Elinogrel
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| Clinical data | |
|---|---|
| Routes of administration |
By mouth, IV |
| ATC code | None |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Metabolism | Mainly unchanged, ~15% N-demethylation[1] |
| Excretion | Urine, faeces |
| Identifiers | |
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| Synonyms | PRT-060128 |
| CAS Number | 936500-94-6 |
| PubChem (CID) | 16066663 |
| ChemSpider | 17226246 |
| UNII | 915Y8E749J  |
| KEGG | D09607 |
| Chemical and physical data | |
| Formula | C20H15ClFN5O5S2 |
| Molar mass | 523.945 g/mol |
| 3D model (Jmol) | Interactive image |
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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]
- ^ 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. - ^ "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, P.A.; Kereiakes, D.; Tantry, U.S. (2010). "Elinogrel potassium". Drugs Fut. 35 (11): 885.
- ^ Michelson, A. D. (2011). "Advances in Antiplatelet Therapy". Hematology. 2011: 62–69. doi:10.1182/asheducation-2011.1.62. PMID 22160013.
- ^ Insciences: Novartis gains worldwide rights to elinogrel, a Phase II anti-clotting compound with potential to reduce risk of heart attack
- ^ BioPortfolio: Novartis drops elinogrel outright
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