Elinogrel

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Elinogrel
Elinogrel skeletal.svg
Clinical data
Synonyms PRT-060128
Routes of
administration
By mouth, IV
ATC code
  • None
Legal status
Legal status
  • Development terminated
Pharmacokinetic data
Metabolism Mainly unchanged, ~15% N-demethylation[1]
Excretion Urine, faeces
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
Formula C20H15ClFN5O5S2
Molar mass 523.945 g/mol
3D model (JSmol)

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. PMC 2828016Freely accessible. PMID 20050853. doi:10.1111/j.1476-5381.2009.00555.x. 
  2. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 63" (PDF). World Health Organization. pp. 50–1. Retrieved 1 December 2016. 
  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. PMID 22160013. doi:10.1182/asheducation-2011.1.62. 
  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