Oveporexton

Last updated

Oveporexton
Oveporexton.svg
Clinical data
Other namesTAK-861; TAK861
Routes of
administration 		Oral [1] [2]
Drug class Orexin OX2 receptor agonist; Wakefulness-promoting agent
Identifiers
  • N-[(2S,3R)-2-{{#parsoidfragment:2}}3-(3,5-difluorophenyl)-2-fluorophenyl]methyl]-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]ethanesulfonamide
CAS Number
PubChem CID
UNII
Chemical and physical data
Formula C23H25F5N2O4S
Molar mass 520.52 g·mol−1
3D model (JSmol)
  • CCS(=O)(=O)N[C@@H]1[C@@H](N(CC1(F)F)C(=O)C(C)(C)O)CC2=C(C(=CC=C2)C3=CC(=CC(=C3)F)F)F
  • InChI=1S/C23H25F5N2O4S/c1-4-35(33,34)29-20-18(30(12-23(20,27)28)21(31)22(2,3)32)10-13-6-5-7-17(19(13)26)14-8-15(24)11-16(25)9-14/h5-9,11,18,20,29,32H,4,10,12H2,1-3H3/t18-,20+/m0/s1
  • Key:KVMGAIOTUIGROS-AZUAARDMSA-N

Oveporexton (INN Tooltip International Nonproprietary Name; developmental code name TAK-861) is an orexin receptor agonist and wakefulness-promoting agent which is under development for the treatment of narcolepsy (types 1 and 2) and idiopathic hypersomnia. [1] [2] [3] It is taken by mouth. [1] [2]

The drug acts as a selective agonist of the orexin OX2 receptor. [1] [2] It has wakefulness-promoting effects in animals, including in rodents and monkeys. [2] In addition, oveporexton has been found to be effective in the treatment of narcolepsy and cataplexy in phase 3 clinical trials in humans. [4] [5] [6] The drug is a first-in-class medication and targets the root symptomatic cause of narcolepsy (type 1) by remediating the orexin (hypocretin) deficiency that is present in the condition. [7] [8] [9]

Oveporexton is being developed by Takeda. [1] As of July 2025, it has completed phase 3 clinical trials for treatment of narcolepsy, whereas no recent development has been reported for treatment of idiopathic hypersomnia. [1] [5] [10] Takeda plans to submit a New Drug Application (NDA) of oveporexton for the treatment of narcolepsy to the United States Food and Drug Administration (FDA) in 2025. [5] Oveporexton is a follow-on and replacement compound for Takeda's earlier lead drug danavorexton (TAK-925), which is administered intravenously and stopped being developed due to unexpected liver toxicity findings. [10]

See also

References

  1. 1 2 3 4 5 6 "Oveporexton". AdisInsight. 16 December 2024. Retrieved 26 February 2025.
  2. 1 2 3 4 5 Mitsukawa K, Terada M, Yamada R, Monjo T, Hiyoshi T, Nakakariya M, et al. (September 2024). "TAK-861, a potent, orally available orexin receptor 2-selective agonist, produces wakefulness in monkeys and improves narcolepsy-like phenotypes in mouse models". Scientific Reports. 14 (1) 20838. Bibcode:2024NatSR..1420838M. doi:10.1038/s41598-024-70594-1. PMC   11379823 . PMID   39242684.
  3. ↑ Kallweit MS, Kallweit NP, Kallweit U (29 November 2023). "Pharmacological Treatments of Sleep–Wake Disorders: Update 2023". Clinical and Translational Neuroscience. 7 (4): 42. doi: 10.3390/ctn7040042 . ISSN   2514-183X.
  4. ↑ Walters J (7 October 2025). "Positive Data Presentation on Oveporexton for Narcolepsy". Psychiatric Times. Retrieved 7 October 2025.
  5. 1 2 3 Beaney A (14 July 2025). "Takeda's oral narcolepsy drug shines in two Phase III trials". Clinical Trials Arena. Retrieved 7 October 2025.
  6. ↑ Dauvilliers Y, Plazzi G, Mignot E, Lammers GJ, Del Río Villegas R, Khatami R, et al. (May 2025). "Oveporexton, an Oral Orexin Receptor 2-Selective Agonist, in Narcolepsy Type 1". The New England Journal of Medicine. 392 (19): 1905–1916. doi:10.1056/NEJMoa2405847. PMID   40367374.{{cite journal}}: CS1 maint: overridden setting (link)
  7. ↑ Abad VC (2023). "Pharmacological options for narcolepsy: are they the way forward?". Expert Rev Neurother. 23 (9): 819–834. doi:10.1080/14737175.2023.2249234. PMID   37585269.
  8. ↑ Matsuyama K (8 September 2025). "Takeda Nears First Therapy for Narcolepsy's Root Cause". Bloomberg.com. Archived from the original on 8 September 2025. Retrieved 7 October 2025.
  9. ↑ Vinluan F (9 September 2025). "Takeda Is Waking Up the Narcolepsy Market With First-in-Class Drug, But Alkermes Is on Its Heels". MedCity News. Retrieved 7 October 2025.
  10. 1 2 Mullard A (September 2025). "Leading orexin receptor agonist clears phase III for narcolepsy". Nat Rev Drug Discov. 24 (9): 655. doi:10.1038/d41573-025-00137-4. PMID   40775090.
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