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Ticagrelor is the first reversible, direct-acting, potent P2Y 12  receptor antagonist in management of acute coronary syndromes. It is rapidly absorbed and extensively metabolized. AR-C124910XX, the major active metabolite, antagonizes the P2Y 12  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 patient response. Thus, this study is designed to explore the effects of  CYP3A4 ∗ 1G  and  CYP3A5 ∗ 3  polymorphisms on the pharmacokinetics and pharmcodynamics of ticagrelor in healthy Chinese subjects. The results indicated that the  CYP3A4 ∗ 1G  polymorphism significantly influenced the pharmacokinetics of AR-C124910XX, and it may be more important than  CYP3A5 ∗ 3  with respect to influencing ticagrelor pharmacokinetics by increasing CYP3A4 activity. However, the significant effect of  CYP3A4 ∗ 1G  polymorphism on AR-C124910XX plasma levels did not translate into detectable effect on inhibition of platelet aggregation. Therefore, it seems not necessary to adjust the dosage of ticagrelor according to the  CYP3A4  or  3A5  genotype.

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