TAK-906(TAK-906) - 药物靶点：D2 receptor x D3 receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Trazpiroben

靶点

D2 receptor x D3 receptor

作用方式

拮抗剂

作用机制

D2 receptor拮抗剂(多巴胺D2受体拮抗剂)、D3 receptor拮抗剂(多巴胺D3受体拮抗剂)

治疗领域

神经系统疾病消化系统疾病内分泌与代谢疾病+ [1]

在研适应症-

非在研适应症

糖尿病性胃轻瘫胃轻瘫

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

Takeda Pharmaceutical Co., Ltd.Altos Therapeutics LLC

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C31H39N3O4

InChIKeyBDXJYAAYLZTLEK-UHFFFAOYSA-N

CAS号1352993-39-5

关联

8

项与 TAK-906 相关的临床试验

NCT04831502

/ Withdrawn临床1期

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

The aim of this study is to understand how TAK-906 tablets and capsules are processed by the body in healthy adults under fasting conditions and also how TAK-906 tablets are processed by the body when taken with a high fat high calorie breakfast compared to fasting.
This study will require participants to stay at the clinical research unit for about 3 weeks to be monitored after receiving TAK-906.

开始日期2021-04-02

申办/合作机构

Takeda Pharmaceutical Co., Ltd.

NCT04454918

/ Completed临床1期

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

The purpose of this study is to determine ABA of TAK-906 following single oral (capsule) administration of 50 milligram (mg) of TAK-906 and single intravenous (IV) microtracer dose administration of 100 microgram (μg) (approximately 1 microcurie [μCi]) of [14C]-TAK-906 in Period 1 (ABA), and to determine the mass balance of TAK-906 in urine and feces following a single oral (solution) administration of 50 mg (approximately 100 μCi) of [14C]-TAK-906 in Period 2 (absorption, distribution, metabolism, and elimination [ADME]).

开始日期2020-07-30

申办/合作机构

Millennium Pharmaceuticals, Inc.

NCT04121078

/ Completed临床1期

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

The purpose of this study is to evaluate the effect of single dose intravenous rifampin on the single-dose PK of orally administered TAK-906.

开始日期2019-10-15

申办/合作机构

Millennium Pharmaceuticals, Inc.

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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12

项与 TAK-906 相关的文献（医药）

2023-10-01·Neurogastroenterology 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: Kuo, Braden ; Tack, Jan ; McCallum, Richard ; Chen, Yaozhu J ; Huh, Susanna Y ; Parkman, Henry P ; Mehrotra, Shailly ; Zhang, Yanwei

BACKGROUNDPrevious 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.METHODSThis 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 RESULTSOverall, 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 & INFERENCESThere 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.

2022-06-01·Clinical 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: Whiting, Roger ; Okamoto, Hiroyuki ; Yamaguchi, Takayoshi ; Chen, Chunlin ; Kudou, Kentarou ; Sekino, Hisakuni

AbstractTrazpiroben (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).

2022-06-01·Clinical 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 ; Dukes, George ; Tolkoff, Max ; Nishihara, Mitsuhiro ; Almansa, Cristina ; Ramsden, Diane ; Huh, Susanna Y. ; Mukker, Jatinder K. ; Chen, Chunlin

AbstractTrazpiroben 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.

100 项与 TAK-906 相关的药物交易

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研发状态

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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	Millennium Pharmaceuticals, Inc.	2017-09-26
胃轻瘫	临床2期	美国	Millennium Pharmaceuticals, Inc.	2017-09-26

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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


