Drug intelligence / Profile preview

vorapaxar + aspirin

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

Overview

Vorapaxar + aspirin is a combination therapy used to reduce the risk of serious or life-threatening cardiovascular events, such as heart attack and stroke, in patients with a history of myocardial infarction (MI) or peripheral arterial disease (PAD). Vorapaxar is a first-in-class small molecule antagonist of protease-activated receptor 1 (PAR-1), the primary thrombin receptor on platelets. By inhibiting PAR-1, vorapaxar blocks thrombin-induced platelet aggregation. Aspirin acts as an antiplatelet agent by irreversibly inhibiting cyclooxygenase-1 (COX-1), thereby reducing thromboxane A2 production and further decreasing platelet aggregation. The combination is typically used for secondary prevention in patients at high risk for recurrent atherothrombotic events[1][2][3][5]. Clinical trials have demonstrated that adding vorapaxar to standard antiplatelet therapy with aspirin can further reduce the incidence of major cardiovascular events but increases bleeding risk[6][8].

Other names
acetylsalicylic acid
02

Targets

F2R (Protease-activated receptor 1)PGHS-1 (Prostaglandin G/H Synthase 1)

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