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'''Vorapaxar''' (formerly SCH-530,348) is a ] receptor (]) antagonist based on the natural product ]. Discovered by ] and currently being developed by ], it is a experimental pharmaceutical treatment for acute coronary syndrome chest pain caused by coronary artery disease.<ref name=chack>{{cite journal|author= Samuel Chackalamannil|title=Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity|journal=]|year=2008|doi =10.1021/jm800180e|volume= 51|pages= 3061}}</ref> '''Vorapaxar''' (formerly SCH-530,348) is a ] receptor (]) antagonist based on the natural product ]. Discovered by ] and currently being developed by ], it is a experimental pharmaceutical treatment for acute coronary syndrome chest pain caused by coronary artery disease.<ref name=chack>{{cite journal|author= Samuel Chackalamannil|title=Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity|journal=]|year=2008|doi =10.1021/jm800180e|volume= 51|pages= 3061}}</ref>


In January 2010, clinical trials being conducted by Merck were halted for patients with stroke and mild heart conditions.<ref>, '']'', January 13, 2010</ref> Merck is uncertain whether further development of vorapaxar will continue. In January 2011, clinical trials being conducted by Merck were halted for patients with stroke and mild heart conditions.<ref>, '']'', January 13, 2011</ref> Merck is uncertain whether further development of vorapaxar will continue.


==References== ==References==

Revision as of 14:20, 14 January 2011

Pharmaceutical compound
Vorapaxar
Clinical data
Other namesSCH-530348
Identifiers
IUPAC name
  • Ethyl N-vinyl]-3-methyl-1-oxo-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzoisobenzofuran-7-yl]carbamate
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.116.767 Edit this at Wikidata
Chemical and physical data
FormulaC29H33FN2O4
Molar mass492.58 g/mol g·mol

Vorapaxar (formerly SCH-530,348) is a thrombin receptor (PAR-1) antagonist based on the natural product himbacine. Discovered by Schering-Plough and currently being developed by Merck & Co., it is a 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. Merck is uncertain whether further development of vorapaxar will continue.

References

  1. Samuel Chackalamannil (2008). "Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity". Journal of Medicinal Chemistry. 51: 3061. doi:10.1021/jm800180e.
  2. Merck Blood Thinner Studies Halted in Select Patients, Bloomberg News, January 13, 2011

External links


Antithrombotics (thrombolytics, anticoagulants and antiplatelet drugs) (B01)
Antiplatelet drugs
Glycoprotein IIb/IIIa inhibitors
ADP receptor/P2Y12 inhibitors
Prostaglandin analogue (PGI2)
COX inhibitors
Thromboxane inhibitors
Phosphodiesterase inhibitors
Other
Anticoagulants
Vitamin K antagonists
(inhibit II, VII, IX, X)
Factor Xa inhibitors
(with some II inhibition)
Heparin group/
glycosaminoglycans/
(bind antithrombin)
Direct Xa inhibitors ("xabans")
Direct thrombin (IIa) inhibitors
Other
Thrombolytic drugs/
fibrinolytics
Non-medicinal
Categories: