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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。
Volaporase is a selective, oral, potent, and competitive inhibitor of protease-activated receptor 1 (PAR-1), with a strong inhibitory effect on thrombin-induced platelet aggregation. Valapagas quickly absorbed after oral administration, has a unique pharmacokinetic properties, half-life up to 7 d (159 ~ 311 h). It is mainly bile and gastrointestinal metabolism and elimination. Two large phase III trials of patients with acute and chronic coronary atherosclerosis showed that valapresf can prevent a history of myocardial infarction or thrombotic cardiovascular disease in patients with peripheral arterial disease and also reduce myocardial infarction, Mortality in patients with stroke and emergency coronary revascularization.