Casopitant
- A04AD13 (WHO)
- (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
- 414910-27-3
- 23725089
- 25069049
- 3B03KPM27L
- D06574
- ChEMBL2107320
- DTXSID40961762
- Interactive image
- 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
- InChI=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
- Key:XGGTZCKQRWXCHW-JRLVAEJTSA-N
Casopitant (INNTooltip International Nonproprietary Name),[1]: 208 former tentative trade names Rezonic (U.S.) and Zunrisa (Europe), is an NK1 receptor antagonist which was undergoing research for the treatment of chemotherapy-induced nausea and vomiting.[2][3] It was under development by GlaxoSmithKline.[2] In July 2008, the company filed a marketing authorisation application with the European Medicines Agency. The application was withdrawn and development was discontinued in September 2009 because GlaxoSmithKline decided that further safety assessment was necessary.[2][4] However, a 2022 review listed casopitant as under development as a potential novel antidepressant for the treatment of major depressive disorder, with a phase 2 clinical trial having been completed.[5]
References
- ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List56" (PDF). World Health Organization. 2006. Retrieved 17 November 2016.
- ^ a b c Name, Drug (25 December 2021). "Casopitant". AdisInsight. Retrieved 21 August 2022.
- ^ Lohr L (2008). "Chemotherapy-induced nausea and vomiting". Cancer Journal. 14 (2): 85–93. doi:10.1097/PPO.0b013e31816a0f07. PMID 18391612. S2CID 43224257.
- ^ "GlaxoSmithKline withdraws its marketing authorisation application for Zunrisa" (PDF). London: EMEA. 13 October 2009. Archived from the original (PDF) on 15 October 2009. Retrieved 21 December 2009.
- ^ Sakurai H, Yonezawa K, Tani H, Mimura M, Bauer M, Uchida H (July 2022). "Novel Antidepressants in the Pipeline (Phase II and III): A Systematic Review of the US Clinical Trials Registry". Pharmacopsychiatry. 55 (4): 193–202. doi:10.1055/a-1714-9097. PMC 9259184. PMID 35045580.
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- Agonists: Substance P
- Antagonists: Aprepitant
- Befetupitant
- Burapitant
- Casopitant
- CI-1021
- CP-96345
- CP-99994
- CP-122721
- Dapitant
- Elinzanetant
- Ezlopitant
- Figopitant
- FK-888
- Fosaprepitant
- Fosnetupitant
- GR-203040
- GW-597599
- HSP-117
- L-733,060
- L-741,671
- L-743,310
- L-758,298
- Lanepitant
- LY-306740
- Maropitant
- Netupitant
- NKP-608
- Nolpitantium besilate
- Orvepitant
- Rolapitant
- RP-67580
- SDZ NKT 343
- Serlopitant
- T-2328
- Telmapitant
- Tradipitant
- Vestipitant
- Vofopitant
- Agonists: Neurokinin A
- Antagonists: GR-159897
- Ibodutant
- Nepadutant
- Saredutant
- Agonists: Neurokinin B
- Senktide
- Antagonists: Elinzanetant
- Fezolinetant
- Osanetant
- Pavinetant
- SB-218,795
- SB-222,200
- Talnetant
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