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词条 Casopitant
释义

  1. See also

  2. References

{{Drugbox
| 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 The application was withdrawn in September 2009 because GSK decided that further safety assessment was necessary.[3]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}}
  • NK1 receptor antagonist
  • Aprepitant
  • Fosaprepitant
  • L-733,060
  • Maropitant
  • Vestipitant
{{div col end}}

References

1. ^{{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}}
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 }}
{{Antiemetics and antinauseants}}{{Antidepressants}}{{Anxiolytics}}{{Neurokinin receptor modulators}}{{gastrointestinal-drug-stub}}{{nervous-system-drug-stub}}

8 : Abandoned drugs|Antiemetics|NK1 receptor antagonists|Acetamides|Piperazines|Piperidines|Trifluoromethyl compounds|Fluoroarenes

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