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Abandoned drugs
Elinogrel
Другие языки:

Elinogrel

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Elinogrel
Elinogrel skeletal.svg
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
  • N-[(5-Chlorothiophen-2-yl)sulfonyl]-N′-{4-[6-fluoro-7-(methylamino)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl]phenyl}urea
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
Formula C20H15ClFN5O5S2
Molar mass 523.94 g·mol−1
3D model (JSmol)
  • 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=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.


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