Influence of genetic polymorphisms on the pharmacokinetics of tacrolimus in patients with organ transplantation
WANG Hua-ming
HU Yong-fang
Abstract：Tacrolimus (FK506), a widely used immunosuppressant, exerts a key effect in patients with or-gan transplantation. The drug requires therapeutic monitoring due to its narrow therapeutic index and great inter-in-dividual variability. FK506 is known to be a substrate of CYP3A and P-glycoprotein (P-gp). FK506 is metabolized by CYP3A and transported by P-gp. The difference in expression level and the bioactivity of these proteins may ex-plain individual variations of FK506 pharmacokinetics. The differences in bioactivities of CYP3A and P-gp are be-lieved to be due to CYP3A and MDR1 genetic "mutation. Therefore, genetic variations of CYP3A and MDR1 may play an important role in the inter-individual variability of FK506. In this article, we reviewed the effect of CYP3A and MDR1 gene polymorphisms on pharmacokinetics of FK506 in patients with organ transplantation.
Keywords：tacrolimuspharmacokineticsCYP3A5MDR1gene polymorphism
Publication Date：2009-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：4( 1300-1303 )