Discovery of an orally available PAR-1 antagonist as a novel antiplatelet agent

Antiplatelet therapy is a key treatment in atherothrombotic disease and platelet is activated via multiple pathways. Current agents do not interfere with all pathways including the protease-activated receptor-1 (PAR-1) pathway stimulated by thrombin. New antiplatelet agents targeting PAR-1 are aimed to reduce thrombosis ideally without increasing bleeding risk. This article provides a review of the new class of agents, PAR-1 antagonists.