SCH 530348: a novel oral thrombin receptor antagonist.

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Bonaca MP, Morrow DA

SCH 530348: a novel oral thrombin receptor antagonist.

Future Cardiol. 2009 Sep;5(5):435-42. doi: 10.2217/fca.09.27.

PubMed ID

19715408 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Vorapaxar	Proteinase-activated receptor 1	Protein	Humans	Yes	Antagonist	Details