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

Sergio Leonardi, Pierluigi Tricoci, Richard C. Becker

Research output: Chapter in Book/Report/Conference proceedingChapter

3 Citations (Scopus)

Abstract

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.

Original languageEnglish
Title of host publicationAdvances in Cardiology
Pages87-99
Number of pages13
Volume47
DOIs
Publication statusPublished - Aug 2012

Publication series

NameAdvances in Cardiology
Volume47
ISSN (Print)00652326
ISSN (Electronic)16622839

Fingerprint

PAR-1 Receptor
Platelet Aggregation Inhibitors
Acute Coronary Syndrome
Thromboxanes
Platelet Activation
varespladib methyl
Hemorrhage
Thrombin Receptors
Thrombin
Adenosine Diphosphate
Aspirin
Therapeutics
Blood Platelets
Safety
Recurrence

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine
  • Medicine(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

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. In Advances in Cardiology (Vol. 47, pp. 87-99). (Advances in Cardiology; Vol. 47). https://doi.org/10.1159/000338045

Protease-activated receptor-1 inhibitors : A novel class of antiplatelet agents for the treatment of patients with acute coronary syndrome. / Leonardi, Sergio; Tricoci, Pierluigi; Becker, Richard C.

Advances in Cardiology. Vol. 47 2012. p. 87-99 (Advances in Cardiology; Vol. 47).

Research output: Chapter in Book/Report/Conference proceedingChapter

Leonardi, Sergio ; Tricoci, Pierluigi ; Becker, Richard C. / 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 2012. pp. 87-99 (Advances in Cardiology).
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