Does SCH 530348 reduce the risk of ischemic events without significantly increasing the rate of bleeding in patients with acute coronary syndromes or requiring secondary prevention of atherothrombotic events?
SCH 530348 is a novel, orally active PAR-1 antagonist that inhibits thrombin-mediated platelet aggregation and is entering Phase III trials for ACS and secondary prevention.
SCH 530348, a synthetic tricyclic 3-phenylpyridine, is an orally active fourth generation himbacine-based antagonist of the protease-activated receptor (PAR)-1, the primary receptor for thrombin on platelets in humans. SCH 530348 is the first in a new class of compounds that inhibit thrombin-mediated platelet aggregation without affecting the enzymatic activity of thrombin on fibrinogen. Preclinical and initial clinical studies have demonstrated this compound to be a highly potent inhibitor of thrombin-induced platelet activation, to have excellent oral bioavailability and to have a favorable safety profile. These data suggest that this compound has the potential to reduce the risk of ischemic events without significantly increasing the rate of bleeding. Two large Phase III clinical outcome trials are currently underway to evaluate the safety and efficacy of SCH 530348 for the management of acute coronary syndromes and the secondary prevention of atherothrombotic events.
Bonaca et al. (Fri,) studied this question.
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