intestine. Cyclosporine 131-142 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 8849485-7 1996 Of the 28 xenobiotics included in the study, 16 drugs, all well-known CYP 3A inhibitors, inhibited ciclosporin metabolism in the small intestine. Cyclosporine 99-110 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 70-76 8846621-5 1995 Significant amounts of CYP3A are present in the gastrointestinal tract, and may contribute to presystemic extraction of drugs such as cyclosporin. Cyclosporine 134-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 23-28 7628296-0 1995 Human liver cytochrome P4503A biotransformation of the cyclosporin derivative SDZ IMM 125. Cyclosporine 55-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-18 7895601-7 1994 Other CYP3A substrates (cyclosporin A, naringenin, and midazolam) also demonstrated potent inhibition of terfenadine biotransformation in human liver microsomes (IC50 = 17-24 microM). Cyclosporine 24-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-11 7965756-3 1994 It has been suggested that much of the variability in cyclosporine clearance is due to differences in the cytochrome P450 3A4 (CYP3A4) content in the liver and intestinal mucosa. Cyclosporine 54-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-125 7965756-3 1994 It has been suggested that much of the variability in cyclosporine clearance is due to differences in the cytochrome P450 3A4 (CYP3A4) content in the liver and intestinal mucosa. Cyclosporine 54-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-133 8013282-5 1994 The CYP3A substrate/inhibitor, cyclosporine A (CsA) had little effect on tropisetron hydroxylation (< 10%), whereas CsA and triacetyloleandomycin reduced ondansetron 7- and 8-hydroxylation up to 27%. Cyclosporine 47-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-9 8013282-8 1994 The CYP3A specific metabolism of CsA was also competitively inhibited by tropisetron (Ki = 2.1 mM) and ondansetron (Ki = 31 microM). Cyclosporine 33-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-9 8114683-3 1994 Using a panel of prototypical substrates and inhibitors for specific cytochromes P450, we identified substrates for CYP3A4 (midazolam, erythromycin, cyclosporin, and dexamethasone) as inhibitors of catechol formation from both etoposide and teniposide. Cyclosporine 149-160 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 116-122 1424421-1 1992 It has been shown recently that cyclosporine is largely metabolized by P450IIIA (CYP3A), an enzyme whose catalytic activity varies significantly among patients. Cyclosporine 32-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-86 8265621-1 1993 Human cytochrome P450 3A4 is recognized as the catalyst for the oxygen-dependent metabolism of a diverse group of medically important chemicals, including the immunosuppressive agent cyclosporin; macrolide antibiotics, such as erythromycin; drugs such as benzphetamine, nifedipine, and cocaine; and steroids; such as cortisol and testosterone to name but a few. Cyclosporine 183-194 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-25 8119047-4 1993 Macrolides inhibit cytochrome P450IIIA4 (CYP3A4), which appears to be the most common metabolic enzyme in the human liver and is involved in the metabolism of many drugs, including cyclosporin, warfarin and terfenadine. Cyclosporine 181-192 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 1643634-12 1992 Complete inhibition of the potentiation of MRA by human liver microsomes was found when the CYP3A substrates cyclosporin A and erythromycin were used in the reaction system. Cyclosporine 109-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-97