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Elinogrel

Clinical data
Other names	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
Excretion	Urine, faeces
Identifiers
IUPAC name N--N′-{4-phenyl}urea
CAS Number	936500-94-6
PubChem CID	16066663
ChemSpider	17226246
UNII	915Y8E749J
KEGG	D09607
CompTox Dashboard (EPA)	DTXSID50918262
Chemical and physical data
Formula	C20H15ClFN5O5S2
Molar mass	523.94 g·mol
3D model (JSmol)	Interactive image
SMILES 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, 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. Development was terminated in 2012.

History

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

References

1. 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.
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 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.
4. 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.
5. "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.
6. "Novartis drops elinogrel outright". BioPortfolio. Archived from the original on 2012-07-29.

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