RegulationPriority Review (United States), Breakthrough Therapy (United States), Orphan Drug (United States), Priority Review (China), Breakthrough Therapy (China), Orphan Drug (Japan), Orphan Drug (Australia), Priority Review (Australia)

Structure/Sequence

Molecular FormulaC23H25F5N2O4S

InChIKeyKVMGAIOTUIGROS-AZUAARDMSA-N

CAS Registry2460722-04-5

Clinical Trials associated with Oveporexton

NCT07363720

/ RecruitingPhase 3

A Double-blind, Placebo-Controlled, Randomized Withdrawal Trial to Evaluate the Efficacy and Safety of TAK-861 for the Treatment of Narcolepsy With Cataplexy (Narcolepsy Type 1)

The main aim of this study is to assess how effective TAK-861 is for treating narcolepsy type 1 and if this effect is maintained over time. Participants will take TAK-861 for a few months and if they meet certain criteria, they will be randomly assigned (by chance, like flipping a coin) to continue taking TAK-861 or take placebo (fake medicine) for up to 4 weeks to see if their narcolepsy symptoms return.

Start Date29 Jan 2026

Sponsor / Collaborator

Takeda Pharmaceutical Co., Ltd.

NCT06505031

/ CompletedPhase 3

A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of TAK-861 for the Treatment of Narcolepsy With Cataplexy (Narcolepsy Type 1)

The main aim of this study is to learn how effective TAK-861 is in improving excessive sleepiness during the day (called excessive daytime sleepiness or EDS) after 3 months of treatment. Other aims are to learn how effective TAK-861 is in lowering the number of sudden, unexpected attacks of muscle weakness while staying conscious (cataplexy) in a week; to learn the effect TAK-861 has on participants' ability to maintain attention, participant's overall quality of life, the spectrum of narcolepsy symptoms and daily life functions; and to learn about the safety of TAK-861.

Start Date08 Oct 2024

Sponsor / Collaborator

Takeda Pharmaceutical Co., Ltd.

NCT06470828

/ CompletedPhase 3

A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of TAK-861 for the Treatment of Narcolepsy With Cataplexy (Narcolepsy Type 1)

The main aim of this study is to learn how effective TAK-861 is in improving excessive sleepiness during the day (called excessive daytime sleepiness or EDS) after 3 months of treatment. Other aims are to learn how effective TAK-861 is in lowering the number of sudden, unexpected attacks of muscle weakness while staying conscious (cataplexy) in a week; to learn the effect TAK-861 has on participants' ability to maintain attention, participant's overall quality of life, the spectrum of narcolepsy symptoms, and daily life functions; and to learn about the safety of TAK-861.

Start Date02 Jul 2024

Sponsor / Collaborator

Takeda Pharmaceutical Co., Ltd.

100 Clinical Results associated with Oveporexton

100 Translational Medicine associated with Oveporexton

100 Patents (Medical) associated with Oveporexton

Literatures (Medical) associated with Oveporexton

01 Feb 2026·JAMA Neurology

Effects of Oveporexton, an Orexin Receptor 2–Selective Agonist, on Cognition in Narcolepsy Type 1

Article

Author: Barateau, Lucie ; Dauvilliers, Yves ; Mignot, Emmanuel ; Scammell, Thomas E. ; Latzman, Robert D. ; Harel, Brian T. ; Pizza, Fabio ; Volfson, Dmitri ; Khachadourian, Vahe ; Tanaka, Shinichiro ; Lammers, Gert Jan ; Plazzi, Giuseppe ; Olsson, Tina ; Naylor, Melissa ; Stukalin, Ellie ; Maruff, Paul

Importance:

Cognitive symptoms negatively impact people with narcolepsy type 1 (NT1). While the effects of orexin receptor 2 (OX2R) agonists have been explored on diagnostic features of the disorder (excessive daytime sleepiness and cataplexy), effects on cognitive symptoms are not characterized.

