Protease-Activated Receptor 1 Inhibitors: Novel Antiplatelet Drugs in Prevention of Atherothrombosis

Abstract

Protease-activated receptor (PAR)-1 inhibitors have recently become popular in the use of atherosclerosis among clinicians. Atherosclerosis can cause cardiovascular and cerebrovascular events leading to one of the major causes of mortality worldwide. Thrombin-mediated platelets can cause atherosclerotic plaques, and these platelets are activated by thrombin through the PAR-1. Vorapaxar and atopaxar are novel antiplatelet drugs that inhibit the thrombin-induced platelet activation by antagonizing the PAR-1. The objective of this article is to review the mechanism of action of vorapaxar and atopaxar and explain the rationale for using them in atherothrombosis patients including myocardial infarction, peripheral arterial disease, and stroke.

Anti‐platelet agents: past, present and future

“…This led to the development of specific inhibitors of PAR-1 for use as antiplatelet agents [72]. Vorapaxar [73] and atopaxar are two such agents and have been shown to be effective in clinical trials [74]. However, there is no evidence that they are more effective than other agents and have a bleeding risk associated with them.…”