Effect of CYP3A4^∗1G and CYP3A5^∗3 Polymorphisms on Pharmacokinetics and Pharmacodynamics of Ticagrelor in Healthy Chinese Subjects.

ABSTRACT: Ticagrelor is the first reversible, direct-acting, potent P2Y₁₂ receptor antagonist in management of acute coronary syndromes. It is rapidly absorbed and extensively metabolized. AR-C124910XX, the major active metabolite, antagonizes the P2Y₁₂ receptor at approximately equal potency. The metabolism of ticagrelor to AR-C124910XX involves CYP3A4 and CYP3A5. CYP3A polymorphisms have been well documented, and CYP3A4^∗1G (g.20230G>A, rs2242480) and CYP3A5^∗3 (g.6986A>G, rs776746) are the most important single nucleotide polymorphisms in Chinese. Genetic differences in CYP3A4 and CYP3A5 expression in human volunteers and patients might affect the clearance of ticagrelor or AR-C124910XX in vivo resulting in subsequent variable

SUBMITTER: Liu S 

PROVIDER: S-EPMC5374142 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature