Tarafenacin(Tarafenacin) - 药物靶点：M3 receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

M3 receptor

作用机制

M3 receptor拮抗剂(毒蕈碱型乙酰胆碱受体M3拮抗剂)

治疗领域

泌尿生殖系统疾病

在研适应症-

非在研适应症

膀胱过度活动症综合征膀胱过度活动症尿失禁

原研机构

Laboratorios Salvat SA

在研机构-

非在研机构

Kwang Dong Pharmaceutical Co., Ltd.

Editorial Salvat SL

Laboratorios Salvat SA

最高研发阶段无进展临床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C21H20F4N2O2

InChIKeyUXZDMXYRRQJIBJ-IBGZPJMESA-N

CAS号385367-47-5

关联

3

项与 Tarafenacin 相关的临床试验

KCT0000207 / Recruiting临床2期

A PROSPECTIVE, MULTI-CENTRE, PLACEBO CONTROLLED, RANDOMIZED, DOUBLE BLIND, PHASE II STUDY TO COMPARE THE EFFICACY AND TOLERABILITY OF TARAFENACIN 0.2 MG AND TARAFENACIN 0.4 MG TO PLACEBO ADMINISTERED AS ORAL DAILY DOSE FOR THREE MONTHS IN PATIENTS SUFFERING FROM OVERACTIVE BLADDER

开始日期2011-09-26

申办/合作机构

Kwang Dong Pharmaceutical Co., Ltd.

NCT01458197 / Completed临床2期

A Prospective, Multi-center, Placebo-controlled, Randomized, Double-blind, Phase 2 Study to Compare the Efficacy and Tolerability of Tarafenacin 0.2 mg and Tarafenacin 0.4 mg to Placebo Administered as Oral Daily Dose for Three Months in Patients Suffering From Overactive Bladder.

Primary Objective:
To evaluate the dose-response relationship of tarafenacin on efficacy.
Secondary Objectives:
To compare 12 weeks' efficacy of different doses of tarafenacin to that of placebo in patients suffering from Overactive Bladder. .
To compare the tolerability of different doses of tarafenacin to that of placebo in patients suffering from Overactive Bladder. .

开始日期2011-09-01

申办/合作机构

Kwang Dong Pharmaceutical Co., Ltd.

NCT00507169 / Completed临床2期

SVT-40776 in Patients Suffering From Overactive Bladder Syndrome

The study will examine which dose of SVT-40776 is best in terms of efficacy, safety and tolerability compared to placebo and tolterodine

开始日期2006-09-01

申办/合作机构

Editorial Salvat SL

100 项与 Tarafenacin 相关的临床结果

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100 项与 Tarafenacin 相关的转化医学

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100 项与 Tarafenacin 相关的专利（医药）

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6

项与 Tarafenacin 相关的文献（医药）

2022-01-01·Current Therapeutic Research

Drugs Currently Undergoing Preclinical or Clinical Trials for the Treatment of Overactive Bladder: A Review

Review

作者: Joseph, Silvia ; Peedicayil, Jacob ; Maria, Steffi A

BackgroundOveractive bladder (OAB) is a common clinical condition for which current drug treatment comprises drugs blocking the cholinergic nerve supply, or augmenting the adrenergic nerve supply, to the detrusor muscle of the urinary bladder. Current treatments have drawbacks, including lack of efficacy and the development of adverse effects in some patients. Hence, new and better drugs for treating OAB will be clinically useful.ObjectiveThis review is meant to provide information on drugs currently undergoing preclinical or clinical trials for the treatment of OAB published in journal articles or elsewhere.MethodsThe cited articles were retrieved from PubMed and Google Scholar from January 1, 1990, to December 31, 2021. The search terms used were contraction or contractility, detrusor, inhibition, isolated or in vitro, in vivo, overactive bladder, and relaxant effect or relaxation.ResultsThere are 4 classes of new drugs under various stages of development for the treatment of OAB. These are drugs acting on the autonomic nerve supply to the detrusor muscle of the urinary bladder that include the anticholinergics tarafenacin and afacifenacin and the β₃ adrenoceptor agonists solabegron and ritobegron; drugs acting on ion channels in the detrusor muscle (eg, potassium channel openers and calcium channel blockers), drugs acting on cellular enzymes like phosphodiesterase-5 inhibitors and Rho kinase inhibitors, and drugs acting on miscellaneous targets (eg, pregabalin and trimetazidine).ConclusionsDrugs currently used to treat OAB target only the cholinergic and adrenergic cellular signalling pathways. There are many other drugs under trial targeting other cellular pathways that may be useful for treating OAB. Their approval for clinical use might improve the treatment of patients with OAB. (Curr Ther Res Clin Exp. 2022; 83:XXX-XXX).

