Oveporexton

Pharmaceutical compound From Wikipedia, the free encyclopedia

Oveporexton (INNTooltip 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]

Other namesTAK-861; TAK861
Routes of
administrationOral[1][2]
Drug classOrexin OX2 receptor agonist; Wakefulness-promoting agent
CAS Number
Quick facts Clinical data, Other names ...
Oveporexton
Clinical data
Other namesTAK-861; TAK861
Routes of
administration		Oral[1][2]
Drug classOrexin OX2 receptor agonist; Wakefulness-promoting agent
Identifiers
  • N-[(2S,3R)-2-[[3-(3,5-difluorophenyl)-2-fluorophenyl]methyl]-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]ethanesulfonamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC23H25F5N2O4S
Molar mass520.52 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
Close

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 submitted a New Drug Application (NDA) of oveporexton for the treatment of narcolepsy to the United States Food and Drug Administration (FDA) in February 2026.[1][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

Related Articles

Wikiwand AI