Oveporexton

Oveporexton
Clinical data
Other names	TAK-861; TAK861
Routes of; administration	Oral
Drug class	Orexin OX2 receptor agonist; Wakefulness-promoting agent
Identifiers
	IUPAC name 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	2460722-04-5;
PubChem CID	154617563;
ChemSpider	130299567;
UNII	59MF6P2ATF;
KEGG	D13223;
Chemical and physical data
Formula	C23H25F5N2O4S
Molar mass	520.52 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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 (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. It is taken by mouth.

The drug acts as a selective agonist of the orexin OX₂ receptor. It has wakefulness-promoting effects in animals, including in rodents and monkeys. In addition, oveporexton has been found to be effective in the treatment of narcolepsy and cataplexy in phase 3 clinical trials in humans. 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.

Oveporexton is being developed by Takeda. 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. 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. 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.