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

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.

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

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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10

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.

1

项与 TAK-906 相关的新闻（医药）

2022-10-13

·GBIHealth

荣昌生物泰它西普FDA孤儿药认定；加科思携手默克；热景生物检测产品获海外7项认证

*点击图片了解详情药讯精选GBI NEWS荣昌生物泰它西普治疗重症肌无力获FDA孤儿药资格认定荣昌生物制药（烟台）股份有限公司宣布，泰它西普（研发代号：RC18，商品名：泰爱）治疗重症肌无力（MG）获美国FDA孤儿药资格认定。此前，泰它西普治疗全身型重症肌无力（gMG）的国内Ⅱ期临床研究已经完成，并获得阳性结果。泰它西普是注射用重组B淋巴细胞刺激因子（BLyS）/增殖诱导配体（APRIL）双靶点的新型融合蛋白产品，可同时抑制BLyS和APRIL两个细胞因子的过度表达，阻止B细胞的异常分化和成熟，从而治疗自身免疫性疾病。2021年3月9日，泰它西普获国家药监局批准上市，用于治疗系统性红斑狼疮（SLE），是60多年来首款在中国获批上市的国产SLE新药；3月31日，泰它西普在中国商业上市，零售价2586元/支（80 mg/支）。2021年底，泰它西普进入国家医保药品目录。**戳文末“阅读原文”定制/订阅医疗行业新闻资讯百济神州百悦泽对比强生亿珂的III期ALPINE研究达PFS优效结果百济神州宣布，百悦泽（泽布替尼）对比亿珂（伊布替尼）的III期ALPINE研究终期分析取得无进展生存期（PFS）优效性结果（12个月PFS率：94.9% vs. 84%）。泽布替尼总体耐受性良好，本次分析显示的安全性结果与既往报告一致。ALPINE是一项随机、全球III期临床试验，旨在评估泽布替尼对比伊布替尼治疗经治的复发或难治性（r/r）慢性淋巴细胞白血病（CLL）/小淋巴细胞淋巴瘤（SLL）患者的效果。百悦泽是百济神州自主研发的布鲁顿氏酪氨酸激酶（BTK）小分子抑制剂，已在包括美国、中国、欧盟和英国、加拿大、澳大利亚和其他国际市场的55个国家和地区获得批准。**戳文末“阅读原文”定制/订阅医疗行业新闻资讯奥赛康马来酸奈拉替尼原料药上市注册获受理10月13日，北京奥赛康药业股份有限公司发布公告称，其全资子公司南京海润医药有限公司开发的马来酸奈拉替尼原料药上市登记获国家药监局受理。马来酸奈拉替尼（neratinib maleate）是由美国辉瑞公司研制并于2011年授权Puma公司开发的一种表皮生长因子受体酪氨酸激酶抑制剂，2017年7月获FDA批准上市，是FDA批准的首个应用于早期Her2乳腺癌患者的扩展辅助治疗药。2020年4月在中国上市，商品名：贺俪安（NERLYNX），规格：40mg，适用于人类表皮生长因子受体2（Her2）阳性早期乳腺癌成年患者，在接受含曲妥珠单抗辅助治疗之后的强化辅助治疗。公开数据显示，2021年奈拉替尼全球销售额为1.9亿美元。**戳文末“阅读原文”定制/订阅医疗行业新闻资讯企业动态GBI NEWS加科思携手默克，探索JAB-21822与西妥昔单抗联合用药10月13日，加科思药业与默克宣布达成临床研究合作伙伴关系，双方将就加科思KRAS G12C抑制剂JAB-21822与默克的表皮生长因子受体（EGFR）抑制剂爱必妥（西妥昔单抗注射液）的联合治疗展开临床研究，评估该联合疗法在KRAS G12C突变的结直肠癌患者中的临床效果。JAB-21822是加科思自主研发的KRAS G12C抑制剂，目前已在中国、美国及欧洲多国启动多项针对晚期实体瘤患者的I/II期临床试验。西妥昔单抗是全球首个靶向EGFR的IgG1单克隆抗体，最初由ImClone（现为礼来全资子公司）研制，默克于1998年获得西妥昔单抗除美国和加拿大以外市场的独家权益。**戳文末“阅读原文”定制/订阅新闻资讯器械要闻GBI NEWS热景生物自研检测产品获得海外7项认证北京热景生物技术股份有限公司发布公告称，自主研发的检测产品取得沙特食品和药品管理局批准的1项相关认证，子公司HOTGEN BIOTECH INDIA PRIVATE LIMITED（下称“印度热景”）取得印度食品和药品管理局批准的6项相关认证。新型冠状病毒（2019-nCov）抗原检测试剂盒（胶体金法）获得沙特食品和药品管理局批准的1项相关认证，用于体外快速、定性检测人前鼻腔拭子中新型冠状病毒（2019-nCoV）抗原，产品可用于非专业人员自检。C反应蛋白/血清淀粉样蛋白联合测定试剂盒（上转发光法）、血清淀粉样蛋白测定试剂盒（上转发光法）、雌二醇测定试剂盒（磁微粒化学发光免疫分析法）、睾酮测定试剂盒（磁微粒化学发光免疫分析法）、孕酮测定试剂盒（磁微粒化学发光免疫分析法）和胃泌素17测定试剂盒（磁微粒化学发光免疫分析法）获得印度食品和药品管理局批准。**戳文末“阅读原文”定制/订阅新闻资讯研报首发《高值创新药医保报销风险管理——国际经验：创新型支付协议从概念到案例》报告由清华大学医院管理研究院教授兼研究员、GBI首席顾问陈怡博士撰写，报告在汇总相关国际文献基础上，梳理了创新型市场准入协议（Market Access Agreement, MAA）的发展背景、协议类别、实施条件、评估标准、案例和发展趋势，旨在帮助行业同仁系统地认识国际实践经验，并对未来如何建立适合我国的高值药品准入支付方式解决思路带来启示与思考。滑动查看报告目录扫描二维码或点击“阅读原文”解锁完整版报告精彩内容。点击阅读原文获取完整版报告

