Danavorexton(Danavorexton) - 药物靶点：OX2R_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Danavorexton、TAK 925、TAK-925

+ [1]

靶点

OX2R

作用方式

激动剂

作用机制

OX2R激动剂(食欲素受体2激动剂)

治疗领域

神经系统疾病呼吸系统疾病其他疾病

在研适应症-

非在研适应症

白天过度嗜睡特发性睡眠过度发作性睡病+ [1]

原研机构

Takeda Pharmaceutical Co., Ltd.

在研机构-

非在研机构

Millennium Pharmaceuticals, Inc.

Takeda Pharmaceutical Co., Ltd.

权益机构-

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C21H32N2O5S

InChIKeyUXZAJSZFFARTEI-YRPNKDGESA-N

CAS号2114324-48-8

关联

10

项与 Danavorexton 相关的临床试验

NCT05814016

/ Terminated临床2期

A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety, Tolerability, Efficacy, Pharmacokinetics, and Pharmacodynamics of a Single Intravenous Infusion of Danavorexton in Participants With Moderate to Severe Obstructive Sleep Apnea Undergoing General Anesthesia for Abdominal Surgery

The main aim is to see if danavorexton can help improve people's breathing in the recovery room after abdominal surgery.

开始日期2023-05-11

申办/合作机构

Takeda Pharmaceutical Co., Ltd.

NL-OMON52033

/ CompletedN/A

A Randomized, Double-Blind, Placebo-Controlled, 2-Way Crossover, Phase 1 Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Danavorexton in Healthy Subjects Undergoing Opioid-Induced Respiratory Depression - Takeda - TAK-925-1021 Study

开始日期2022-03-15

申办/合作机构

Takeda Pharmaceutical Co., Ltd.

NCT05180890

/ Completed临床1期

A Phase 1b, Randomized, Double-Blind, Placebo-Controlled, 3-Period Crossover Study to Evaluate the Safety, Tolerability, Pharmacodynamic, and Pharmacokinetic Effects of Overnight Intravenous TAK-925 in Patients With Obstructive Sleep Apnea

The main aim of the study is to check the side effects from overnight treatment with danavorexton and assess the tolerability of varying doses of danavorexton administered intravenously.
Before starting treatment with danavorexton, participants will keep a sleep diary and use an under-mattress sensor for at least 7 nights to check regular sleep habits.
There will be 3 Treatment Period up to 14 days apart. In each Treatment Period, participants will receive an intravenous (through the vein) infusion of either danavorexton or a placebo starting in the evening and continuing over a 10-hour period. A placebo looks exactly like danavorexton but does not have any medicine in it.
Participants will take part in a follow-up phone appointment about a week after the last Treatment Period.

开始日期2022-03-10

申办/合作机构

Takeda Pharmaceutical Co., Ltd.

100 项与 Danavorexton 相关的临床结果

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100 项与 Danavorexton 相关的转化医学

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100 项与 Danavorexton 相关的专利（医药）

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20

项与 Danavorexton 相关的文献（医药）

2025-04-01·ANESTHESIOLOGY

Alluring Potential to Accelerate Emergence and Ameliorate Opioid-induced Respiratory Depression without Antagonizing Analgesia: Danavorexton Enters the Anesthetic Landscape

Article

作者: Kelz, Max B. ; Imamura, Toshihiro

2025-04-01·ANESTHESIOLOGY

Relax and Take a Deep(-er) Breath with Danavorexton

Article

作者: Ende, Holly B. ; Cheruku, Sreekanth R. ; Wanderer, Jonathan P.

2025-04-01·ANESTHESIOLOGY

TAK-925 (Danavorexton), an Orexin Receptor 2 Agonist, Reduces Opioid-induced Respiratory Depression and Sedation without Affecting Analgesia in Healthy Men

Article

作者: van Lemmen, Maarten ; van Velzen, Monique ; Lu, Hong ; Jansen, Simone C. ; Meyer, Seetha ; Wu, Rebecca L. ; Tolkoff, Max ; Naylor, Melissa ; von Rosenstiel, Philipp ; Hang, Yaming ; Sullivan, Danielle ; Dahan, Albert ; Sheikh, Sarah ; Olsson, Tina ; van der Schrier, Rutger

Background::

Orexin neuropeptides help regulate sleep/wake states, respiration, and pain. However, their potential role in regulating breathing, particularly in perioperative settings, is not well understood. TAK-925 (danavorexton), a novel orexin receptor 2–selective agonist, directly activates neurons associated with respiratory control in the brain and improves respiratory parameters in rodents undergoing fentanyl-induced sedation. This study assessed the safety and effect of danavorexton on ventilation in healthy men in an established remifentanil-induced respiratory depression model.

