Pumosetrag(Pumosetrag) - 药物靶点：5-HT3 receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [1]

靶点

5-HT3 receptor

作用机制

5-HT3 receptor激动剂(5-羟色胺受体3激动剂)

治疗领域

消化系统疾病口颌疾病耳鼻咽喉疾病+ [1]

在研适应症-

非在研适应症

便秘消化不良反流性食管炎+ [3]

原研机构

Mitsubishi Tanabe Pharma Corp.

在研机构-

非在研机构

Mitsubishi Tanabe Pharma Corp.EDUSA Corp.Edusa Pharmaceuticals, Inc.

+ [2]

最高研发阶段终止临床3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C15H17N3O2S

InChIKeyAFUWQWYPPZFWCO-LBPRGKRZSA-N

CAS号153062-94-3

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关联

3

项与 Pumosetrag 相关的临床试验

NCT01161602 / Completed临床2期

A Phase IIa, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety, Tolerability and Pharmacodynamics of Multiple Dose Levels of Pumosetrag in Patients With Symptoms Associated With Gastroesophageal Reflux Disease (GERD) Receiving a Standard Refluxogenic Meal

The purpose of this study is to determine if pumosetrag is effective in treating Gastroesophageal Reflux Disease (GERD) symptoms in patients who have a history of GERD symptoms and are currently taking an acid suppression therapy, such as a Proton Pump Inhibitor (PPI).

开始日期-

申办/合作机构

Edusa Pharmaceuticals, Inc.

NCT00547469 / Unknown status临床2/3期

A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Effectiveness of DDP733 in Female Patients With Irritable Bowel Syndrome With Constipation

This study will evaluate the safety and effectiveness of the investigational drug DDP733 in treating female patients with IBS-c. A placebo control will be utilized.

开始日期2007-10-01

申办/合作机构

Dynogen Pharmaceuticals, Inc.

NCT00215566 / Completed临床2期

A Phase 2a, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety, Tolerability, and Pharmacodynamics of Multiple Doses and Dose Levels of DDP733 in Patients With Irritable Bowel Syndrome With Constipation

This study will evaluate the safety, tolerability and pharmacodynamics of the investigational drug DDP733 in treating subjects with IBS-c. A placebo control will be utilized.

开始日期2005-09-01

申办/合作机构

Dynogen Pharmaceuticals, Inc.

100 项与 Pumosetrag 相关的临床结果

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100 项与 Pumosetrag 相关的转化医学

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100 项与 Pumosetrag 相关的专利（医药）

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6

项与 Pumosetrag 相关的文献（医药）

2014-01-01·Neurogastroenterology & Motility3区 · 医学

Novel partial 5HT3 agonist pumosetrag reduces acid reflux events in uninvestigated GERD patients after a standard refluxogenic meal: a randomized, double‐blind, placebo‐controlled pharmacodynamic study

3区 · 医学

Article

作者: Orr, W. C. ; Francis, D. D. ; DeVault, K. ; Katzka, D. ; Harmsen, W. S. ; Choung, R. S. ; Locke, G. R. ; Talley, N. J. ; Crowell, M. D. ; Zinsmeister, A. R. ; Winkle, P. J.

AbstractBackgroundLow basal lower esophageal sphincter (LES) pressure and transient LES relaxations are major causes of gastroesophageal reflux disease (GERD). Pumosetrag, a novel selective partial 5HT3 receptor agonist, showed a promising effect on reducing reflux events in health. We aimed to evaluate the effect of pumosetrag on changes in reflux episodes, lower esophageal sphincter pressure (LESP), and specific symptoms in patients with GERD receiving a refluxogenic meal.MethodsPatients with GERD, who developed heartburn and/or regurgitation after ingestion of a refluxogenic meal, were randomized to 1 of 3 dose levels of pumosetrag (0.2, 0.5, or 0.8 mg) or placebo. Before and after 7 days of treatment, patients underwent manometry, intraesophageal multichannel, intraluminal impedance and pH after a standard refluxogenic meal.Key ResultsA total of 223 patients with GERD [125 (56%) women, mean (SD) age = 36 (12) years] were enrolled. No overall treatment effects were detected for the total number of reflux episodes (acidic and weakly acidic) (p > 0.5); however, significant treatment effects (p < 0.05) on the number of acid reflux episodes were observed with lower values on pumosetrag 0.2 mg (10.8 ± 1.1), 0.5 mg (9.5 ± 1.1), and 0.8 mg (9.9 ± 1.1) compared with placebo (13.3 ± 1.1). Significant treatment effects (p < 0.05) were also observed for the percentage of time pH was <4, with less time for pumosetrag at 0.5 mg (10%) and 0.8 mg (10%) compared with placebo (16%).Conclusions & InferencesIn GERD, the partial 5HT3 agonist pumosetrag significantly reduced the rate of acid reflux events but did not result in a significant change in LESP or symptomatic improvement over a 1‐week treatment period.

