Intravenous AR-C69931MX provided rapid, safe, and more effective inhibition of platelet function than clopidogrel in patients with acute coronary syndromes.
Do direct P2T receptor antagonists like AR-C69931MX improve inhibition of platelet aggregation compared to thienopyridines in patients with acute coronary syndromes?
The direct P2T receptor antagonist AR-C69931MX provides rapid, potent, and reversible platelet inhibition that is more effective than clopidogrel in patients with acute coronary syndromes.
Abstract Rupture of atherosclerotic plaques and subsequent thrombus formation in coronary arteries are key events in the progression of coronary artery disease and the pathogenesis of acute coronary syndromes. Platelets play a crucial role in this thrombus formation and the success of aspirin in reducing cardiovascular morbidity and mortality has spurred on the search for antiplatelet agents that have an alternative mechanism of action and may, therefore, add to the therapeutic effects of aspirin. The thienopyridines, ticlopidine and clopidogrel, act via metabolites on the platelet ADP receptor subtype designated P 2T , and these agents have proven clinical efficacy, either as alternatives to aspirin or, in prevention of coronary stent thrombosis, in combination with aspirin. Potent P 2T receptor antagonists have been developed that act directly on the receptor and have a rapid onset of action. One such antagonist, AR‐C69931MX, is being developed for clinical use. AR‐C69931MX is a potent antagonist of ADP‐induced platelet activation, aggregation, and secretion and also antagonises platelet responses to all other agonists in view of the central role of the P 2T receptor in amplifying platelet responses. Phase II studies of intravenous AR‐C69931MX in patients with acute coronary syndromes show that this agent has a rapid onset of action, rapidly achieving steady‐state inhibition of platelet aggregation, with a half‐life of only a few minutes. AR‐C69931MX appears to be safe and well tolerated as adjunctive therapy in these patients, and more effective inhibition of platelet function is achieved than with the thienopyridine clopidogrel. Orally active antagonists are also being developed that may be more effective than the thienopyridines. Drug Dev. Res. 52:202–212, 2001. © 2001 Wiley‐Liss, Inc.
Robert F. Storey (Mon,) conducted a review in Acute coronary syndromes. AR-C69931MX vs. Clopidogrel was evaluated. Intravenous AR-C69931MX provided rapid, safe, and more effective inhibition of platelet function than clopidogrel in patients with acute coronary syndromes.