Methods::

This single-center, double-blind, placebo-controlled, two-way crossover, phase 1 trial randomized (1:1) 13 healthy men to danavorexton (11 mg [low-dose], then 19 mg [high-dose]) or placebo, under remifentanil infusion, on two occasions separated by a 36-h or longer washout period. Remifentanil infusion was titrated under isohypercapnic conditions to achieve an approximately 30 to 40% decrease in minute ventilation (from approximately 20 to approximately 14 l/min) before danavorexton/placebo administration. Assessments included safety, ventilation measurements, sedation, and pain tolerance.

Results::

A total of four (30.8%) danavorexton-treated participants and one (8.3%) placebo-treated participant experienced treatment-emergent adverse events (all mild in severity). Insomnia, lasting 1 day, occurred in one participant, and was considered related to danavorexton. Compared with placebo, low- and high-dose danavorexton significantly increased ventilation variables (observed mean [95% CI] change, sensitivity analysis model-based P values) including minute volume (8.2 [95% CI, 5.0 to 11.4] and 13.0 [95% CI, 9.4 to 16.5] l/min), tidal volume (312 [95% CI, 180 to 443] and 483 [95% CI, 309 to 657] ml), and respiratory rate (3.8 [95% CI, 1.9 to 5.7] and 5.2 [95% CI, 2.7 to 7.7] breaths/min; all P < 0.001). High-dose danavorexton significantly decreased sedation on a visual analog scale (–29.7 [95% CI, –54.1 to –5.3] mm; P < 0.001) and the Richmond Agitation Sedation Scale (0.4 [95% CI, 0.0 to 0.7]; P < 0.001) compared with placebo. Improvements in respiratory variables continued beyond completion of danavorexton infusion. No significant differences in pain tolerance were observed between danavorexton doses or between danavorexton and placebo (approximately 13% increase from baseline; low dose, P = 0.491; high dose, P = 0.140).

Conclusions::

Danavorexton has effects on respiration and wakefulness in an opioid-induced respiratory depression setting without reversing opioid analgesia.

5

项与 Danavorexton 相关的新闻（医药）

2025-05-09

·药研网

5.25亿美元打水漂？武田清理EGFR、B7-H3等项目

2025年5月8日，武田制药（Takeda）在公布其2024财年第四季度财报时，宣布对其研发管线进行重大调整。在肿瘤领域，武田制药宣布终止了其在2021年以5.25亿美元收购Maverick Therapeutics时获得的两个T细胞接合剂（TCE）项目：TAK-186（针对EGFR）：此项目在1/2期临床试验中已接近关键节点，武田决定停止进一步发展。TAK-280（针对B7-H3）：此项目在临床中也表现出一定潜力，但在继续推进之前，武田选择终止。此外，STING激动剂dazostinag也被撤出肿瘤研发管线，这一药物曾与默沙东的Keytruda联合进行2期临床试验。此次调整直接导致武田制药的1期和2期肿瘤管线规模减半，显示出公司在聚焦创新疗法上的决心。除了肿瘤领域的调整，武田制药还对其他研发项目进行了优化：danavorexton（TAK-925）：一种orexin-2受体激动剂，其2期临床试验因入组缓慢而被终止。TAK-007：一种CD19靶向CAR-NK疗法，原本用于B细胞恶性肿瘤治疗，已于去年停用。TAK-500：STING激动剂项目被撤出管线。武田制药表示，这些研发管线的调整是基于数据驱动的决策，旨在将公司资源集中于更具潜力的领域和项目。尽管精简了部分项目，武田制药目前仍保留6项处于3期临床阶段的高价值项目，涵盖罕见血液疾病、银屑病及神经疾病等多个领域。其中，治疗红细胞增多症的rusfertide在3月公布的3期试验结果中取得积极疗效，有望成为未来的重磅产品，峰值销售预估可达10亿至20亿美元。End声明：本公众号所有发文章(包括原创及转载文章)系出于传递更多信息之目的，且注明来源和作者。本公众号欢迎分享朋友圈或大群，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载/商务/投稿 | 联系微信15618157102（sum_Gmi）商务合作稿件征集点击了解详情往期回顾1集采政策重要拐点22025 AACR 中国ADC创新药物“起飞” | 附资料32025 ASCO热点速递 | 信达、荣昌、科伦集体登场!（附ADC/双/多抗最新进展一览表）