2012-04-01·Life Sciences3区 · 医学

Inotropic effects of prokinetic agents with 5-HT4 receptor agonist actions on human isolated myocardial trabeculae

3区 · 医学

Article

作者: Saxena, Pramod R. ; de Maeyer, Joris H. ; Chai, Wenxia ; Maassen Van Den Brink, Antoinette ; Villalon, Carlos M. ; de Vries, Rene ; van den Bogeardt, Antoon J. ; Danser, A. H. Jan ; Schuurkes, Jan A. J. ; Chan, Kayi Y.

AIMSBesides acting as gastrointestinal prokinetic agents, 5-hydroxytryptamine(4) (5-HT(4)) receptor agonists can induce positive inotropism in human isolated atrium, but not in ventricles. We pharmacologically evaluated the gastroprokinetic 5-HT(4) receptor agonists tegaserod, prucalopride, R199715, cisapride, the cisapride metabolite norcisapride, and the 5-HT(3) receptor agonist MKC773 on human isolated myocardial trabeculae, and compared their effects with those induced by 5-HT and 5-methoxytryptamine (5-MeOT).MAIN METHODSAtrial and ventricular trabeculae were paced and changes in contractile force were studied in the absence or presence of the 5-HT(4) receptor antagonist GR113808. Partial agonism was assessed using 5-HT(4) receptor agonists as antagonists against 5-HT. To test the contribution of L-type calcium channels, the inotropic responses to 5-HT and 5-MeOT were studied in the absence or presence of verapamil.KEY FINDINGSLike 5-HT and 5-MeOT, cisapride and tegaserod, but not prucalopride, R19971 and MKC-733, induced concentration-dependent positive inotropic responses on atrial trabeculae, which were abolished by GR113808. The L-type calcium channel blocker verapamil attenuated inotropic responses to 5-HT and 5-MeOT. None of the agonists affected the contraction of left ventricular trabeculae. Concentration response curves to 5-HT were shifted to the right in the presence of prucalopride, cisapride, tegaserod and R199715, but not MKC-773.SIGNIFICANCEWe conclude that (i) inotropic responses to 5-HT and 5-MeOT seem to depend on L-type calcium channels, (ii) tegaserod and cisapride behave as partial 5-HT(4) receptor agonists, while prucalopride, norcisapride and MKC-733 cause no significant effects on human atrial trabeculae, (iii) R199715 seems to behave as a 5-HT(4) receptor antagonist.

2008-03-01·Alimentary Pharmacology & Therapeutics1区 · 医学

A novel partial 5HT3 agonist DDP733 after a standard refluxogenic meal reduces reflux events: a randomized, double‐blind, placebo‐controlled pharmacodynamic study

1区 · 医学

Article

作者: Dierkhising, R. A. ; Murray, J. A. ; Kammer, P. P. ; Zinsmeister, A. R. ; Talley, N. J. ; Choung, R. S. ; Landau, S. B. ; Ferguson, D. D. ; Nurbhai, S.

SummaryBackground DDP733, a selective partial 5HT3 receptor agonist, increases lower oesophageal sphincter pressure in experimental animal models. However, its effect on gastro‐oesophageal reflux or lower oesophageal sphincter pressure in humans remains unknown.Aim To evaluate the effect of DDP733 on reflux episodes in healthy volunteers receiving a refluxogenic meal.Methods A randomized, double‐blind, placebo‐controlled cross‐over study evaluated the pharmacodynamic effects of DDP733 (0.5, 0.8 and 1.4 mg). Healthy subjects underwent oesophageal manometry and intra‐oesophageal multichannel intraluminal impedance and pH after a refluxogenic meal.Results DDP733 0.5 mg significantly (P = 0.013) reduced the rate of reflux episodes after a refluxogenic meal from 10 (±2.2) on placebo to 6 (±1.2) on drug over a 2‐h period. DDP733 0.8 and 1.4 mg had no significant effect on reducing the number of reflux episodes. Significant differences in resting lower oesophageal sphincter pressure and the proportion of time pH was <4 (placebo minus drug) after a refluxogenic meal were not observed. No serious adverse events were reported.Conclusion In healthy subjects, the partial 5HT3 agonist DDP733 at a dose of 0.5 mg significantly reduces the rate of reflux events, but did not result in a significant change in lower oesophageal sphincter pressure at 1 h postdosing.

100 项与 Pumosetrag 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12402

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
便秘	临床3期	加拿大	Dynogen Pharmaceuticals, Inc.	2007-10-01
便秘	临床3期	美国	Dynogen Pharmaceuticals, Inc.	2007-10-01
便秘	临床3期	美国	Dynogen Pharmaceuticals, Inc.	2007-10-01
胃食管反流	临床3期	-	EDUSA Corp.	-
胃食管反流	临床3期	-	EDUSA Corp.	-
肠易激综合征	临床3期	-	EDUSA Corp.	-
肠易激综合征	临床3期	-	Mitsubishi Tanabe Pharma Corp.	-
肠易激综合征	临床3期	-	Mitsubishi Tanabe Pharma Corp.	-
肠易激综合征	临床3期	-	EDUSA Corp.	-
便秘	临床前	加拿大	Dynogen Pharmaceuticals, Inc.	2007-10-01