Research progress on clinical gene polymorphism of clopidogrel resistance / 中国药学杂志

ABSTRACT

Clopidogrel plays an important role in anti-platelet aggregation, especially in acute coronary syndrome and percutaneous coronary intervention. However, clopidogrel resistance is common in clinical treatment. There are many factors response to clopidogrel resistance.Current researches concentrated in CYP450 enzyme gene polymorphism with clopidogrel resistance. There are few reviews on genetic polymorphisms of transporter and receptor binding sites, furthermore, the gene polymorphisms among different ethnic groups in plateau populations are very rare. In this paper, we mainly reviewed the relationship between gene polymorphism of drug-transporter and bioavailability of clopidogrel, the whole process of drug-metabolizing enzyme′s bioconversion of clopidogrel and the active metabolite of clopidogrel combine with the receptors.A mutation in the ABCB1 gene of the transporter was found to affect the bioavailability of clopidogrel. The key role of polymorphisms in the metabolic enzyme gene is CYP2C19 and CES1. The dose should be adjusted according to genotyping. The biologically active gene P2Y12 polymorphism affects the efficacy of clopidogrel. Therefore, understanding the clopidogrel gene polymorphism influencing factors can help individualized administration of clopidogrel to minimize thrombotic events caused by insufficient antiplatelet effect or hemorrhagic events caused by excessive anti-platelet effect.