艾波度坦(Ibodutant) - 药物靶点：NK2R_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

NK2R

作用机制

NK2R拮抗剂(神经激肽-2-受体拮抗剂)

治疗领域

消化系统疾病其他疾病

在研适应症-

非在研适应症

腹泻肠易激综合征腹泻型肠易激综合征

原研机构

A. Menarini Industrie Farmaceutiche Riunite SRL

在研机构-

非在研机构

A. Menarini Industrie Farmaceutiche Riunite SRL

A. Menarini Asia-Pacific Holdings Pte Ltd.Rottendorf Pharma GmbH

+ [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)终止

特殊审评-

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结构

分子式C37H48N4O4S

InChIKeyYQYSVMKCMIUCHY-WJOKGBTCSA-N

CAS号522664-63-7

关联

6

项与艾波度坦相关的临床试验

NCT02320318 / Withdrawn临床3期

A 12-week Double-blind, Randomised, Placebo-controlled, Parallel Group Phase III Study, Followed by a 4-week Randomised Withdrawal Period to Evaluate the Efficacy and Safety of Oral Ibodutant 10 mg Once Daily in Female Patients With Irritable Bowel Syndrome With Diarrhoea (IBS-D).

Irritable Bowel Syndrome with diarrhoea (IBS-D) is a functional gastrointestinal disorder characterised by chronic or recurrent abdominal pain or discomfort and diarrhoea. The aim of this trial is the evaluation of the efficacy and safety of oral ibodutant 10 mg once daily as compared to placebo in women with IBS-D over a 12-week treatment period.

开始日期2015-10-01

申办/合作机构

A. Menarini Industrie Farmaceutiche Riunite SRL

NCT02107196 / Completed临床3期

A 12-Week Double-blind, Randomised, Placebo-controlled, Parallel Group Phase III Study, Followed by a 4-Week Randomised Withdrawal Period to Evaluate the Efficacy and Safety of Oral Ibodutant 10 mg Once Daily in Female Patients With Irritable Bowel Syndrome With Diarrhea

Irritable Bowel Syndrome with diarrhoea (IBS-D) is a functional gastrointestinal disorder characterised by chronic or recurrent abdominal pain or discomfort and diarrhoea. This trial aims at the evaluation of the efficacy and safety of oral ibodutant 10 mg once daily as compared to placebo in women with IBS-D over a 12-week treatment period.

开始日期2014-03-01

申办/合作机构

A. Menarini Industrie Farmaceutiche Riunite SRL

NCT02120027 / Terminated临床3期

A 52-Week, Double-blind, Randomised, Placebo-controlled, Parallel-group Phase III Study With Re-randomisations at Week 25 to Evaluate the Efficacy and Safety of Oral Ibodutant 10 mg Once Daily in Female Patients With Irritable Bowel Syndrome With Diarrhoea (IBS-D)

Irritable Bowel Syndrome with diarrhoea (IBS-D) is a functional gastrointestinal disorder characterised by chronic or recurrent abdominal pain or discomfort and diarrhoea. This trial aims at the evaluation of the efficacy and safety of oral ibodutant 10 mg once daily as compared to placebo in women with IBS-D over a 24-week treatment period.

开始日期2014-02-01

申办/合作机构

A. Menarini Industrie Farmaceutiche Riunite SRL

100 项与艾波度坦相关的临床结果

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100 项与艾波度坦相关的转化医学

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100 项与艾波度坦相关的专利（医药）

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17

项与艾波度坦相关的文献（医药）

2024-03-03·Expert Opinion on Investigational Drugs

Drugs of the future for diarrhea-predominant irritable bowel syndrome: an overview of current investigational drugs

Review

作者: Nikfar, Shekoufeh ; Mozaffari, Shilan ; Abdollahi, Mohammad

INTRODUCTIONIrritable bowel syndrome (IBS) has a significant impact on society and quality of life. Current treatments are ineffective, and new investigational drugs are necessary.AREAS COVEREDNumerous potential therapies are developing, targeting different areas such as cannabinoid signaling, opioid receptors, tachykinin (NK2) receptors, β3-adrenergic receptors, intestinal microbiota, inflammation, and 5HT receptors. Clinical trial evidence has shown that loperamide, eluxadoline, alosetron, ramosetron, bile acid sequestrants, and rifaximin can modulate GI alterations and benefit patients with IBS-D. Among the potential therapies, ibodutant, ibudilast, blautix, BOS-589, solabegron, vibegron, olorinab, ebastine, and ORP-101 have demonstrated possible effects but remain confirmed.EXPERT OPINIONIndividuals with IBS-D require cost-effective treatment options that do not impede their productivity or that of their caregivers. This is necessary for consistent healthcare and improved quality of life. Therefore, we should focus on developing new, efficient, and affordable medications for IBS-D. The government, insurers, and society must recognize this need and collaborate to ensure its fulfillment.

