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Protease-activated receptor-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with acute coronary syndrome.

Publication ,  Journal Article
Leonardi, S; Tricoci, P; Becker, RC
Published in: Advances in cardiology
January 2012

The unifying basis of acute coronary syndrome (ACS) is the complication of a vulnerable coronary plaque, an event primarily mediated by platelet activation. Three major pathways are predominantly involved in this process: thromboxane A(2) via the thromboxane A(2) receptor, adenosine diphosphate via the P2Y(12) receptor, and thrombin via the protease-activated receptor (PAR)-1, with the latter being the most potent platelet activator. Despite the effective inhibition of the first two pathways with aspirin and an expanding family of P2Y(12) inhibitors, respectively, the recurrence of ischemic events in patients with ACS remains high. There is also a growing concern regarding the safety profile in terms of bleeding with more powerful antiplatelet agents, which has tempered expectations of newly developed compounds. PAR-1 inhibitors are a novel class of antiplatelet agents that inhibit thrombin-mediated platelet activation. Preliminary data indicate that these compounds have the potential to improve ischemic prognosis without increasing the bleeding risk. In this chapter we will discuss the rationale for developing this novel class of antiplatelet agents and specifically, the two compounds in most advanced clinical development, vorapaxar and atopaxar.

Duke Scholars

Published In

Advances in cardiology

DOI

EISSN

1662-2839

ISSN

0065-2326

Publication Date

January 2012

Volume

47

Start / End Page

87 / 99

Related Subject Headings

  • Receptors, Thrombin
  • Receptor, PAR-1
  • Pyridines
  • Platelet Aggregation
  • Myocardial Ischemia
  • Lactones
  • Imines
  • Humans
  • Cardiovascular System & Hematology
  • Animals
 

Citation

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Leonardi, S., Tricoci, P., & Becker, R. C. (2012). Protease-activated receptor-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with acute coronary syndrome. Advances in Cardiology, 47, 87–99. https://doi.org/10.1159/000338045
Leonardi, Sergio, Pierluigi Tricoci, and Richard C. Becker. “Protease-activated receptor-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with acute coronary syndrome.Advances in Cardiology 47 (January 2012): 87–99. https://doi.org/10.1159/000338045.
Leonardi, Sergio, et al. “Protease-activated receptor-1 inhibitors: a novel class of antiplatelet agents for the treatment of patients with acute coronary syndrome.Advances in Cardiology, vol. 47, Jan. 2012, pp. 87–99. Epmc, doi:10.1159/000338045.
Journal cover image

Published In

Advances in cardiology

DOI

EISSN

1662-2839

ISSN

0065-2326

Publication Date

January 2012

Volume

47

Start / End Page

87 / 99

Related Subject Headings

  • Receptors, Thrombin
  • Receptor, PAR-1
  • Pyridines
  • Platelet Aggregation
  • Myocardial Ischemia
  • Lactones
  • Imines
  • Humans
  • Cardiovascular System & Hematology
  • Animals