Vorapaxar, platelet aggregation inhibitor, inhibiting PAR-1 receptor (Protease-Activated Receptor)
| Author : Pierre Allain
||Date : 2012-5-2
Vorapaxar is an antagonist of thrombin on platelets, it blocks the receptor called protease-activated receptor, PAR-1 and thus inhibits the platelet-aggregating effect of thrombin. In addition to its effect on the conversion of fibrinogen into fibrin, thrombin actives PAR-1 receptors and has a platelet-aggregating effect.
A clinical study published in the NEJM of April 12th, 2012 shows that vorapaxar, administered by oral route at the dose of 2.5 mg to patients with cardiovascular antecedents, particularly myocardial infarctions, reduced the frequency of the cardiovascular events but increased the bleeding in particular the intracranial hemorrhages, which can thwart the development of vorapaxar.
Notice : One can classify antiplatelet drugs in 4 groups:
- Inhibitors of cyclooxygenases, like aspirin
- Inhibitors of ADP receptors, like clopidogrel
- Inhibitors of glycoprotein IIb/IIIa, like abciximab
- Inhibitors of PAR-1 receptors of thrombin, like vorapaxar
For more information, to see antiplatelets.