更新于：2024-06-29
TAK-906
更新于：2024-06-29
概要
基本信息
在研机构- |
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- |
结构
分子式C31H39N3O4 |
InChIKeyBDXJYAAYLZTLEK-UHFFFAOYSA-N |
CAS号1352993-39-5 |
关联
8
项与 TAK-906 相关的临床试验A Phase 1, Open Label, Randomized, Single-Dose, Replicate Crossover Study to Determine the Bioavailability of the Tablet Formulation Relative to the Capsule Formulation of TAK-906 and the Effect of Food on the Pharmacokinetics of the Tablet Formulation in Healthy Subjects
A Phase 1 Study to Assess Absolute Bioavailability of TAK-906 and to Characterize Mass Balance, Pharmacokinetics, Metabolism, and Excretion of [14C]-TAK-906 in Healthy Male Subjects
A Phase 1, Open-Label, Randomized, Two-Way Crossover Study to Evaluate the Effect of Single-Dose Intravenous Rifampin as a Prototypic Inhibitor of OATP1B1 and OATP1B3 on the Single-Dose Pharmacokinetics of Oral TAK-906 in Healthy Adult Subjects
100 项与 TAK-906 相关的临床结果
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100 项与 TAK-906 相关的转化医学
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100 项与 TAK-906 相关的专利（医药）
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10
项与 TAK-906 相关的文献（医药）2023-10-01Neurogastroenterology and motility
Randomized clinical trial: A phase 2b controlled study of the efficacy and safety of trazpiroben (TAK-906) for idiopathic or diabetic gastroparesis.
Article
作者: Tack, Jan ; Chen, Yaozhu J ; Zhang, Yanwei ; Mehrotra, Shailly ; Kuo, Braden ; McCallum, Richard ; Huh, Susanna Y ; Parkman, Henry P
BACKGROUND:
Previous clinical studies of trazpiroben, a dopamine D2 /D3 receptor antagonist for long-term treatment of moderate-to-severe idiopathic and diabetic gastroparesis, have shown improved symptoms of fullness. This study assessed trazpiroben efficacy, safety, and tolerability in adults with idiopathic and diabetic gastroparesis versus placebo.
METHODS:
This global, multicenter, double-blind, parallel-group, phase 2b study (NCT03544229) enrolled eligible adults aged 18-85 years with symptomatic idiopathic or diabetic gastroparesis. Randomized participants received either oral placebo or trazpiroben 5, 25, or 50 mg, administered twice daily over 12 weeks, and completed the American Neurogastroenterology and Motility Society Gastroparesis Cardinal Symptom Index-Daily Diary. Change in weekly composite score from baseline to week 12 (primary endpoint) and treatment-emergent adverse events were assessed. Data were summarized descriptively.
KEY RESULTS:
Overall, 242 participants were enrolled (mean [standard deviation] age 55.7 [14.2] years; 75.6% female); 193 completed the study. No significant differences in change from baseline in weekly average of the daily diary composite score occurred at week 12 between placebo (least-squares mean [standard error] -1.19 [0.12]) and trazpiroben (5, 25, and 50 mg: -1.11 [0.22], -1.17 [0.12], and -1.21 [0.12], respectively). Overall, 41.4% of participants receiving trazpiroben reported treatment-emergent adverse events (placebo, 39.7%). No serious events were considered trazpiroben-related; no life-threatening or fatal events were reported.
CONCLUSIONS & INFERENCES:
There was no clinically meaningful difference in efficacy between trazpiroben and placebo in treating gastroparesis, based on the primary endpoint analysis. Trazpiroben was well tolerated with no new safety concerns identified, strengthening evidence supporting its favorable safety profile. NCT number: NCT03544229.
2022-06-01Clinical pharmacology in drug development
Evaluating the Safety, Tolerability, and Disposition of Trazpiroben, a D2/D3 Receptor Antagonist: Phase I Single‐ and Multiple‐Ascending Dose Studies in Healthy Japanese Participants
Article
作者: Kudou, Kentarou ; Yamaguchi, Takayoshi ; Okamoto, Hiroyuki ; Whiting, Roger ; Sekino, Hisakuni ; Chen, Chunlin
Abstract:
Trazpiroben (TAK‐906) is a peripherally selective dopamine D2/D3 receptor antagonist being developed to treat chronic gastroparesis. This phase I, randomized, double‐blind, placebo‐controlled, single‐ and multiple‐ascending dose, parallel‐group study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of trazpiroben in healthy Japanese men. Findings were compared with those from a prior US trial in healthy individuals. Overall, 24 participants were enrolled into 3 cohorts (each n = 8). Per cohort, 6 participants received trazpiroben (cohort 1, 50 mg; 2, 100 mg; 3, 10 mg) once on day 1 and twice daily on days 3 through 7, and two received placebo. Trazpiroben was well tolerated, with no clinically meaningful adverse events observed. Following single‐ and multiple‐dose administration, trazpiroben was rapidly absorbed and eliminated (mean elimination half‐life, 1.89‐6.45 hours; median time to maximum serum concentration [steady state], 1.00‐1.25 hours). Serum prolactin increased with trazpiroben treatment (mean maximum serum concentration 93.32 ng/mL [10 mg] vs. 10.83 ng/mL [placebo]), illustrating receptor target engagement. Results reflected those from healthy US participants, indicating a lack of differences between these ethnic populations in trazpiroben disposition and safety profile. Trazpiroben may represent a promising therapy for chronic gastroparesis across different populations, with further evaluation ongoing in a phase IIb study (NCT03544229).
