A novel inhibitor of protease-activated receptor 1: A review of chemical structure and mode of action

Mehrnoosh Hashemzadeh, Joseph M. Arreguin, Tyler Roberts, Mohammad R Movahed

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

Limitations of current antiplatelet therapies have led to the discovery of new antiplatelet agents with new modes of action. Vorapaxar has been developed as a thrombin receptor antagonist. This drug works against the protease-activated receptor 1 (PAR1) and inhibits platelet aggregation mediated by PAR1. This article reviews this new class of antiplatelet therapy in detail with an acute focus on the TRACER (Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome) and TRA 2°P-TIMI 50 (Trial to Assess the Effects of Vorapaxar in Preventing Heart Attack and Stroke in Patients With Atherosclerosis-Thrombolysis In Myocardial Infarction 50) trials. Vorapaxar has proven to be beneficial when administered to stable atherosclerotic patients. However, it has been shown to increase risk of intracranial hemorrhage in patients with known, previous history of cerebrovascular incidence. Despite these limitations, TRA 2°P-TIMI 50 results showed that vorapaxar appears to have a definitive therapeutic benefit when administered alongside aspirin or when it is used as an addition to dual antiplatelet therapy for patients with stable atherosclerosis.

Original languageEnglish (US)
Pages (from-to)68-73
Number of pages6
JournalReviews in Cardiovascular Medicine
Volume16
Issue number1
DOIs
StatePublished - 2015

Fingerprint

PAR-1 Receptor
Thrombin Receptors
Atherosclerosis
Myocardial Infarction
Intracranial Hemorrhages
Platelet Aggregation Inhibitors
Therapeutics
Acute Coronary Syndrome
Platelet Aggregation
Aspirin
Stroke
vorapaxar
Incidence
Pharmaceutical Preparations

Keywords

  • Acute coronary syndrome
  • Antiplatelet
  • Atherosclerosis
  • PAR1 inhibitor
  • Thienopyridines
  • Thrombin receptor antagonist
  • Vorapaxar

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine

Cite this

A novel inhibitor of protease-activated receptor 1 : A review of chemical structure and mode of action. / Hashemzadeh, Mehrnoosh; Arreguin, Joseph M.; Roberts, Tyler; Movahed, Mohammad R.

In: Reviews in Cardiovascular Medicine, Vol. 16, No. 1, 2015, p. 68-73.

Research output: Contribution to journalArticle

Hashemzadeh, Mehrnoosh ; Arreguin, Joseph M. ; Roberts, Tyler ; Movahed, Mohammad R. / A novel inhibitor of protease-activated receptor 1 : A review of chemical structure and mode of action. In: Reviews in Cardiovascular Medicine. 2015 ; Vol. 16, No. 1. pp. 68-73.
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