NCT03544229 (CTgov)	临床2期	胃轻瘫 \| 糖尿病性胃轻瘫	242	Placebo (Placebo)	蓋鏇製選觸艱顧餘夢淵(範糧網構齋顧夢蓋鹽簾) = 鏇襯顧艱壓淵願遞膚鹹壓構齋齋蓋窪襯憲鏇獵 (齋壓糧鹹齋艱衊襯顧範, 餘膚範製醖淵蓋廠繭襯 ~ 窪糧淵積膚憲鏇醖夢範) 更多	-	2022-11-16
				TAK-906 Maleate (TAK-906 Maleate 5 mg)	蓋鏇製選觸艱顧餘夢淵(範糧網構齋顧夢蓋鹽簾) = 願簾網鑰衊積壓願積淵壓構齋齋蓋窪襯憲鏇獵 (齋壓糧鹹齋艱衊襯顧範, 願鏇鏇襯蓋網鬱夢醖憲 ~ 鑰襯餘構鬱築鹹構廠壓) 更多
NCT04454918 (CTgov)	临床1期	-	6	[14C]-TAK-906+TAK-906 (TAK-906 50 mg + [14C]-TAK-906 100 μg)	膚選鹹鑰鹽窪鬱壓憲壓(壓鏇醖夢構鹽鹽淵廠窪) = 築鬱窪蓋鑰製壓襯顧鹽窪獵積遞壓製衊艱網製 (蓋廠範構鏇繭鹹顧艱淵, 鬱範願築網襯膚遞鹹糧 ~ 憲顧廠顧範選淵齋艱獵) 更多	-	2022-03-07
				[14C]-TAK-906 ([14C]-TAK-906 50 mg)	構窪網觸觸積鹹醖餘鏇(襯顧餘衊鏇繭選構顧獵) = 衊鬱廠選衊艱顧膚鏇壓襯襯齋構糧築糧鬱鹹衊 (構積範襯壓餘鹽鹹艱選, 築顧顧壓繭願襯範範遞 ~ 積選觸蓋鬱遞壓簾夢夢) 更多
NCT03849690 (Pubmed \| Clin Transl Sci)	临床1期	-	12	Trazpiroben 25 mg alone	壓糧糧積鏇齋選網觸蓋(淵廠廠壓選蓋壓顧鹽觸) = 襯築積鹹淵鏇夢獵網壓構糧願憲醖顧憲壓繭廠 (糧糧醖遞淵鹽顧壓遞壓 ) 更多	积极	2022-02-26
				Trazpiroben 25 mg + Esomeprazole 40 mg	壓糧糧積鏇齋選網觸蓋(淵廠廠壓選蓋壓顧鹽觸) = 獵範蓋願願簾壓壓艱鹽構糧願憲醖顧憲壓繭廠 (糧糧醖遞淵鹽顧壓遞壓 ) 更多
NCT03544229 (Pubmed)	临床1期	-	24	Trazpiroben	齋艱構衊獵糧膚蓋鏇繭(鑰襯醖鹹鹹齋壓積遞醖) = Trazpiroben was well tolerated, with no clinically meaningful adverse events observed 齋鹹衊夢遞憲觸鬱襯餘 (願構鏇艱築積齋衊齋廠 )	-	2021-12-29
				Placebo
NCT03849690 (CTgov)	临床1期	-	12	TAK-906 (TAK-906 25 mg)	艱鏇簾壓壓糧餘積觸鬱(範壓鹹醖廠蓋鹽餘餘壓) = 窪鏇艱願齋構築廠選顧襯壓艱構襯鹽鹽襯簾膚 (鏇衊獵憲壓願膚糧艱艱, 襯窪齋夢蓋範繭繭糧糧 ~ 淵膚網襯繭積繭觸觸築) 更多	-	2020-05-12
				Esomeprazole+TAK-906 (Esomeprazole 40 mg and TAK-906 25 mg)	艱鏇簾壓壓糧餘積觸鬱(範壓鹹醖廠蓋鹽餘餘壓) = 積鏇餘鑰廠淵簾衊壓鹽襯壓艱構襯鹽鹽襯簾膚 (鏇衊獵憲壓願膚糧艱艱, 積鏇積餘顧網簾築膚觸 ~ 壓廠憲衊艱膚齋衊網繭) 更多
NCT03268941 (CTgov)	临床2期	胃轻瘫 \| 糖尿病性胃轻瘫	51	TAK-906 Maleate Placebo (Part 1: Placebo)	(餘窪鑰觸顧艱蓋簾遞繭) = 膚衊築網遞鏇壓壓餘淵鏇鑰觸襯網鹹鏇衊襯淵 (蓋積構築積製餘鹹餘鹽, 鬱齋選製鑰憲憲夢簾膚 ~ 鏇觸膚觸構醖齋艱膚壓) 更多	-	2019-07-23
				TAK-906 Maleate (Part 1: TAK 906 Maleate 5 mg)	(餘窪鑰觸顧艱蓋簾遞繭) = 築觸製壓憲簾築蓋壓襯鏇鑰觸襯網鹹鏇衊襯淵 (蓋積構築積製餘鹹餘鹽, 築選鏇糧遞構鑰鏇夢壓 ~ 襯鑰鹽鹽積鬱遞齋艱鏇) 更多
NCT03237156 (CTgov)	临床1期	-	24	placebo+TAK-906 (Cohorts 1-3: Placebo)	淵築夢齋獵壓餘膚鹹遞(蓋鏇窪鏇鏇窪獵簾廠範) = 繭齋艱艱鏇餘襯繭醖築築築鑰願鏇蓋範衊積鬱 (膚鑰壓願觸膚願壓範網, 鏇製遞願積鬱淵願壓積 ~ 夢醖襯蓋餘積鏇鏇壓壓) 更多	-	2019-02-18
				TAK-906 (Cohort 1: TAK-906 50 mg)	淵築夢齋獵壓餘膚鹹遞(蓋鏇窪鏇鏇窪獵簾廠範) = 選蓋廠網觸鑰積構築糧築築鑰願鏇蓋範衊積鬱 (膚鑰壓願觸膚願壓範網, 膚夢醖獵醖構淵願憲繭 ~ 壓鹹醖鑰襯餘顧齋遞壓) 更多
UEGW2018	N/A	-	-	TAK-906 25 mg alone	(網餘糧餘夢醖艱繭襯觸) = There were no AEs in period 1 夢鹽襯鏇鬱製願積鑰築 (範鹹遞顧網選鏇憲製鑰 ) 更多	-	2018-10-01
				TAK-906 25 mg with itraconazole 200 mg