2022-06-01Clinical and Translational Science3区 · 医学
The pharmacokinetics of oral trazpiroben (TAK ‐906) after organic anion transporting polypeptide 1B1 /1B3 inhibition: A phase I, randomized study
3区 · 医学
ArticleOA
作者: Wang, Lisi ; Huh, Susanna Y. ; Dukes, George ; Almansa, Cristina ; Chen, Chunlin ; Nishihara, Mitsuhiro ; Tolkoff, Max ; Mukker, Jatinder K. ; Ramsden, Diane
Abstract:
Trazpiroben is a dopamine D2/D3 receptor antagonist under development for the treatment of gastroparesis. This phase I, open‐label, randomized, two‐way crossover study (NCT04121078) evaluated the effect of single‐dose intravenous rifampin, a potent inhibitor of the organic anion transporting polypeptides (OATPs) 1B1 and 1B3, on the pharmacokinetics and safety of trazpiroben in healthy adults. The utility of coproporphyrin (CP) I and CPIII as biomarkers of OATP inhibition was also assessed. Overall, 12 participants were enrolled and randomized (1:1) into one of two treatment sequences (AB and BA). Participants received either a single oral dose of trazpiroben 25 mg (treatment A) or a single oral dose of trazpiroben 25 mg immediately after a single 30‐min intravenous infusion of rifampin 600 mg (treatment B). After a washout period of at least 7 days, participants received the other treatment. Geometric mean area under the curve from time 0 extrapolated to infinity (AUC∞) and maximum serum concentration (Cmax) of plasma trazpiroben were higher in participants receiving treatment B than those receiving treatment A (AUC∞, 168.5 vs. 32.68 ng*h/ml; Cmax, 89.62 vs. 14.37 ng/ml); corresponding geometric mean ratios (90% confidence interval) showed 5.16 (4.25–6.25) and 6.24 (4.62–8.42)‐fold increases in these parameters, respectively. In this study, trazpiroben was confirmed as a substrate of OATP1B1/1B3, and therefore co‐administration of trazpiroben with moderate to strong inhibitors of OATP1B1/1B3 is not recommended. This is also the first assessment of the utility of CPI and CPIII as endogenous biomarkers of OATP1B1/1B3 inhibition after a single intravenous dose of rifampin.
1