Objective:

To explore the effects of oveporexton, an oral OX2R-selective agonist, on cognition in people with NT1.

Design, Setting, and Participants:

This is a secondary analysis of the TAK-861-2001 phase 2, 8-week, parallel-group, double-blind, placebo-controlled randomized clinical trial, conducted from January 2023 to December 2023, with a 4-week follow-up period. TAK-861-2001 was a multicenter study conducted in clinical settings. Eligible participants were 18 to 70 years of age, with an International Classification of Sleep Disorders, Third Edition diagnosis of NT1. Data analysis was performed from July 2024 to July 2025.

Interventions:

Participants were randomized 1:1:1:1:1 to twice-daily oral oveporexton or matching placebo, dosed 3 hours apart, in dose groups of 0.5/0.5 mg, 2/2 mg, 2/5 mg, 7 mg/placebo, or placebo/placebo, for 8 weeks.

Main Outcomes and Measures:

Cognitive symptoms were assessed using the Psychomotor Vigilance Task (PVT) for attention, the Continuous Paired Associate Learning (CPAL) test for memory, and the One Back (ONB) test and International Digit Symbol Substitution Test–symbols (IDSST-s) for executive function.

Results:

Of 161 eligible individuals screened, 48 did not meet study inclusion criteria, 1 withdrew, and 112 were included in the study. Of 112 participants, mean (SD) age was 34.0 (11.5) years, and 58 participants (51.8%) were female. A total of 112 participants were randomized and received 1 or more doses of oveporexton (0.5/0.5 mg, n = 23; 2/2 mg, n = 21; 2/5 mg, n = 23; 7 mg, n = 23) or placebo (n = 22). Oveporexton improved attention, memory, and executive function over 8 weeks. Least-squares (LS) mean placebo-adjusted changes from baseline were −10.77 (95% CI, −16.74 to −4.79), −9.45 (95% CI, −15.66 to −3.24), −8.60 (95% CI, −14.84 to −2.36), and −8.69 (95% CI, −14.90 to −2.47) PVT lapses with 0.5/0.5 mg, 2/2 mg, 2/5 mg, and 7 mg/placebo doses, respectively. LS mean placebo-adjusted changes were −22.52 (95% CI, −34.95 to −10.10), −16.92 (95% CI, −30.12 to −3.71), −15.51 (95% CI, −28.82 to −2.21), and −17.59 (95% CI, −30.50 to −4.68) for CPAL errors; −0.05 (95% CI, −0.10 to −0.01), −0.07 (95% CI, −0.12 to −0.02), −0.07 (95% CI, −0.12 to −0.02), and −0.05 (95% CI, −0.10 to 0.00) units for ONB log10-transformed performance speed; and 4.72 (95% CI, −1.38 to 10.83), 7.33 (95% CI, 1.06-13.61), 7.85 (95% CI, 1.75-13.95), and 11.82 (95% CI, 5.75-17.89) for IDSST-s correct responses.

Conclusions and Relevance:

In this secondary analysis of the TAK-861-2001 randomized clinial trial, the OX2R agonist oveporexton improved NT1-associated cognitive symptoms in adults.

Trial Registration:

ClinicalTrials.gov Identifier: NCT05687903

01 Jan 2026·Annals of Medicine and Surgery

Orexin receptor 2 agonists: a pathophysiologic approach to narcolepsy type 1

Author: Siddiqui, Erum ; Mauhmoud, Abubakr ; Khan, Muhammad Saad ; Arif, Zainab ; Hujjat, Syeda Fadak Zahra

