|Systematic (IUPAC) name|
|Mol. mass||492.58 g/mol|
|(what is this?)|
Vorapaxar (formerly SCH 530348) is a thrombin receptor (protease-activated receptor, PAR-1) antagonist based on the natural product himbacine. Discovered by Schering-Plough and currently being developed by Merck & Co., it is an experimental pharmaceutical treatment for acute coronary syndrome chest pain caused by coronary artery disease.
In January 2011, clinical trials being conducted by Merck were halted for patients with stroke and mild heart conditions. In a randomized double-blinded trial comparing vorapaxar with placebo in addition to standard therapy in 12,944 patients who had acute coronary syndromes, there was no significant reduction in a composite end point of death from cardiovascular causes, myocardial infarction, stroke, recurrent ischemia with rehospitalization, or urgent coronary revascularization. However, there was increased risk of major bleeding.
A trial published in February 2012, found no change in all cause mortality while decreasing the risk of cardiac death and increasing the risk of major bleeding, including intracranial hemorrhages. After 2 years, the data and safety monitoring board recommended discontinuation of the study treatment in patients with a history of stroke owing to the risk of intracranial hemorrhage.
Vorapaxar was recommended for FDA approval on January 15, 2014.
- Samuel Chackalamannil; Wang, Yuguang; Greenlee, William J.; Hu, Zhiyong; Xia, Yan; Ahn, Ho-Sam; Boykow, George; Hsieh, Yunsheng et al. (2008). "Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity". Journal of Medicinal Chemistry 51 (11): 3061–4. doi:10.1021/jm800180e. PMID 18447380.
- Merck Blood Thinner Studies Halted in Select Patients, Bloomberg News, January 13, 2011
- Tricoci et al. (2012). "Thrombin-Receptor Antagonist Vorapaxar in Acute Coronary Syndromes". New England Journal of Medicine 366 (1): 20–33. doi:10.1056/NEJMoa1109719. PMID 22077816.
- Morrow, DA; Braunwald, E; Bonaca, MP; Ameriso, SF; Dalby, AJ; Fish, MP; Fox, KA; Lipka, LJ; Liu, X; Nicolau, JC; Ophuis, AJ; Paolasso, E; Scirica, BM; Spinar, J; Theroux, P; Wiviott, SD; Strony, J; Murphy, SA; TRA 2P–TIMI 50 Steering Committee and, Investigators (Apr 12, 2012). "Vorapaxar in the secondary prevention of atherothrombotic events.". The New England Journal of Medicine 366 (15): 1404–13. doi:10.1056/NEJMoa1200933. PMID 22443427.
- "Merck Statement on FDA Advisory Committee for Vorapaxar, Merck’s Investigational Antiplatelet Medicine". Merck. Retrieved 16 January 2014.
- Stu Borman (2005). "Hopes Ride on Drug Candidates: Researchers reveal potential new medicines for thrombosis, anxiety, diabetes, and cancer". Chemical & Engineering News 83 (16): 40–44.
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