Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety

摘要: Dual antiplatelet therapy, composed of aspirin plus a P2Y12-receptor antagonist, is the cornerstone treatment for patients with acute coronary syndrome (ACS). A number U.S. Food and Drug Administration–approved antagonists are available treating ACS, including thienopyridine compounds clopidogrel prasugrel. Ticagrelor, first new class agents, noncompetitive, direct-acting antagonist. Unlike compounds, ticagrelor does not require metabolism activity. Also, whereas prasugrel irreversible inhibitors P2Y12 receptor, binds reversibly to inhibit receptor signaling subsequent platelet activation. In pharmacodynamic studies, demonstrated faster onset more potent inhibition aggregation than clopidogrel. These properties may contribute reduced rates thrombotic outcomes compared clopidogrel, as in phase III clinical trial. However, addition bleeding, distinctive adverse effects this chemical entity have been reported inhibitors. Although represents an advancement thorough understanding compound therapy remains be elucidated.