Products
Vorapaxar was approved in the form of film-coated tablets in the United States in 2014, in the EU in 2015, and in many countries in 2016 (Zontivity, MSD).
Structure and properties
Vorapaxar (C29H33FN2O4, Mr = 492.6 g/mol) is present as a white powder. It is a tricyclic 3-phenylpyridine derivative of himbacin, a natural alkaloid derived from an Australian magnolia species.
Effects
Vorapaxar has platelet aggregation inhibitory properties, preventing the formation of blood clots in the vessels. The effects are due to competitive antagonism at PAR-1 (protease-activated receptor-1), a G-protein-coupled receptor (GPCR) expressed on platelets. Binding of thrombin to PAR-1 leads to platelet aggregation. In contrast, Vorapaxar has no effect on the cleavage of fibrinogen to fibrin. This is in contrast to other antithrombotics (eg, thrombin inhibitors).
Indications
For prevention of cardiovascular complications (eg, myocardial infarction, stroke) in patients with myocardial infarction or occlusion in the leg arteries.
Dosage
According to the SmPC. The drug has a long half-life and therefore needs to be taken only once daily.
Contraindications
For complete precautions, see the drug label.
Interactions
Vorapaxar is a substrate of CYP3A4.
Adverse effects
The most common potential adverse effects include bleeding.