免疫疗法细胞疗法临床3期临床1期抗体药物偶联物

2025-05-09

·求实药社

武田砍掉多条临床管线，聚焦重点领域

来源：新猎药人笔记2025年5月8日，武田制药（Takeda）在其第四季度财报中宣布了一系列研发管线的调整，旨在优化资源配置，聚焦于最具潜力的项目。此次调整是公司战略转型的一部分，目的是在面临市场竞争和专利到期挑战时，保持长期增长潜力。• 肿瘤领域：武田制药终止了在2021年以5.25亿美元收购Maverick Therapeutics时获得的两个T细胞接合剂（TCE）项目，即TAK-186（针对EGFR）和TAK-280（针对B7-H3），这两个项目均处于1/2期临床试验阶段。此外，公司还停止了STING激动剂dazostinag的开发，该药物曾与默沙东的Keytruda联合进行2期临床试验。这些调整使武田制药的1期和2期肿瘤管线规模减半。• 其他领域：武田制药还停止了danavorexton（TAK-925，一种orexin-2受体激动剂）的2期临床试验，该试验因入组缓慢而被终止。此外，公司还从管线中移除了TAK-007（一种CD19靶向CAR-NK疗法）和TAK-500（STING激动剂）。武田制药表示，这些调整是基于数据驱动的决策，目的是将资源集中于最有潜力的项目上。公司目前有六个处于3期临床阶段的项目，这些项目被认为具有高价值潜力，包括治疗罕见血液疾病、银屑病和神经学疾病的疗法。例如，rusfertide在3月的3期临床试验中取得了积极结果，有望为公司带来10亿至20亿美元的峰值收入。结束语：武田制药的此次管线调整和资源重新分配，显示了其在面对市场挑战时的战略灵活性和对创新疗法的持续承诺。通过聚焦于最有潜力的项目，公司希望在未来的市场竞争中保持领先地位，并为患者提供更具变革性的治疗选择。免责声明：文章内容仅供参考，不构成投资建议。投资者据此操作，风险自担, 关于对文中陈述、观点判断保持中立，不对所包含内容的准确性、可靠性或完整性提供任何明示或暗示的保证。请读者仅作参考，并请自行承担全部。联系我们I-RNA 2025展位火热预定中！扫码立即咨询电话：13816031174（同微信）赞助形式包括但不仅限于演讲席位、会场展位、会刊彩页、晚宴赞助、会议用品宣传等。点击此处“阅读全文”咨询更多！

临床2期并购临床3期财报

2024-02-09

·Firstwordpharma

Phase IIb success propels Takeda's narcolepsy asset into late-stage testing

Takeda announced plans to initiate Phase III studies for its oral orexin receptor 2 (OX2R) agonist TAK-861 in narcolepsy type 1 (NT1), following positive findings from a Phase IIb trial. Sarah Sheikh, head of global development, said the “clear and compelling results” enable the company to commence late-stage testing as early as the first half of fiscal year 2024. The Phase IIb study, involving 112 patients with NT1, demonstrated statistically significant and clinically meaningful improvements in both objective and subjective measures of wakefulness for TAK-861 versus placebo at week 8. The primary endpoint, a maintenance of wakefulness test, was consistent with key secondary outcome measures, including the Epworth Sleepiness Scale and Weekly Cataplexy Rate. The drug was well tolerated, with no treatment-related serious adverse events.Takeda, which also ran a Phase IIb trial of TAK-861 in narcolepsy type 2 (NT2), stated it had no intentions of advancing the candidate in this indication. Findings from both studies will be presented at an upcoming scientific conference.Not all rosesTakeda’s orexin franchise encountered troubled waters in late 2021, when the Phase II programme for another oral OX2R agonist TAK-994 in NT1 and NT2 was axed after the emergence of a safety signal. The franchise also includes an investigational intravenous OX2R agonist TAK-925.Sheikh remarked that the drugmaker will continue to leverage its “deep and growing understanding of orexin biology” to investigate multiple orexin agonists across a wide range of indications, including conditions with normal orexin levels such as NT2.