Narcolepsy type 1 (NT1) is a chronic neurological disorder characterized by excessive daytime sleepiness, cataplexy, and disturbed nocturnal sleep, resulting from the loss of hypothalamic neurons that produce orexin. Current therapies, including stimulants, antidepressants, and sodium oxybate, primarily offer symptomatic relief without addressing the underlying orexin deficiency and often have safety or adherence limitations. Orexin receptor 2 (OX2R) agonists represent a novel therapeutic strategy aimed at restoring physiological wakefulness by directly targeting the core neurochemical deficit. TAK-994, the first oral OX2R agonist, demonstrated remarkable efficacy in reducing cataplexy and improving wakefulness but was discontinued due to dose-dependent hepatotoxicity. TAK-861 (oveporexton), a next-generation OX2R agonist with improved structural properties, has shown encouraging Phase 2 results with comparable efficacy and a favorable safety profile, including minimal hepatic effects and once-daily dosing convenience. If validated in large-scale Phase 3 studies, TAK-861 could become the first disease-modifying therapy for NT1, representing a paradigm shift from symptomatic management to mechanism-based treatment. The ongoing development of OX2R agonists highlights a promising frontier in precision sleep medicine, offering renewed hope for patients by targeting orexin restoration.

01 Jul 2025·Nature Reviews Neurology

Benefits of oveporexton in narcolepsy type 1

Article

Author: Wood, Heather

News (Medical) associated with Oveporexton

13 May 2026

·www.fiercepharma.com

Takeda, slimming down for 'new era,' plots 4,500 layoffs in latest restructuring drive

The Japanese pharma is targeting 2026 revenues of 4.64 trillion Japanese yen ($29.4 billion). With a new CEO prepared to take the reins next month and three key launches on deck for 2026 and 2027, Takeda is ready to shake off the generic-related declines that have plagued revenues in recent years as it eyes a “new era” to be marked by growth acceleration, according to the Japanese pharma.However, several thousand employees won’t be entering the new chapter with the company. In its full-year earnings presentation (PDF) on May 13, Takeda filled in details on its 2026 “transformation program,” which looks to centralize corporate functions, reduce management layers and target process simplification. The multiyear slim-down is expected to hit about 4,500 roles during the 2026 fiscal year, resulting in about 170 billion Japanese yen ($1.07 billion) in restructuring costs and some 100 billion yen ($633 million) in gross savings for 2026, the company said. More than 200 billion yen ($1.26 billion) in annualized savings is projected by 2028. Takeda recently telegraphed a round of job reductions in the U.S, affecting 634 roles assigned to the company’s U.S. headquarters in Cambridge, Massachusetts, as part of the $1.26 billion efficiency drive. The latest restructuring comes on the heels of 2024-2025’s “enterprise-wide efficiency program,” which saw over 4,000 positions impacted over the two years, Takeda noted. Takeda’s cost-savings push began in 2024, as revenues for its blockbuster attention-deficit/hyperactivity disorder med Vyvanse rapidly declined in the face of generics swarming the market upon its patent expiration, a struggle that has haunted the organization since. With the company predicting last year that 2025 would be the last year of major generic headwinds to Vyvanse, Takeda is hoping that its three upcoming new launches will help put its Vyvanse-related sales woes in the rearview. In fiscal 2026, which ends in March 2027, the company anticipates full-year revenues of 4.64 trillion Japanese yen ($29.4 billion), reflecting “mature portfolio headwinds in a year that we pivot to new launches,” it explained in its presentation. The new launches include potential regulatory approvals for Takeda’s three leading late-stage assets in narcolepsy treatment oveporexton, polycythemia vera candidate rusfertide and psoriasis medicine zasocitinib. Oveporexton and rusfertide are both under priority review with the FDA and could see a U.S. commercial launch during the second half of 2026, while the company is making “decisive investments” to support a zasocitnib regulatory filing later this year. “We are very, very excited about these three launches, and we’re laser-focused on the execution,” CEO-Elect Julie Kim said on the company’s earnings conference call with investors. As the company zeroes in on transitioning to a “new cohort of blockbuster brands” that positions it for “long-term profitable growth and patient impact,” Kim said in a release, Takeda is outlining its metamorphosis in two phases. The first step, dubbed “Horizon One,” will see the company establish a trio of new growth drivers while ensuring the “resilience and competitiveness” of its core in-line brands. After that, “Horizon Two” will launch another wave of late-stage pipeline assets and maximize revenue from the first launches.Takeda enters its 2026 fiscal year with 684.5 billion yen ($4.3 billion) in free cash flow after collecting full-year 2025 revenues of 4.5 trillion yen ($28.3 billion) in a 1.7% year-over-year decline. Over half (51%) of the company’s yearly revenue came from its collection of growth and launch products, which includes blockbuster inflammatory bowel disease (IBD) drug Entyvio and hereditary angioedema (HAE) drug Takhzyro, among others. Put together, the selection of growth products spread across the company’s six key business areas together earned 2.3 trillion Japanese yen ($14.5 billion) over the year, which “partially mitigated” the continued impacts of Vyvanse’s generic erosion. Vyvanse and other products impacted by patent expirations saw a pooled sales decline of 43% over the year, the company noted in its presentation. Takeda’s full-year 2025 earnings conference call was the last under longtime CEO Christophe Weber, who took over the pharma in 2015 after a 20-year career at GSK. Weber was the first non-Japanese CEO in the company’s over 200-year history and was credited with “building Takeda into the company it is today,” Kim said on the call. Kim, who joined Takeda in 2019, had headed up the company’s U.S. operations since 2022 and was selected as CEO as part of a “thoughtful and intentional” succession process, Weber noted.

