Abstract

Vorapaxar (ZONTIVITY™) is a first-in-class selective antagonist of protease-activated receptor 1 (PAR-1), the primary thrombin receptor on human platelets, which mediates the downstream effects of this critical coagulation factor in haemostasis and thrombosis. Thrombin-induced platelet activation has been implicated in a variety of cardiovascular (CV) disorders including thrombosis, atherosclerosis, and restenosis following percutaneous coronary intervention (PCI). As an antagonist of PAR-1, vorapaxar blocks thrombin-mediated platelet aggregation and thereby has the potential to reduce the risk of atherothrombotic complications of coronary disease. It is given in combination with acetylsalicylic acid (ASA) and, where appropriate, with a third medicine, clopidogrel, both of which also help prevent atherothrombotic events.