Abstract: 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.