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PAR-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with atherothrombosis.

Publication ,  Journal Article
Leonardi, S; Becker, RC
Published in: Handbook of experimental pharmacology
January 2012

Stroke and myocardial infarction are leading causes of death and disability worldwide. Typically, these events are triggered by the rupture or erosion of "vulnerable" atherosclerotic plaque, a phenomenon termed atherothrombosis.Three platelet activation pathways are presumed to be particularly important in the genesis of atherothrombosis and are triggered by 1) cyclo-oxygenase (COX)-1 mediated thromboxane A2 (TXA2) synthesis and activation via the TXA2 receptor, 2) adenosine diphosphate (ADP) via the P2Y12 receptor, and 3) thrombin via the protease activated receptor (PAR)-1.Despite the efficacy of aspirin and of a growing family of P2Y12 receptor antagonists on the first 2 pathways, major cardiovascular events continue to occur in patients with coronary and cerebrovascular disease, suggesting that thrombin-mediated platelet activation may contribute to these adverse events.Recently, a novel class of antiplatelet agents able to inhibit thrombin-mediated platelet activation has been developed, PAR-1 inhibitors. In this chapter, we will discuss the rationale underlying the development of this novel class of agents focus on the two drugs in the most advanced stages of development: vorapaxar (SCH530348) and atopaxar (E5555).

Duke Scholars

Published In

Handbook of experimental pharmacology

DOI

ISSN

0171-2004

Publication Date

January 2012

Issue

210

Start / End Page

239 / 260

Related Subject Headings

  • Thrombosis
  • Receptor, PAR-1
  • Pyridines
  • Platelet Aggregation Inhibitors
  • Plaque, Atherosclerotic
  • Lactones
  • Imines
  • Humans
  • Clinical Trials as Topic
  • Animals
 

Citation

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Leonardi, S., & Becker, R. C. (2012). PAR-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with atherothrombosis. Handbook of Experimental Pharmacology, (210), 239–260. https://doi.org/10.1007/978-3-642-29423-5_10
Leonardi, Sergio, and Richard C. Becker. “PAR-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with atherothrombosis.Handbook of Experimental Pharmacology, no. 210 (January 2012): 239–60. https://doi.org/10.1007/978-3-642-29423-5_10.
Leonardi S, Becker RC. PAR-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with atherothrombosis. Handbook of experimental pharmacology. 2012 Jan;(210):239–60.
Leonardi, Sergio, and Richard C. Becker. “PAR-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with atherothrombosis.Handbook of Experimental Pharmacology, no. 210, Jan. 2012, pp. 239–60. Epmc, doi:10.1007/978-3-642-29423-5_10.
Leonardi S, Becker RC. PAR-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with atherothrombosis. Handbook of experimental pharmacology. 2012 Jan;(210):239–260.

Published In

Handbook of experimental pharmacology

DOI

ISSN

0171-2004

Publication Date

January 2012

Issue

210

Start / End Page

239 / 260

Related Subject Headings

  • Thrombosis
  • Receptor, PAR-1
  • Pyridines
  • Platelet Aggregation Inhibitors
  • Plaque, Atherosclerotic
  • Lactones
  • Imines
  • Humans
  • Clinical Trials as Topic
  • Animals