词条 | Casopitant |
释义 |
| Watchedfields = changed | verifiedrevid = 447887505 | IUPAC_name = (2S,4S)-4-(4-Acetyl-1-piperazinyl)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methyl-1-piperidinecarboxamide | image = Casopitant.svg | width = 275 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | bioavailability = | protein_bound = | metabolism = | excretion = | CAS_number = 414910-27-3 | CAS_supplemental = | ATC_prefix = A04 | ATC_suffix = AD13 | PubChem = 23725089 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChEMBL = 2107320 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 3B03KPM27L | ChemSpiderID = 25069049 | KEGG = D06574 | C=30 | H=35 | F=7 | N=4 | O=2 | molecular_weight = 616.26 g/mol | smiles = CC1=C(C=CC(=C1)F)[C@@H]2C[C@H](CCN2C(=O)N(C)[C@H](C)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)N4CCN(CC4)C(=O)C | StdInChI = 1S/C30H35F7N4O2/c1-18-13-24(31)5-6-26(18)27-17-25(40-11-9-39(10-12-40)20(3)42)7-8-41(27)28(43)38(4)19(2)21-14-22(29(32,33)34)16-23(15-21)30(35,36)37/h5-6,13-16,19,25,27H,7-12,17H2,1-4H3/t19-,25-,27+/m1/s1 | StdInChIKey = XGGTZCKQRWXCHW-JRLVAEJTSA-N | synonyms = (2R,4S)-4-(4-Acetylpiperazin-1-yl)-N(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl2-(4-fluoro-2-methylphenyl)-N-methylpiperidine-1-carboxamide }} Casopitant (INN,[1]{{rp|208}} tentative trade names Rezonic (U.S.), Zunrisa (Europe)) is a neurokinin 1 receptor (NK1R) antagonist undergoing research for the treatment of chemotherapy-induced nausea and vomiting (CINV).[2] It is currently under development by GlaxoSmithKline (GSK). In July 2008, the company filed a marketing authorisation application with the European Medicines Agency. The application was withdrawn in September 2009 because GSK decided that further safety assessment was necessary.[3] See also{{div col|colwidth=30em}}
References1. ^{{cite web | title = International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List56 | url = http://www.who.int/medicines/publications/druginformation/innlists/RL56.pdf | publisher = World Health Organization | accessdate = 17 November 2016 | date = 2006}} {{Antiemetics and antinauseants}}{{Antidepressants}}{{Anxiolytics}}{{Neurokinin receptor modulators}}{{gastrointestinal-drug-stub}}{{nervous-system-drug-stub}}2. ^{{cite journal |author=Lohr L |title=Chemotherapy-induced nausea and vomiting |journal=Cancer J |volume=14 |issue=2 |pages=85–93 |year=2008 |pmid=18391612 |doi=10.1097/PPO.0b013e31816a0f07 |url=}} 3. ^{{cite web|url=http://www.emea.europa.eu/humandocs/PDFs/EPAR/zunrisa/63959809en.pdf |title=GlaxoSmithKline withdraws its marketing authorisation application for Zunrisa |date=13 October 2009 |publisher=EMEA |accessdate=21 December 2009 |location=London }}{{dead link|date=November 2016 |bot=InternetArchiveBot |fix-attempted=yes }} 8 : Abandoned drugs|Antiemetics|NK1 receptor antagonists|Acetamides|Piperazines|Piperidines|Trifluoromethyl compounds|Fluoroarenes |
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