Chemistry:Firazorexton
From HandWiki
Short description: Chemical compound
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| Other names | TAK-994 |
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| Formula | C22H25F3N2O4S |
| Molar mass | 470.51 g·mol−1 |
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Firazorexton (INN; development code TAK-994) is an experimental orexin 2 (OX2) receptor agonist first described in a 2019 patent filed by Takeda Pharmaceutical Company.[1][2]
Firazorexton was studied by Takeda for the treatment of narcolepsy.[3][4][5] It is a small-molecule and orally active compound and acts as a highly selective agonist of the orexin receptor 2 (OX2) with >700-fold selectivity over the orexin receptor 1 (OX1).[3][4][6][7] Firazorexton is related to danavorexton (TAK-925).[8] The compound reached phase 2 clinical trials for narcolepsy.[9] However, clinical development was discontinued in October 2021 for safety reasons.[8][10][11][12][13]
See also
References
- ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN)". WHO Drug Information 34 (1): 93–269. 2020. https://www.who.int/medicines/publications/druginformation/issues/INN_List-123.pdf. "Proposed INN: List 123".
- ↑ Kajita Y, Mikami S, Miyanohana Y, Koike T, Daini M, Oyabu N, Ogino M, Takeuchi K, Ito Y, Tokunaga N, Sugimoto T, Miyazaki T, Oda T, Hoashi Y, Hattori Y, Imamura K, "Heterocyclic compound and use therof", WO patent application 2019027058, published 2019-02-07
- ↑ 3.0 3.1 "0141 A Novel, Orally Available Orexin 2 Receptor-Selective Agonist, TAK-994, Shows Wake-Promoting Effects Following Chronic Dosing in an Orexin-Deficient Narcolepsy Mouse Model". Sleep 43 (Supplement 1): A56. April 2020. doi:10.1093/sleep/zsaa056.139. ISSN 0161-8105.
- ↑ 4.0 4.1 "Recently Approved and Upcoming Treatments for Narcolepsy". CNS Drugs 34 (1): 9–27. January 2020. doi:10.1007/s40263-019-00689-1. PMID 31953791.
- ↑ "TAK-994, a Novel Orally Available Brain-Penetrant Orexin 2 Receptor-Selective Agonist, Suppresses Fragmentation of Wakefulness and Cataplexy-Like Episodes in Mouse Models of Narcolepsy". The Journal of Pharmacology and Experimental Therapeutics 385 (3): 193–204. June 2023. doi:10.1124/jpet.122.001449. PMID 37001988.
- ↑ "Discovery of Arylsulfonamides as Dual Orexin Receptor Agonists". Journal of Medicinal Chemistry 64 (12): 8806–8825. June 2021. doi:10.1021/acs.jmedchem.1c00841. PMID 34101446.
- ↑ "How treatable is narcolepsy with current pharmacotherapy and what does the future hold?". Expert Opinion on Pharmacotherapy 22 (12): 1517–1520. August 2021. doi:10.1080/14656566.2021.1915987. PMID 33882765.
- ↑ 8.0 8.1 "Hypocretins (orexins): The ultimate translational neuropeptides". Journal of Internal Medicine 291 (5): 533–556. May 2022. doi:10.1111/joim.13406. PMID 35043499.
- ↑ Clinical trial number NCT04096560 for "A Study of TAK-994 in Adults With Type 1 and Type 2 Narcolepsy" at ClinicalTrials.gov
- ↑ "Takeda Provides Update on TAK-994 Clinical Program". Business Wire. 5 October 2021. https://www.businesswire.com/news/home/20211005006237/en/Takeda-Provides-Update-on-TAK-994-Clinical-Program.
- ↑ "Takeda pauses TAK-994 clinical studies due to safety glitch". The Pharma Letter. 6 October 2021. https://www.thepharmaletter.com/article/takeda-pauses-tak-994-clinical-studies-due-to-safety-glitch.
- ↑ "Takeda Halts Phase II Studies For Key R&D Asset TAK-994 In Narcolepsy". Scrip. Informa Pharma Intelligence. 6 October 2021. https://scrip.pharmaintelligence.informa.com/SC145192/Takeda-Halts-Phase-II-Studies-For-Key-RD-Asset-TAK994-In-Narcolepsy.
- ↑ "Takeda flashes red light on 'breakthrough' narcolepsy drug after PhII trials turned up mysterious safety signal". Endpoints News. 6 October 2021. https://endpts.com/takeda-flashes-red-light-on-narcolepsy-drug-after-phii-trials-turned-up-mysterious-safety-signal/.
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