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oveporexton

Takeda

Approved in China on 22 Jul 2026 for adults and adolescents 16 and over — the first oral OX2R-selective agonist approved anywhere. Under Priority Review in the US and under review in Japan.

Breakthrough TherapyPriority ReviewSakigake

At a glance

Known asoveporexton · TAK-861 · ORZEYFUL
SponsorTakeda
MechanismOral selective orexin receptor 2 (OX2R) agonist
StageApproved
IndicationsNT1
Registered trials6 · 2 recruiting
Last verified4 Aug 2026
Approved
NT1

Where it stands

Oveporexton is the furthest-advanced drug in this class and the reason the class is being watched at all. It is Takeda's oral, selective orexin receptor 2 agonist, sold under the brand name ORZEYFUL, and on 22 July 2026 it became the first medicine of its kind approved anywhere when Chinese regulators cleared it for adults and adolescents aged 16 and over with narcolepsy type 1.

Two Phase 3 trials, FirstLight and RadiantLight, both met all primary and secondary endpoints. That is an unusually clean result for a central nervous system programme, where partial hits on secondary endpoints are the norm.

The applications in the United States and Japan are still pending. The US filing carries Priority Review, which shortens the FDA's review clock, and the programme has previously been granted Breakthrough Therapy designation in the US and Sakigake designation in Japan — both signals that regulators consider the unmet need serious and the early data strong.

Phase 3 FirstLight and RadiantLight both met all primary and secondary endpoints.

Registered trials

All 6 studies on ClinicalTrials.gov that name oveporexton or its development code, pulled from the registry on 4 Aug 2026.

Registry IDStudyPhaseStatusPrimary completion
NCT07363720 A Trial of TAK-861 for the Treatment of Narcolepsy With Cataplexy88 participants Phase 3 Recruiting 2 Oct 2026
NCT05816382 A Study of TAK-861 for the Treatment of Selected Central Hypersomnia Conditions500 participants Phase 2/Phase 3 Recruiting 28 Feb 2028
NCT06505031 A Study of TAK-861 in People With Narcolepsy Type 1105 participants Phase 3 Completed 4 Jun 2025
NCT06470828 A Study of TAK-861 for the Treatment of Narcolepsy Type 1168 participants Phase 3 Completed 3 Jun 2025
NCT05687903 A Study of TAK-861 in Participants With Narcolepsy Type 1112 participants Phase 2 Completed 14 Dec 2023
NCT05687916 A Study of TAK-861 in Participants With Narcolepsy Type 271 participants Phase 2 Completed 13 Dec 2023

Trial records are maintained by the sponsor and change without notice. Follow each link for current recruitment status and eligibility.

oveporexton — common questions

Is oveporexton approved?

Yes, in China. It was approved there on 22 July 2026 for adults and adolescents aged 16 and over with narcolepsy type 1, making it the first oral OX2R-selective agonist approved in any country. It is not yet approved in the United States or Japan, where applications remain under review.

When will the FDA decide on oveporexton?

The FDA accepted Takeda's New Drug Application with Priority Review on 10 February 2026 and set a PDUFA target date in the third quarter of 2026 without naming a specific day. As of Takeda's Q1 FY2026 earnings release on 30 July 2026 the application was still under review, with launch preparations underway for the second half of 2026.

What is oveporexton's brand name?

ORZEYFUL. That is the name under which it was approved in China. Brand names can differ by market, so the name used in the United States or Japan may not be the same if those applications are approved.

Did the oveporexton Phase 3 trials succeed?

Yes. The two pivotal Phase 3 studies, FirstLight and RadiantLight, each met all primary and secondary endpoints.

What else is oveporexton called?

Its development code is TAK-861 and its brand name in China is ORZEYFUL. All three names refer to the same compound.

How is oveporexton different from TAK-994?

TAK-994 was Takeda's earlier oral orexin agonist. It was stopped during Phase 2 after liver safety signals emerged. Oveporexton is the successor compound that Takeda carried forward instead.

The rest of the class

Compounds sharing at least one indication with oveporexton come first.

alixorexton

Alkermes plc · Phase 3 · NT1 / NT2 / IH

cleminorexton

Centessa Pharmaceuticals · Phase 3 · NT1 / NT2 / IH

E2086

Eisai Co. · Phase 2 · NT1

TAK-360

Takeda Pharmaceutical Company · Phase 2 · NT1 / NT2 / IH

ALKS 4510

Alkermes plc · Phase 1 · Fatigue in MS / Fatigue in Parkinson's

ALKS 7290

Alkermes plc · Phase 1 · ADHD

BP-205

Harmony Biosciences Holdings · Phase 1 · Not yet specified

ORX142

Centessa Pharmaceuticals · Phase 1 · Neurological / Neurodegenerative

ORX489

Centessa Pharmaceuticals · Phase 1 · Neuropsychiatric

Published evidence

Peer-reviewed papers reporting data on oveporexton. A sponsor announcement says what a company decided; a paper says what the data showed, and can be read by anyone. Papers about the orexin system as a whole rather than this compound are under research.

  1. Effects of oveporexton, an orexin receptor 2-selective agonist, on cognition in narcolepsy type 1: a secondary analysis of a randomized clinical trial

    Lammers GJ, Plazzi G, Mignot E, Pizza F, Dauvilliers Y, et al. · JAMA Neurology · 1 Feb 2026 · PMID 41359331

    Secondary analysis of the 112-patient Phase 2 trial. Oveporexton improved attention, memory and executive function against placebo across all four dose groups over eight weeks. Cognition was not a primary endpoint and is not part of any approved indication, so this is exploratory.

  2. Effects of an orexin receptor 2-selective agonist on salivary secretion in rats

    Ichishima J, Nakakariya M, Kimura H · Scientific Reports · 17 Mar 2026 · PMID 41844849

    Excess saliva is the side effect reported most often across this drug class, oveporexton included, and until this paper nobody had measured it directly. The authors dosed rats with OX-202, a different OX2R-selective agonist, and measured saliva against pilocarpine as a positive control. It is a rat study of a related compound rather than of oveporexton itself, so read it as a test of whether the mechanism causes the effect, not as a measurement of this drug. Open access.

Source

This entry was last checked against its primary source on 4 Aug 2026 by Simon Stawski: https://www.takeda.com/newsroom/newsreleases/2026/orzeyful-approved-china-narcolepsy/

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