2021-12-01·Digestive Diseases and Sciences3区 · 医学

7,8-Dihydroxyflavone Enhanced Colonic Cholinergic Contraction and Relieved Loperamide-Induced Constipation in Rats

3区 · 医学

Article

作者: Qu, Zhiqiang ; Sun, Yongye ; Luan, Xiao ; He, Baoguo ; Wang, Bingxiang ; Han, Qingfang ; He, Juan ; Han, Lei ; Xu, Luo ; Ma, Li

BACKGROUNDWhether 7,8-dihydroxyflavone (7,8-DHF), a tyrosine kinase receptor B (TrkB) agonist, modulates colonic smooth muscle motility and/or alleviates constipation has not yet been studied.AIMSHere, we aimed to determine how 7,8-DHF influences carbachol (CCh)-stimulated contraction of colonic strips and the in vivo effect of 7,8-DHF on constipation.METHODSMuscle strips were isolated from rat colons for recording contractile tension and performing western blotting. Constipation was induced in rats with loperamide.RESULTSAlthough it specifically activated TrkB, 7,8-DHF applied alone neither activated PLCγ1 in the colonic strips nor induced colonic strip contraction. However, 7,8-DHF enhanced CCh-stimulated PLCγ1 activation and strip contraction. The PLCγ1 antagonist U73122 suppressed both CCh-stimulated and 7,8-DHF-enhanced/CCh-stimulated contraction. While clarifying the underlying mechanism, we revealed that 7,8-DHF augmented muscarinic M3 receptor expression in the colonic strips. The M3-selective antagonist tarafenacin specifically inhibited the 7,8-DHF-enhanced/CCh-stimulated contraction of the colonic strips. Since 7,8-DHF increased Akt phosphorylation, and LY294002 (an antagonist of PI3K upstream of Akt) dramatically inhibited both 7,8-DHF-augmented M3 expression and 7,8-DHF-enhanced/CCh-stimulated contractions, we assumed that 7,8-DHF/TrkB/Akt was associated with the modulation of M3 expression in the colonic strips. ANA-12, a specific TrkB antagonist, not only inhibited TrkB activation by 7,8-DHF but also suppressed 7,8-DHF-enhanced cholinergic contraction, 7,8-DHF/CCh-mediated activation of PLCγ1/Akt, and M3 overexpression in colonic strips. In vivo 7,8-DHF, also by promoting intestinal motility and M3 expression, significantly alleviated loperamide-induced functional constipation in rats.CONCLUSIONSOur results suggest that 7,8-DHF regulates colonic motility possibly via a TrkB/Akt/M3 pathway and may be applicable for alleviating constipation.

2016-07-02·Expert Opinion on Pharmacotherapy3区 · 医学

Current and future pharmacotherapy for treating overactive bladder

3区 · 医学

Review

作者: Robinson, Dudley ; Thiagamoorthy, Ganesh ; Cardozo, Linda

INTRODUCTIONDrugs which prevent acetylcholine mediated involuntary detrusor contractions are the mainstay of overactive bladder(OAB) treatment but there are now several alternative therapeutic options available.AREAS COVEREDCurrent and future drug therapies for OAB are highlighted. These include novel antimuscarinic molecules (imidafenacin and tarafenacin); novel combination therapies with β3-adrenoceptor agonists or muscarinic agonists (tolenix) and a novel vaginal delivery method for oxybutynin. β3-adrenoceptor agonists(β3-AR) have been shown to be efficiacious in the management of OAB. The evidence supporting the first licensed β3-AR agonist, mirabegron, is assessed, as well as other putative β3-AR agonists in development such as solabegron, ritobegron, aryloxypropanolamine, TRK-380, and CL 316,243. The role of vaginal oestrogen is highlighted followed by a detailed analysis of botulinum-A toxin.EXPERT OPINIONAnticholinergics were the first OAB drug therapy on the market and have the largest dataset available. Despite obvious limitations, these are still first line medical therapy. There are a number of new OAB therapies under investigation and we await their contribution to the management armamentarium. Other novel drugs have been licenced and these are now vying for pole position in the treatment algorithm. One must exercise caution however until the long term effects of any new medicines are known.

100 项与 Tarafenacin 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
膀胱过度活动症	临床2期	韩国	Kwang Dong Pharmaceutical Co., Ltd.	2011-09-01
膀胱过度活动症综合征	临床2期	-	Editorial Salvat SL	2006-09-01
尿失禁	临床2期	-	Kwang Dong Pharmaceutical Co., Ltd.	-
尿失禁	临床2期	-	Laboratorios Salvat SA	-