Drug intelligence / Profile preview

oveporexton

Development stage
Discontinued
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Oveporexton is Takeda's investigational **oral small-molecule orexin receptor 2 selective agonist** being developed primarily for **narcolepsy type 1**. It is designed to restore deficient orexin signaling, the core pathophysiology of narcolepsy type 1, by selectively stimulating the orexin receptor 2 pathway to improve wakefulness and reduce REM-sleep related phenomena such as cataplexy. Publicly reported Phase 2b data and subsequent Phase 3 FirstLight and RadiantLight studies showed statistically significant and clinically meaningful improvements in excessive daytime sleepiness, wakefulness, cataplexy, symptom severity, quality of life, attention, and daily functioning, with insomnia and urinary urgency/frequency among the most commonly reported adverse events. Takeda has described oveporexton as a potential first-in-class therapy and indicated plans for regulatory submissions following positive Phase 3 results.

Brand names
Orzeyful
Other names
n-[(2s,3r)-2-[[3-(3,5-difluorophenyl)-2-fluorophenyl]methyl]-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]ethanesulfonamide2460722-04-5
02

Targets

HCRTR2 (Orexin/hypocretin receptor type 2)

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