Cannabaceae

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Elinogrel
Clinical data
Other namesPRT-060128
Routes of
administration		By mouth, IV
ATC code
  • None
Legal status
Legal status
  • Development terminated
Pharmacokinetic data
MetabolismMainly unchanged, ~15% N-demethylation[1]
ExcretionUrine, 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
FormulaC20H15ClFN5O5S2
Molar mass523.94 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,[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 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.
source: https://en.wikipedia.org/wiki/Elinogrel

One thought on “Cannabaceae”

  1. Well, that’s interesting to know that Psilotum nudum are known as whisk ferns. Psilotum nudum is the commoner species of the two. While the P. flaccidum is a rare species and is found in the tropical islands. Both the species are usually epiphytic in habit and grow upon tree ferns. These species may also be terrestrial and grow in humus or in the crevices of the rocks.
    View the detailed Guide of Psilotum nudum: Detailed Study Of Psilotum Nudum (Whisk Fern), Classification, Anatomy, Reproduction

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