Protease-activated receptor-1 antagonists in long-term antiplatelet therapy. Current state of evidence and future perspectives

International Journal of Cardiology
I C MoschonasA D Tselepis

Abstract

Atherothrombosis and its clinical manifestations are among the leading causes of death in the developed world. The current standard-of-care antiplatelet therapy for the treatment of such events comprises aspirin and a thienopyridine or ticagrelor. However, recurrent ischemic events due to residual cardiovascular risk are a common phenomenon in these patients. It is believed that this residual risk is caused, at least in part, by thrombin, which signals through protease-activated receptors (PARs) and especially PAR-1. Thus, PAR-1 antagonism could represent an effective approach in the treatment of atherothrombotic disease. In this context, two potent and selective agents have been developed, vorapaxar and atopaxar. However, only vorapaxar has completed phase 3 clinical trials. In the present review, the main pharmacodynamic and pharmacokinetic properties of the PAR-1 antagonists are briefly described and the latest clinical data on vorapaxar are presented.

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Citations

Jun 10, 2017·Thrombosis and Haemostasis·Janina JamasbiWolfgang Siess
Aug 5, 2016·Journal of Cardiovascular Pharmacology and Therapeutics·Iraklis C Moschonas, Alexandros D Tselepis
Jan 16, 2021·Journal of Thrombosis and Thrombolysis·Iraklis C Moschonas, Alexandros D Tselepis

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