Drug intelligence / Profile preview

vorapaxar

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Vorapaxar is an oral antiplatelet drug classified as a protease‑activated receptor‑1 (PAR‑1) antagonist. It inhibits thrombin-induced platelet aggregation by selectively and competitively blocking the PAR‑1 receptor on platelets. This mechanism reduces the risk of thrombotic cardiovascular events in patients with a history of myocardial infarction or peripheral arterial disease. Vorapaxar does not affect ADP-mediated platelet aggregation or coagulation parameters and is typically used alongside aspirin and/or clopidogrel. The drug was discovered by Schering-Plough and developed by Merck & Co., with its primary brand name being Zontivity[5][8][4].

Brand names
Zontivity
Other names
vorapaxarCarbamic acid, [(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]-, ethyl esterEthyl N-[(3R,3aS,4S,4aR,7R,8aR,9aR)-4-[(E)-2-[5-(3-fluorophenyl)-2-pyridyl]vinyl]-3-methyl-1-oxo-decahydro-benzo[f]isobenzofuran]-7-carbamate
02

Targets

F2R (Protease-activated receptor 1)

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