Executive ChangePriority Review

13 May 2026

·endpoints.news

Takeda to target 4,500 jobs as incoming CEO continues restructuring

Takeda will cut roughly 9% of its workforce over the next fiscal year as the next CEO puts her stamp on a yearslong restructuring. About 4,500 roles will be affected, the company said Wednesday in its fourth-quarter earnings presentation. That figure doesn’t account for hiring plans, including 2,200 roles that are currently open and new jobs that will be created throughout the year, a Takeda spokesperson told Endpoints News. No further details were shared about the timeline and which roles will be affected. Takeda is the latest biopharma to announce four-digit layoffs, following Novo Nordisk’s September 2025 decision to cut 9,000 jobs and Merck’s July announcement targeting 6,000 positions. Bayer CEO Bill Anderson confirmed this month that it’s made 14,000 reductions as part of a broader restructuring. Takeda’s outgoing CEO Christophe Weber laid out plans in 2024 to simplify the company’s structure, remove layers and broaden roles. Incoming CEO Julie Kim also cited efficiency as a priority as she prepares to take the reins in June. Going forward, Takeda said it would prioritize resources to advance its late-stage pipeline, including three products that Kim hopes will be blockbusters: the narcolepsy drug oveporexton, the blood cancer drug rusfertide, and a plaque psoriasis drug called zasocitinib. The FDA is currently mulling applications for oveporexton and rusfertide, with decisions expected in the third quarter of the calendar year. Meanwhile, Takeda made a handful of pipeline cuts last quarter, including a Phase 1 program for nausea and vomiting called TAK-004 and a Phase 2b program for the enzyme replacement therapy TAK-755 in immune thrombotic thrombocytopenic purpura. The Japanese pharma cited strategic reasons for both cuts. Takeda also returned the rights for a frontotemporal dementia candidate called TAK-594 to Denali after severing the partnership . The company is also discontinuing a booster program for its dengue vaccine Qdenga after data suggested additional dosing wasn’t needed for sustained protection.