临床2期临床结果临床失败

100 项与 Danavorexton 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Danavorexton	-	-

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
阻塞性睡眠呼吸暂停综合征	临床2期	美国	Takeda Pharmaceutical Co., Ltd.	2023-05-11
特发性睡眠过度	临床1期	美国	Millennium Pharmaceuticals, Inc.	2020-01-26
特发性睡眠过度	临床1期	日本	Millennium Pharmaceuticals, Inc.	2020-01-26
白天过度嗜睡	临床1期	美国	Millennium Pharmaceuticals, Inc.	2019-11-21
发作性睡病	临床1期	日本	Takeda Pharmaceutical Co., Ltd.	2017-11-04

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


WSC2023	N/A	阻塞性睡眠呼吸暂停综合征	-	TAK-925 (low-dose: 0.6mg [20mins] and 2.2mg [55mins]; high-dose: 1.8mg [20mins] and 6.6mg [55mins])	範製膚壓齋鏇膚選積選(膚廠餘窪餘鑰淵鑰觸鹹) = 憲餘壓願積積獵襯範簾選蓋願觸壓膚遞繭製夢 (醖築網鬱淵範鹹壓膚製, -18.2 ~ -0.9(low-dose);-1.2 to -10.1 to 7.7(high-dose)) 更多	-	2023-10-23
WSC2023	N/A	阻塞性睡眠呼吸暂停综合征	-	Danavorexton 5mg	窪顧窪膚獵艱夢醖糧觸(憲醖夢鏇獵夢夢遞蓋襯) = 積鹽憲鏇繭膚積網範齋憲餘觸膚糧壓簾壓繭構 (鏇選願獵鏇簾糧積壓鏇, -8 ~ 2)	-	2023-10-23
				Danavorexton 17mg	窪顧窪膚獵艱夢醖糧觸(憲醖夢鏇獵夢夢遞蓋襯) = 鑰壓鹹淵餘壓艱鹽網鹽憲餘觸膚糧壓簾壓繭構 (鏇選願獵鏇簾糧積壓鏇, -14 ~ 4) 更多
NCT04091438 (CTgov)	临床1期	特发性睡眠过度	28	Placebo (Placebo)	觸顧製糧憲網製獵繭鹹 = 壓鑰艱觸廠蓋鹹餘壓壓遞網衊願鏇窪網獵顧構 (壓積醖廠構積醖鹹鬱選, 齋繭構憲廠餘夢窪選網 ~ 繭觸膚選顧觸選窪蓋膚) 更多	-	2023-09-26
				TAK-925 (TAK-925 112 mg)	觸顧製糧憲網製獵繭鹹 = 積鹽範膚築糧襯觸顧選遞網衊願鏇窪網獵顧構 (壓積醖廠構積醖鹹鬱選, 獵齋窪築遞範淵衊鏇顧 ~ 餘願餘淵鬱願壓夢積夢) 更多
NCT03522506 (CTgov)	临床1期	-	20	Placebo (Placebo)	憲壓觸願醖襯範淵窪艱(餘壓窪襯衊鹽窪淵構淵) = 淵鏇廠鏇窪鹽鬱夢鏇艱餘構鏇齋襯範壓齋壓齋 (網醖齋選積壓窪築膚糧, 2.305) 更多	-	2019-11-26
				TAK-925 (TAK-925 44 mg)	憲壓觸願醖襯範淵窪艱(餘壓窪襯衊鹽窪淵構淵) = 廠鑰壓醖艱衊齋淵糧積餘構鏇齋襯範壓齋壓齋 (網醖齋選積壓窪築膚糧, 2.445) 更多
NCT03522506 (WSC2019)	临床1期	orexin levels	-	TAK-925	壓襯鹽窪淵衊壓繭網膚(鑰鹹齋糧淵鏇鑰憲壓蓋) = 鏇餘齋襯鑰觸鑰鑰壓選憲鹽鹹淵築鬱顧製艱襯 (遞繭製繭願構壓鏇艱糧 )	积极	2019-09-20
				Modafinil 300 mg	壓襯鹽窪淵衊壓繭網膚(鑰鹹齋糧淵鏇鑰憲壓蓋) = 獵糧膚廠廠衊衊膚鑰製憲鹽鹹淵築鬱顧製艱襯 (遞繭製繭願構壓鏇艱糧 )