title: Atopaxar: a review of its mechanism of action and role in patients with coronary artery disease.
abstract: Platelet activation and aggregation is a complex and key process in thrombus formation after the rupture of an atherosclerotic plaque, which can lead to an acute coronary syndrome. Aspirin, an irreversible inhibitor of thromboxane A(2) synthesis, in combination with an inhibitor of P2Y(12) ADP platelet receptors (clopidogrel, prasugrel or ticagrelor), represents the current standard of care of antiplatelet therapy for patients with acute coronary syndrome and in those patients undergoing percutaneous coronary intervention. Despite the benefit of these agents, the risk of thrombotic events and bleeding complications may still occur while on such antiplatelet treatment regimens, thus representing an important limitation. Thrombin is one of the most important platelet activators. The inhibition of thrombin-mediated platelet activation by means of protease-activated receptor-1 inhibitors represents an attractive therapeutic option for patients with atherothrombotic disease processes. This article provides an overview on atopaxar (E5555), an orally active protease-activated receptor-1 antagonist that has recently completed Phase II clinical investigation.
authors.affiliation: University of Florida College of Medicine-Jacksonville, 655 West 8th Street, Jacksonville, FL 32209, USA.
authors.forename: Fabiana
authors.initials: F
authors.lastname: Rollini
authors.forename: Antonio
authors.initials: A
authors.lastname: Tello-Montoliu
authors.forename: Dominick J
authors.initials: DJ
authors.lastname: Angiolillo
mesh_terms: D054058:Acute Coronary Syndrome / Q000188:drug therapy; D000818:Animals; D000077144:Clopidogrel; D003324:Coronary Artery Disease / Q000188:drug therapy*; D003328:Coronary Thrombosis / Q000517:prevention & control; D006801:Humans; D007097:Imines / Q000494:pharmacology* / Q000627:therapeutic use*; D015539:Platelet Activation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D011725:Pyridines / Q000494:pharmacology* / Q000627:therapeutic use*; D018179:Receptors, Thrombin / Q000037:antagonists & inhibitors*; D013988:Ticlopidine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: C540445:E 5555; D007097:Imines; D010975:Platelet Aggregation Inhibitors; D011725:Pyridines; D018179:Receptors, Thrombin; D000077144:Clopidogrel; D013988:Ticlopidine