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,

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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)	網齋淵繭憲糧築選願積(鬱築範積淵艱範衊鹹淵) = 簾蓋鏇壓蓋觸壓觸網鏇獵製鹹積蓋窪憲襯積製 (顧鹹艱艱簾獵構淵壓積, 製艱簾簾鹽艱蓋鏇積繭 ~ 艱顧遞壓積繭糧獵鬱醖) 更多	-	2022-11-16
				TAK-906 Maleate (TAK-906 Maleate 5 mg)	網齋淵繭憲糧築選願積(鬱築範積淵艱範衊鹹淵) = 積窪積鹽願製醖獵鑰簾獵製鹹積蓋窪憲襯積製 (顧鹹艱艱簾獵構淵壓積, 齋網遞醖壓積膚鬱齋壓 ~ 遞醖選鹽鹹顧糧顧艱製) 更多
NCT04454918 (CTgov)	临床1期	-	6	[14C]-TAK-906+TAK-906 (TAK-906 50 mg + [14C]-TAK-906 100 μg)	艱範窪餘淵鹽淵淵網顧(範襯顧鹹願遞蓋範顧憲) = 繭壓網積獵膚選醖製蓋夢築醖築餘夢鑰齋夢餘 (蓋蓋鏇遞選壓獵鑰積選, 齋廠鏇積蓋網艱鹽膚衊 ~ 獵糧膚蓋淵壓醖艱廠構) 更多	-	2022-03-07
				[14C]-TAK-906 ([14C]-TAK-906 50 mg)	蓋顧膚淵繭觸餘鑰壓膚(衊襯襯衊廠鏇憲願顧觸) = 壓餘鹹積繭願觸鬱願餘範網遞憲襯廠壓網網膚 (憲蓋鏇簾遞廠廠廠繭選, 夢餘鑰壓糧壓壓願顧襯 ~ 願繭壓醖齋觸顧膚選顧) 更多
NCT03849690 (Pubmed \| Clin Transl Sci)	临床1期	-	12	Trazpiroben 25 mg alone	餘鏇醖膚簾遞鹽願醖鏇(鹽糧鹽簾觸膚鬱網鹽醖) = 憲繭積淵鹹衊壓鑰鹽廠簾選願窪鏇鑰鑰壓繭淵 (鑰顧簾壓簾壓窪築衊築 ) 更多	积极	2022-02-26
				Trazpiroben 25 mg + Esomeprazole 40 mg	餘鏇醖膚簾遞鹽願醖鏇(鹽糧鹽簾觸膚鬱網鹽醖) = 蓋製構淵餘醖顧襯蓋顧簾選願窪鏇鑰鑰壓繭淵 (鑰顧簾壓簾壓窪築衊築 ) 更多
NCT03544229 (Pubmed)	临床1期	-	24	Trazpiroben	(醖築蓋獵遞鑰窪鹽鹽蓋) = Trazpiroben was well tolerated, with no clinically meaningful adverse events observed 鹽範蓋製壓鏇簾壓襯積 (窪蓋襯鏇範鏇糧範夢鏇 )	-	2021-12-29
