Elinogrel

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Elinogrel
Elinogrel skeletal.svg
Systematic (IUPAC) name
N-[(5-chlorothiophen-2-yl)sulfonyl]-N'-{4-[6-fluoro-7-(methylamino)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl]phenyl}urea
Clinical data
Pregnancy cat.
  • N/A
Legal status
  • Investigational
Routes Oral, intravenous
Pharmacokinetic data
Metabolism Mainly unchanged, ca. 15% N-demethylation[1]
Excretion Urine, faeces
Identifiers
CAS number 936500-94-6
ATC code None
PubChem CID 16066663
UNII 915Y8E749J YesY
KEGG D09607
Synonyms PRT-060128
Chemical data
Formula C20H15ClFN5O5S2 
Mol. mass 523.945 g/mol

Elinogrel (INN,[2] USAN) was an experimental antiplatelet drug acting as a P2Y12 inhibitor. Similarly to ticagrelor and in contrast to clopidogrel, elinogrel was a reversible inhibitor that acted fast and short (for about 12 hours), and it was not a prodrug but pharmacologically active itself. The substance was used in form of its potassium salt, intravenously for acute treatment and orally for long-term treatment.[3] Development was terminated in 2012.

History[edit]

The substance was originally developed by Portola Pharmaceuticals, with Phase II clinical trials conducted around 2008–2011.[4] In February 2009, Novartis bought worldwide rights to develop it further, intending to conduct Phase III studies and commercialise the drug.[5] The development of the drug was terminated in January 2012 by Novartis.[6]

References[edit]

  1. ^ Siller-Matula, J. M.; Krumphuber, J.; Jilma, B. (2010). "Pharmacokinetic, pharmacodynamic and clinical profile of novel antiplatelet drugs targeting vascular diseases". British Journal of Pharmacology 159 (3): 502–517. doi:10.1111/j.1476-5381.2009.00555.x. PMC 2828016. PMID 20050853.  edit
  2. ^ International Nonproprietary Names for Pharmaceutical Substances (INN): Proposed INN List 101
  3. ^ Gurbel, P.A.; Kereiakes, D.; Tantry, U.S. (2010). "Elinogrel potassium". Drugs Fut 35 (11): 885. 
  4. ^ Michelson, A. D. (2011). "Advances in Antiplatelet Therapy". Hematology 2011: 62–69. doi:10.1182/asheducation-2011.1.62. PMID 22160013.  edit
  5. ^ Insciences: Novartis gains worldwide rights to elinogrel, a Phase II anti-clotting compound with potential to reduce risk of heart attack
  6. ^ BioPortfolio: Novartis drops elinogrel outright