Identification of drugs inhibiting thein vitrometabolism of tacrolimus by human liver microsomes
- 1 March 1996
- journal article
- Published by Wiley in British Journal of Clinical Pharmacology
- Vol. 41 (3) , 187-190
- https://doi.org/10.1111/j.1365-2125.1996.tb00181.x
Abstract
1 Tacrolimus, an immunosuppressive macrolide, is metabolized by enzymes of the cytochrome P450 3A subfamily. In this study, 34 drugs were tested for their interactions with tacrolimus metabolism by human liver microsomes.2 Fifteen drugs which inhibit thein vitrometabolism of tacrolimus were identified: bromocriptine, corticosterone, dexamethasone, ergotamine, erythromycin, ethinyloestradiol, josamycin, ketoconazole, miconazole, midazolam, nifedipine, omeprazole, tamoxifen, troleandomycin and verapamil.Keywords
This publication has 9 references indexed in Scilit:
- Isolation, identification, and biological activities of oxidative metabolites of FK506, a potent immunosuppressive macrolide lactone.Drug Metabolism and Disposition, 2025
- Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes.Drug Metabolism and Disposition, 2025
- Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat.Drug Metabolism and Disposition, 2025
- Further metabolism of FK506 (tacrolimus). Identification and biological activities of the metabolites oxidized at multiple sites of FK506.Drug Metabolism and Disposition, 2025
- FK 506 metabolism in human liver microsomes: investigation of the involvement of cytochrome P450 isozymes other than CYP3A4.Drug Metabolism and Disposition, 2025
- Measurement of blood concentrations of FK506 (tacrolimus) and its metabolites in seven liver graft patients after the first dose by h.p.l.c.‐MS and microparticle enzyme immunoassay (MEIA).British Journal of Clinical Pharmacology, 1994
- Metabolism of FK506, a potent immunosuppressive agent, by cytochrome P450 3A enzymes in rat, dog and human liver microsomesBiochemical Pharmacology, 1994
- TacrolimusDrugs, 1993
- Structural Investigations of 13‐O‐Demethyl‐FK506 and Its Isomers Generated by in vitro Metabolism of FK506 Using Human‐Liver MicrosomesHelvetica Chimica Acta, 1993