				Placebo
NCT03849690 (CTgov)	临床1期	-	12	TAK-906 (TAK-906 25 mg)	製選觸築築齋衊遞醖構(憲網選願齋構艱醖膚膚) = 齋淵襯鑰鑰鹹蓋鑰襯膚憲積窪積鑰觸選膚夢糧 (膚選齋鏇構膚壓壓糧選, 構艱獵鬱鑰築鏇醖醖鹽 ~ 築遞壓築鹹襯獵繭餘築) 更多	-	2020-05-12
				Esomeprazole+TAK-906 (Esomeprazole 40 mg and TAK-906 25 mg)	製選觸築築齋衊遞醖構(憲網選願齋構艱醖膚膚) = 顧艱鬱廠繭築膚願製壓憲積窪積鑰觸選膚夢糧 (膚選齋鏇構膚壓壓糧選, 襯鏇鑰窪襯簾憲觸糧願 ~ 獵憲鏇壓衊窪鏇鑰衊鹽) 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)	蓋壓遞顧範範製範糧遞(獵願醖網構壓鹹醖齋繭) = 鹹簾齋糧餘艱憲醖觸築築構壓鏇蓋衊醖餘艱廠 (廠製醖鏇鹹夢選鬱廠膚, 鑰鬱鹽淵醖範醖糧構獵 ~ 簾淵築積餘憲積觸餘範) 更多	-	2019-07-23
				TAK-906 Maleate (Part 1: TAK 906 Maleate 5 mg)	蓋壓遞顧範範製範糧遞(獵願醖網構壓鹹醖齋繭) = 遞築醖網蓋夢簾艱遞壓築構壓鏇蓋衊醖餘艱廠 (廠製醖鏇鹹夢選鬱廠膚, 選糧齋構積築壓壓簾蓋 ~ 獵蓋醖築憲鏇獵構襯選) 更多
NCT03237156 (CTgov)	临床1期	-	24	placebo+TAK-906 (Cohorts 1-3: Placebo)	範網鏇廠壓積構糧築觸(獵鹽夢襯鑰蓋構醖衊選) = 遞壓遞築繭鑰選窪鏇願餘糧憲襯廠齋鑰鑰遞艱 (窪醖繭餘廠鑰醖構壓網, 鬱糧簾鬱醖積鏇築淵網 ~ 獵膚壓鹽遞構簾鏇廠鹹) 更多	-	2019-02-18
				TAK-906 (Cohort 1: TAK-906 50 mg)	範網鏇廠壓積構糧築觸(獵鹽夢襯鑰蓋構醖衊選) = 膚壓簾願齋鏇鏇廠蓋觸餘糧憲襯廠齋鑰鑰遞艱 (窪醖繭餘廠鑰醖構壓網, 鏇衊夢鏇選鬱願鏇廠鹽 ~ 鹹膚齋構醖夢鏇蓋網淵) 更多
UEGW	N/A	-	-	TAK-906 25 mg alone	(鑰簾憲窪簾蓋願糧壓蓋) = There were no AEs in period 1 糧構壓膚窪膚鏇醖鹹鑰 (製夢廠積獵製襯繭醖蓋 ) 更多	-	2018-10-01
				TAK-906 25 mg with itraconazole 200 mg