VaccinePhase 2Phase 1

13 May 2026

·firstwordpharma.com

Takeda expands cost-cutting drive with 4500 roles on the line

Takeda was among the biggest pharma downsizers in the first quarter and had already warned that more cuts were coming.Now, the Japanese drugmaker has detailed a new "transformation programme" expected to affect roughly 4500 roles in fiscal 2026 as it looks to centralise corporate functions, trim management layers and simplify operations.The restructuring, unveiled during Takeda's quarterly earnings presentation on Wednesday, is projected to generate more than JPY 200 billion ($1.3 billion) in annualised savings by fiscal 2028. The company will book roughly JPY 170 billion in restructuring charges along the way, but expects to pocket around JPY 100 billion in savings this year alone.The move follows a steady stream of Takeda layoffs since it undertook an enterprise-wide restructuring programme about two years ago. Earlier this year, it disclosed plans to eliminate 634 positions in the US, including 247 jobs in Massachusetts and another 387 roles spread across other states.The cuts came less than six months after Takeda axed 137 jobs tied to its withdrawal from cell therapy development. Those reductions followed an even larger wave in 2024, when the company cut nearly 1000 positions in Massachusetts alone.'New era'"Based on my leadership team, we've updated the organisational structure to transform the company for accelerated speed and growth," said CEO-elect Julie Kim, who takes the reins from Christophe Weber in June, during the company's earnings call. "This has included reducing layers to bring teams closer to patients and customers, centralising and streamlining corporate functions, and driving greater efficiency through data, technology, and AI."Share added, "In addition to our Takeda executive team, our broader governance structure…provides a strong and stable foundation for this new era."Eye on trio of launchesTakeda said savings from the restructuring will be reinvested to help support a trio of upcoming launches; namely, oveporexton (TAK-861), which could hit the market in the second half as the first orexin agonist approved for narcolepsy type 1 if the FDA signs off on it in the third quarter; rusfertide, a potential first‑in‑class hepcidin mimetic for polycythemia vera that is also awaiting an FDA decision and possible launch next half; and zasocitinib, an oral TYK2 inhibitor for psoriasis that Takeda is planning to file this year for a possible commercial debut in the first half of 2027.Kim said that "the convergence of these catalysts offers a timely opportunity to lay out the path forward for our next chapter of growth," which will come in two stages.The first — referred to as "Horizon One" — has a two- three-year timeframe and centres on establishing oveporexton, rusfertide and zasocitinib as the company's growth drivers. "Horizon Two" will focus on accelerating that growth. This is where the company will be "shifting from our maturing portfolio to a new cohort of blockbuster brands…by scaling our first wave of launches while preparing for and executing the launch of our next wave of late-stage assets," Kim said.Pipeline pruningSome assets won't be going along for the ride, however. Takeda provided an update to its pipeline, including curtailing Phase I development of TAK-004 for nausea and vomiting "due to strategic consideration." The drug's fate mirrors that of a number of the company's nausea and vomiting candidates, such as TAK-105 and TAK-510, as well as TAK-906 in the associated condition of gastroparesis.The drugmaker also disclosed that it will stop Phase III work on the 5% formulation of TAK-961, also known as Glovenin-I, in autoimmune encephalitis. Takeda cited "portfolio/filing strategy" for the decision, noting that data on the formulation will support plans to seek approval of the 10% version of the immunoglobulin.The company also confirmed the removal of TAK-594 from its pipeline for frontotemporal dementia, having ended a co-development partnership with Denali Therapeutics earlier in the year.Looking ahead to the upcoming fiscal year ending March 2027, Takeda said it anticipates full-year revenues of JPY 4.64 trillion and profit of JPY 166 billion.-Matt Dennis contributed to this report.

Phase 1Drug ApprovalPhase 3Phase 2

100 Deals associated with Oveporexton

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Narcolepsy	NDA/BLA	China	Takeda Pharmaceutical Co., Ltd.	16 Jan 2026
Cataplexy	Phase 3	United States	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024
Cataplexy	Phase 3	Japan	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024
Cataplexy	Phase 3	Canada	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024
Cataplexy	Phase 3	France	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024
Cataplexy	Phase 3	Germany	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024
Cataplexy	Phase 3	Italy	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024
Cataplexy	Phase 3	Netherlands	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024
Cataplexy	Phase 3	Norway	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024
Cataplexy	Phase 3	Spain	Takeda Pharmaceutical Co., Ltd.	02 Jul 2024

