Department of Genetics and Genomic Sciences, Icahn School of Medicine at Mount Sinai, New York, New York, USA.
Clin Pharmacol Ther. 2013 Sep;94(3):317-23. doi: 10.1038/clpt.2013.105. Epub 2013 May 22.
Cytochrome P450 (CYP)2C19 catalyzes the bioactivation of the antiplatelet prodrug clopidogrel, and CYP2C19 loss-of-function alleles impair formation of active metabolites, resulting in reduced platelet inhibition. In addition, CYP2C19 loss-of-function alleles confer increased risks for serious adverse cardiovascular (CV) events among clopidogrel-treated patients with acute coronary syndromes (ACSs) undergoing percutaneous coronary intervention (PCI). Guideline updates include emphasis on appropriate indication for CYP2C19 genotype-directed antiplatelet therapy, refined recommendations for specific CYP2C19 alleles, and additional evidence from an expanded literature review (updates at http://www.pharmgkb.org).
细胞色素 P450 (CYP)2C19 催化抗血小板前体药物氯吡格雷的生物活化,而 CYP2C19 功能丧失等位基因会损害活性代谢物的形成,导致血小板抑制作用减弱。此外,携带 CYP2C19 功能丧失等位基因的患者在接受经皮冠状动脉介入治疗 (PCI) 时,发生急性冠脉综合征 (ACS) 后,发生严重心血管 (CV) 事件的风险增加。指南更新包括强调适当的 CYP2C19 基因型指导的抗血小板治疗的适应证,对特定 CYP2C19 等位基因的细化建议,以及来自扩展文献综述的额外证据(更新于 http://www.pharmgkb.org)。