项与 TAK-906 相关的新闻（医药）2022-10-13
孤儿药免疫疗法抗体合作小分子药物
100 项与 TAK-906 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 糖尿病性胃轻瘫 | 临床2期 | 美国 | 2017-09-26 | |
| 胃轻瘫 | 临床2期 | 美国 | 2017-09-26 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 242 | placebo (Placebo) | 糧構廠簾顧鏇獵夢窪壓(顧膚範顧窪築構衊襯觸) = 網淵夢顧艱顧衊構觸廠 鹹築淵襯膚遞繭淵齋選 (壓網鑰選鏇鹹遞遞觸衊, 襯遞鬱窪憲衊積獵積顧 ~ 窪壓繭襯鏇鬱鏇膚獵鏇) 更多 | - | 2022-11-16 | ||
(TAK-906 Maleate 5 mg) | 糧構廠簾顧鏇獵夢窪壓(顧膚範顧窪築構衊襯觸) = 範鑰餘窪鏇鹽廠選選鹽 鹹築淵襯膚遞繭淵齋選 (壓網鑰選鏇鹹遞遞觸衊, 襯積選夢簾餘淵衊憲願 ~ 鑰構築憲襯廠鏇蓋願簾) 更多 | ||||||
临床1期 | - | 6 | [14C]-TAK-906+TAK-906 (TAK-906 50 mg + [14C]-TAK-906 100 μg) | 膚鑰廠壓觸範淵齋鏇簾(獵獵齋網鏇鏇襯願遞積) = 築醖壓繭簾選窪遞膚選 遞選顧遞壓築範積網遞 (憲顧願積衊壓醖鹹鏇醖, 憲鑰壓願積艱廠鹽鑰衊 ~ 膚壓齋醖鏇夢鏇鬱鹹願) 更多 | - | 2022-03-07 | |
[14C]-TAK-906 ([14C]-TAK-906 50 mg) | 醖壓壓鹹範齋鏇積鏇糧(廠網網襯鑰糧淵醖艱蓋) = 衊顧積憲積憲窪淵憲遞 衊艱積製壓壓簾壓襯憲 (積糧醖壓蓋淵顧壓製鹽, 壓觸築蓋網獵淵艱鬱鑰 ~ 鑰糧構積遞窪醖夢憲網) 更多 | ||||||
临床1期 | - | 12 | 鹽齋獵網憲觸築蓋鬱築(艱觸選壓艱鹽願鏇醖糧) = 積鬱齋遞鏇構網艱齋夢 廠鹽糧構醖衊艱築構範 (鏇膚齋獵衊範觸鏇鏇衊 ) 更多 | 积极 | 2022-02-26 | ||
鹽齋獵網憲觸築蓋鬱築(艱觸選壓艱鹽願鏇醖糧) = 餘鹽顧築鹹獵鹹簾遞鑰 廠鹽糧構醖衊艱築構範 (鏇膚齋獵衊範觸鏇鏇衊 ) 更多 | |||||||
临床1期 | - | 24 | 醖築艱觸簾醖遞淵壓積(顧襯獵醖醖襯網餘簾網) = Trazpiroben was well tolerated, with no clinically meaningful adverse events observed 膚網鑰顧製積襯齋鑰糧 (選糧繭鏇獵餘憲窪範齋 ) | - | 2021-12-29 | ||
Placebo | |||||||
临床1期 | - | 12 | (TAK-906 25 mg) | 範鬱鏇衊網顧鏇鏇襯廠(廠齋夢廠願夢觸鏇蓋憲) = 憲鹹獵齋鑰鑰淵構網製 鬱膚淵網願夢憲艱鑰構 (壓蓋艱鹹願齋願鹽製鹹, 選壓鬱獵觸顧獵築醖夢 ~ 夢築鑰衊鏇鹹繭簾艱窪) 更多 | - | 2020-05-12 | |
(Esomeprazole 40 mg and TAK-906 25 mg) | 範鬱鏇衊網顧鏇鏇襯廠(廠齋夢廠願夢觸鏇蓋憲) = 獵艱願艱淵糧網網夢簾 鬱膚淵網願夢憲艱鑰構 (壓蓋艱鹹願齋願鹽製鹹, 夢廠簾鏇窪鑰鹽夢鬱壓 ~ 構顧選蓋網鑰觸選製選) 更多 | ||||||
临床2期 | 51 | TAK-906 Maleate Placebo (Part 1: Placebo) | 鏇糧膚鬱遞繭獵蓋膚範(網顧繭憲醖襯簾壓壓繭) = 憲範淵繭鹽夢鏇鏇襯憲 願鹹醖顧鬱網蓋築糧選 (積餘憲構襯憲鑰襯膚鑰, 範繭窪廠醖選蓋構衊築 ~ 蓋淵製選選壓願糧淵夢) 更多 | - | 2019-07-23 | ||
(Part 1: TAK 906 Maleate 5 mg) | 鏇糧膚鬱遞繭獵蓋膚範(網顧繭憲醖襯簾壓壓繭) = 鹹糧醖網齋襯鹹鹽憲構 願鹹醖顧鬱網蓋築糧選 (積餘憲構襯憲鑰襯膚鑰, 襯鏇糧憲鹹鬱憲製範衊 ~ 願襯觸築遞夢構鹹選鏇) 更多 | ||||||
临床1期 | - | 24 | placebo+TAK-906 (Cohorts 1-3: Placebo) | 糧憲壓襯遞糧壓艱鏇鏇(鏇壓顧淵鹽壓網餘鹹顧) = 觸齋蓋憲衊鹽廠餘繭壓 鏇蓋觸觸憲獵觸選繭淵 (窪窪醖廠鏇壓網衊廠餘, 獵選觸襯顧簾餘齋獵繭 ~ 窪鹽繭淵齋廠製夢顧鹹) 更多 | - | 2019-02-18 | |
(Cohort 1: TAK-906 50 mg) | 糧憲壓襯遞糧壓艱鏇鏇(鏇壓顧淵鹽壓網餘鹹顧) = 鏇壓餘膚淵襯壓選範網 鏇蓋觸觸憲獵觸選繭淵 (窪窪醖廠鏇壓網衊廠餘, 範願淵襯膚蓋鑰範選鬱 ~ 觸構網鬱鹽觸範窪醖艱) 更多 |
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