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06470828 \| NCT06505031 (RadiantLight \| TAK-861-3002, Company_Website) Manual	Phase 3	Narcolepsy	273	安慰剂	-	Positive	08 Sep 2025
				Oveporexton	eyovrennoo(rqwormlwvk) = ttrolcwsnn rrdavqttpg (eqitmrklib ) Met
NCT06470828 \| NCT06505031 (RadiantLight \| TAK-861-3002, PRNewswire) Manual	Phase 3	Narcolepsy	-	TAK-861	eclbpuyaut(qztulmzmqk) = 相比安慰剂组均取得了具有统计学显著性的改善 hhknpohtqw (uiwniwzonu ) Met View more	Positive	16 Jul 2025
				安慰剂
NCT05687903 (TAK-861-2001, BusinessWire \| Pubmed) Manual	Phase 2	Narcolepsy	112	oveporexton twice-daily 0.5/0.5 mg	lyepykeyok(vxbmpwwzel) = xxjivhoezv tqhkwuqrkv (lhgxwkndip ) View more	Positive	14 May 2025
				oveporexton twice-daily 2/2 mg	lyepykeyok(vxbmpwwzel) = iodnxliuvx tqhkwuqrkv (lhgxwkndip ) View more
NCT05687903 (P12-4.002, AAN2025)	Phase 2	Narcolepsy low cerebrospinal fluid orexin levels	112	TAK-861 0.5mg BID	icmkyzzpdc(myzujktksa) = qceklngtbq dwsiyjymwj (glxxzxesrr )	Positive	07 Apr 2025
				TAK-861 2mg BID	icmkyzzpdc(myzujktksa) = lnatpaqifw dwsiyjymwj (glxxzxesrr )
NCT05687903 (TAK-861-2001 \| P12-4.002, CTgov)	Phase 2	Narcolepsy	112	Placebo (Placebo)	lsvkuvbcjd(toufcadlnd) = sbikgupsqt djapzwwple (xxfzavmopq, 2.061) View more	-	09 Jan 2025
				TAK-861 (TAK-861 0.5 mg BID)	lsvkuvbcjd(toufcadlnd) = otataaxmum djapzwwple (xxfzavmopq, 2.128) View more
NCT05687916 (CTgov)	Phase 2	Narcolepsy	71	Placebo (Placebo)	jihvgyukft(xcibxrajhh) = kjajmqcxer umjnayzyfw (wfrciocvgm, 2.246) View more	-	09 Jan 2025
				TAK-861 (TAK-861 2 mg and 5 mg)	jihvgyukft(xcibxrajhh) = wojtxktbmb umjnayzyfw (wfrciocvgm, 2.300) View more
NCT05687903 (TAK-861-2001, NEWS) Manual	Phase 2	Narcolepsy	112	TAK-861	xdobejvcyw(jvnkimryhq) = The primary endpoint demonstrated statistically significant and clinically meaningful increased sleep latency on the Maintenance of Wakefulness Test (MWT) versus placebo across all doses (LS mean difference versus placebo all p ≤0.001). Improvements were sustained over 8 weeks. Mean sleep latency ranged from 16.5 minutes for the lowest 0.5mg/0.5mg dose up to 30.7 minutes for the 2mg/5mg dose, compared to just 7 minutes for placebo. dmdycvncvz (ptcnbvxnme ) View more	Positive	03 Jun 2024
				placebo
WSC2023	Not Applicable	Sleep Disorders, Circadian Rhythm	-	TAK-861 high-dose (HD)	jdswyjbrji(hmrpubnsxw) = reported by 3 (27.3%) subjects on TAK‑861 HD eoqngoajtu (ucnapyvqwz )	-	23 Oct 2023
				TAK-861 low-dose (LD)

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