沃拉帕沙的临床研究进展

沃拉帕沙为选择性、口服、强力、竞争性蛋白酶激活受体1(PAR-1)拮抗剂，对凝血酶诱导的血小板聚集有很强的抑制作用。沃拉帕沙口服后快速吸收，具有独特的药动学特性，半衰期长达7 d(159~311 h)。它主要经胆汁和胃肠道代谢和消除。2个针对急慢性冠状动脉粥样硬化患者的大型Ⅲ期临床试验结果表明，沃拉帕沙可以防止有心肌梗死病史、或者外周动脉疾病患者血栓性心血管病的发作，也可降低心肌梗死、中风和紧急冠脉血管重建患者的死亡率。

Progress of Vorapaxar Clinical Research

Vorapaxar is a selective, orally active, potent, and competitive protease-activated receptor 1 antagonist that potently inhibits thrombin-induced platelet aggregation. Vorapaxar is rapidly absorbed via the oral route and has peculiar pharmacokinetics with a half-life of 7 d(159-311 h). It is metabolized and eliminated primarily by biliary and gastrointestinal routes. Its phase III program included two large trials in patients with acute and chronic coronary atherothrombosis indicated for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral arterial disease. Vorapaxar also has been shown to reduce the rate of a combined endpoint of cardiovascular death, MI, stroke, and urgent coronary revascularization.