Deciphering the Relative Contribution of CYP3A4 Versus P-Glycoprotein for the Shared Substrate Cyclosporine-Commentary on Lown et al.

Authors

Ingolf Cascorbi, Richard B Kim

Published in

Clinical pharmacology and therapeutics. Volume 117. Issue 6. Pages 1546-1561.

Abstract

The oral bioavailability of cyclosporine, a substrate of both CYP3A4 and P-glycoprotein, is subject to large inter-individual variability, which requires frequent monitoring of plasma concentrations. In 1997, the study by Lown et al. showed that-in addition to hepatic CYP3A4-the expression of P-gp in the intestine significantly influences the pharmacokinetics of cyclosporine in kidney transplant patients. The results contributed considerably to a better understanding of the function of the intestinal P-glycoprotein for drug clearance.

PMID:
40388112
Bibliographic data and abstract were imported from PubMed on 19 May 2025.

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