Elinogrel
Chemical compound
- None
- Development terminated
- N-[(5-Chlorothiophen-2-yl)sulfonyl]-N′-{4-[6-fluoro-7-(methylamino)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl]phenyl}urea
- 936500-94-6
- 16066663
- 17226246
- 915Y8E749J
- D09607
- DTXSID50918262
- Interactive image
- CNC1=C(C=C2C(=C1)NC(=O)N(C2=O)C3=CC=C(C=C3)NC(=O)NS(=O)(=O)C4=CC=C(S4)Cl)F
InChI
- InChI=1S/C20H15ClFN5O5S2/c1-23-15-9-14-12(8-13(15)22)18(28)27(20(30)25-14)11-4-2-10(3-5-11)24-19(29)26-34(31,32)17-7-6-16(21)33-17/h2-9,23H,1H3,(H,25,30)(H2,24,26,29)
- Key:LGSDFTPAICUONK-UHFFFAOYSA-N
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
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
- ^ Siller-Matula JM, Krumphuber J, Jilma B (February 2010). "Pharmacokinetic, pharmacodynamic and clinical profile of novel antiplatelet drugs targeting vascular diseases". British Journal of Pharmacology. 159 (3): 502–17. doi:10.1111/j.1476-5381.2009.00555.x. PMC 2828016. PMID 20050853.
- ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 63" (PDF). World Health Organization. pp. 50–1. Retrieved 1 December 2016.
- ^ Gurbel PA, Kereiakes D, Tantry US (November 2010). "Elinogrel potassium: Receptor antagonist antiplatelet therapy". Drugs of the Future. 35 (11): 885–92. doi:10.1358/dof.2010.35.11.1529823. S2CID 79785538.
- ^ Michelson AD (2011). "Advances in antiplatelet therapy". Hematology. American Society of Hematology. Education Program. 2011: 62–9. doi:10.1182/asheducation-2011.1.62. PMID 22160013.
- ^ "Novartis gains worldwide rights to elinogrel, a Phase II anti-clotting compound with potential to reduce risk of heart attack". Insciences. Archived from the original on 2014-07-14.
- ^ "Novartis drops elinogrel outright". BioPortfolio. Archived from the original on 2012-07-29.
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| Glycoprotein IIb/IIIa inhibitors |
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fibrinolytics
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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