Antiplatelet agents are the standard of practice in the management of atherosclerosis and acute coronary syndrome. In contrast to the available antiplatelet agents, vorapaxar represents a novel mechanism of action. It is an antagonist of the platelet protease-activated receptor-1 and inhibits thrombin-induced and thrombin receptor agonist peptide-induced platelet aggregation. The Thrombin Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events-Thrombolysis in Myocardial Infarction 50 (TRA 2°P-TIMI 50) trial led to the approval of vorapaxar by the Food and Drug Administration and European Medicines Agency for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or peripheral arterial disease. TRA 2°P-TIMI 50 trial showed that the use of vorapaxar (2.5 mg once/daily) in addition to standard dual antiplatelet therapy with aspirin and a P2Y12 receptor inhibitor was effective in the secondary prevention of recurrent thrombotic events among patients with previous atherothrombosis, particularly in patients with prior MI; at the expense of an increase in major bleeding. Another recently published Vorapaxar Therapy in Patients With Prior Myocardial Infarction Treated With Newer Generation P2Y12 Receptor Inhibitors Prasugrel and Ticagrelor (VORA-PRATIC) study showed that among post-MI patients treated with potent P2Y12 inhibitors (prasugrel or ticagrelor), vorapaxar reduced platelet-driven global thrombogenicity, an effect that persisted, albeit attenuated, in the absence of aspirin. The current review summarizes an up-to-date literature on pharmacokinetics, pharmacodynamics, and clinical efficacy of vorapaxar and proposes future directions of research.

抗血小板药物是治疗动脉粥样硬化和急性冠状动脉综合征的实践标准。与现有的抗血小板药物相比，vorapaxar 代表了一种新的作用机制。它是血小板蛋白酶激活受体-1 的拮抗剂，可抑制凝血酶诱导和凝血酶受体激动剂肽诱导的血小板聚集。凝血酶受体拮抗剂在动脉粥样硬化血栓性缺血事件的二级预防中 - 心肌梗死溶栓 50 (TRA 2°P-TIMI 50) 试验导致美国食品药品监督管理局和欧洲药品管理局批准 vorapaxar 用于减少血栓性心血管事件有心肌梗塞 (MI) 或外周动脉疾病病史的患者。TRA 2°P-TIMI 50 试验表明使用 vorapaxar (2. 5 mg 每天一次）除了标准的阿司匹林和 P2Y12 受体抑制剂双重抗血小板治疗外，在既往有动脉粥样硬化血栓形成的患者中，特别是在有既往 MI 的患者中，对复发性血栓事件的二级预防是有效的；以增加大出血为代价。另一项最近发表的 Vorapaxar 治疗用新一代 P2Y12 受体抑制剂普拉格雷和替格瑞洛 (VORA-PRATIC) 治疗既往心肌梗塞患者的研究表明，在接受强效 P2Y12 抑制剂（普拉格雷或替格瑞洛）治疗的 MI 后患者中，vorapaxar 降低了血小板驱动全球血栓形成，这种效应在没有阿司匹林的情况下持续存在，尽管减弱了。本综述总结了关于药代动力学、药效学、