氯吡格雷抵抗CYP2C19基因多态性研究现状

Study status of the clopidogrel resistance and CYP2C19 genetic polymorphisms

关键词:  氯吡格雷  氯吡格雷抵抗  CYP2C19  基因多态性  血小板聚集

Key words:  clopidogrel  clopidogrel resistance  CYP2C19  genetic polymorphism  platelet aggregation

摘要:

氯吡格雷是一种新型噻吩吡啶类抗血小板药，它是一种药物前体，经小肠内吸收和肝脏代谢转化为有活性的代谢物后通过阻断血小板膜P2Y2受体与ADP结合而发挥抗血小板作用。但并不是所有的服用患者都同等受益，近年研究表明部分患者存在氯吡格雷抵抗，多数学者认为参与氯吡格雷代谢的CYP2C19等基因多态性与氯吡格雷抵抗密切相关。本文系统综述了氯吡格雷的药物代谢、吸收、转化特点以及近几年国内外在不良心脑血管事件中CYP2C19*2，CYP2C19*3，CYP2C19*17基因多态性与氯吡格雷的疗效关系。

Abstract:

Clopidogrel is a new type of thienopyridine antiplatelet drug. It is a prodrug, the intestinal absorption and metabolism in the liver resulting into active metabolites which block platelet membrane P2Y2 receptor and ADP binding and play antiplatelet effect. But not all patients are equally beneficial, and recent years studies have indicated that some patients have clopidogrel resistance. Most scholars believe that the polymorphisms of CYP2C19 and other genes involved in clopidogrel metabolism are closely related to clopidogrel resistance, this paper reviews the clopidogrel drug metabolism, absorption, transformation characteristics and recent research in adverse cardiovascular and cerebrovascular events of the CYP2C19*2,CYP2C19*3 and CYP2C19*17 gene polymorphism and clopidogrel treatment effect.