| 词条 | Elinogrel |
| 释义 |
| IUPAC_name = N-[(5-Chlorothiophen-2-yl)sulfonyl]-N′- | image = Elinogrel skeletal.svg | width = 275 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Development terminated | routes_of_administration = By mouth, IV | bioavailability = | protein_bound = | metabolism = Mainly unchanged, ~15% N-demethylation[1] | elimination_half-life = | excretion = Urine, faeces | CAS_number = 936500-94-6 | ATC_prefix = None | ATC_suffix = | ATC_supplemental = | PubChem = 16066663 | DrugBank = | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 915Y8E749J | KEGG = D09607 | synonyms = PRT-060128 | ChemSpiderID = 17226246 | chemical_formula = | C=20 | H=15 | Cl=1 | F=1 | N=5 | O=5 | S=2 | molecular_weight = 523.945 g/mol | 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 | StdInChI = 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) | StdInChIKey = 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. HistoryThe 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] References1. ^{{Cite journal | last1 = Siller-Matula | first1 = J. M. | last2 = Krumphuber | first2 = J. | last3 = Jilma | first3 = B. | doi = 10.1111/j.1476-5381.2009.00555.x | title = Pharmacokinetic, pharmacodynamic and clinical profile of novel antiplatelet drugs targeting vascular diseases | journal = British Journal of Pharmacology | volume = 159 | issue = 3 | pages = 502–517 | year = 2010 | pmid = 20050853 | pmc =2828016 }} {{Antithrombotics}}{{Purinergics}}{{blood-drug-stub}}2. ^{{cite web | title = International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 63 | url = http://www.who.int/medicines/publications/druginformation/innlists/RL63.pdf | publisher = World Health Organization | accessdate = 1 December 2016 | pages = 50–1}} 3. ^{{cite journal|journal=Drugs Fut|title=Elinogrel potassium|last1=Gurbel|first1=P.A.|last2=Kereiakes|first2=D.|last3=Tantry|first3=U.S.|year=2010|volume=35|issue=11|page=885}} 4. ^{{Cite journal | last1 = Michelson | first1 = A. D. | doi = 10.1182/asheducation-2011.1.62 | title = Advances in Antiplatelet Therapy | journal = Hematology | volume = 2011 | pages = 62–69 | year = 2011 | pmid = 22160013 | pmc = }} 5. ^Insciences: Novartis gains worldwide rights to elinogrel, a Phase II anti-clotting compound with potential to reduce risk of heart attack 6. ^BioPortfolio: Novartis drops elinogrel outright 2 : Abandoned drugs|ADP receptor inhibitors |
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