2020-10-01·Journal of Pharmacology and Experimental Therapeutics3区 · 医学

Gender-Related Differences of Tachykinin NK₂Receptor Expression and Activity in Human Colonic Smooth Muscle

3区 · 医学

Article

作者: Murphy, Tim V ; Drimousis, Stelina ; Markus, Irit ; Phan-Thien, Kim-Chi ; Liu, Lu ; Perera, D Shevy ; Zhang, Li

The tachykinin NK₂ receptor plays a key role in gastrointestinal motor function. Enteric neurons release neurokinin A (NKA), which activates NK₂ receptors on gastrointestinal smooth muscle, leading to contraction and increased motility. In patients with diarrhea-predominant irritable bowel syndrome, the NK₂ receptor antagonist ibodutant had a greater therapeutic effect in females than males. The present study aimed to determine whether gender influences the expression and activity of NK₂ receptors in human colonic smooth muscle. In vitro functional studies were performed to examine the contractile responses of colonic muscle strips to NKA and the selective NK₂ receptor agonist [Lys⁵,MeLeu⁹,Nle¹⁰]NKA(4-10). Contractions were also measured in the presence of ibodutant to determine its antagonistic potency. The signal transduction pathways coupled to NK₂ receptor activation were investigated using second messenger inhibitors. Western blot and fluorescent immunohistochemistry were conducted to determine the protein expression and localization of NK₂ receptors. NK₂ receptor-mediated contractility was greater in females compared with males. When against NKA, ibodutant was more potent in females. NK₂ receptor expression increased with age in females, but not in males. Phospholipase C-mediated signaling was less prominent in females compared with males, whereas Ca²⁺ sensitization via Rho kinase and protein kinase C appeared to be the dominant pathway in both genders. The distribution of NK₂ receptors in the human colon did not differ between the genders. Overall, gender differences exist in the expression and activity of NK₂ receptors in colonic smooth muscle. These gender distinctions should be considered in the therapeutic development of NK₂ receptor agents. SIGNIFICANCE STATEMENT: The tachykinin NK₂ receptor has been identified as a therapeutic target for the treatment of bowel and bladder dysfunctions. The present study has revealed gender-related variations in NK₂ receptor activity, signaling transduction pathways, antagonist potency, and changes in expression with age. These factors may underlie the gender differences in the treatment of diarrhea-predominant irritable bowel syndrome with NK₂ receptor antagonists. Our findings highlight that gender differences should be considered in the therapeutic development of NK₂ receptor agents.

2019-02-01·Journal of physiology and pharmacology : an official journal of the Polish Physiological Society4区 · 医学

The place of tachykinin NK2 receptor antagonists in the treatment diarrhea-predominant irritable bowel syndrome.

4区 · 医学

Review

作者: Fichna, J ; Malkiewicz, A ; Zielinska, M ; Storr, M ; Szymaszkiewicz, A

Tachykinins act as neurotransmitters and neuromodulators in the central and peripheral nervous system. Preclinical studies and clinical trials showed that inhibition of the tachykinin receptors, mainly NK2 may constitute a novel attractive option in the treatment of irritable bowel syndrome (IBS). In this review, we focused on the role of tachykinins in physiology and pathophysiology of gastrointestinal (GI) tract. Moreover, we summed up recent data on tachykinin receptor antagonists in the therapy of IBS. Ibodutant is a novel drug with an interesting pharmacological profile, which exerted efficacy in women with diarrhea-predominant IBS (IBS-D) in phase II clinical trials. The promising results were not replicable and confirmed in phase III of clinical trials. Ibodutant is not ready to be introduced in the pharmaceutical market and further studies on alternative NK2 antagonist are needed to make NK2 antagonists useful tools in IBS-D treatment.

100 项与艾波度坦相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	艾波度坦	-	DB12042

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
腹泻型肠易激综合征	临床3期	匈牙利	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	波兰	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	斯洛伐克	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	斯洛伐克	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	捷克	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	德国	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	捷克	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	匈牙利	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	德国	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01
腹泻型肠易激综合征	临床3期	波兰	A. Menarini Industrie Farmaceutiche Riunite SRL	2014-02-01

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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


NCT01303224 (Pubmed \| Gut) 人工标引	临床2期	腹泻型肠易激综合征	559	ibodutant	(蓋壓醖積簾鹽顧製願憲) = 鏇構衊遞繭壓齋鹽憲獵壓構廠遞衊膚醖醖願廠 (鏇製衊簾鹹糧選醖醖願 )	积极	2017-08-01
				Placebo	(蓋壓醖積簾鹽顧製願憲) = 壓鑰範鬱蓋鹹糧鏇襯膚壓構廠遞衊膚醖醖願廠 (鏇製衊簾鹹糧選醖醖願 )
NCT02120027 (IRIS-4, CTgov)	临床3期	腹泻型肠易激综合征	558	Ibodutant 10 mg (Ibodutant 10 mg)	顧蓋鑰積艱繭範鹽夢獵(憲獵簾鑰齋獵齋淵蓋鑰) = 鑰夢廠顧製窪繭齋齋艱廠衊夢鏇鹽蓋鹹遞廠艱 (範廠積壓衊遞餘衊願製, 壓鑰築遞構獵網網淵鬱 ~ 壓夢艱衊餘蓋蓋壓觸遞) 更多	-	2017-01-18
				Placebo (Placebo)	顧蓋鑰積艱繭範鹽夢獵(憲獵簾鑰齋獵齋淵蓋鑰) = 衊廠製鬱鹽鹹艱壓憲餘廠衊夢鏇鹽蓋鹹遞廠艱 (範廠積壓衊遞餘衊願製, 鬱選築鏇鑰壓築夢憲壓 ~ 鹹廠繭襯簾網鬱餘鏇夢) 更多
NCT02107196 (IRIS-3, CTgov)	临床3期	腹泻型肠易激综合征 \| 腹泻	535	Ibodutant 10 mg (Ibodutant 10 mg)	壓鹹膚願網網獵憲鹹願(廠積醖窪網繭衊積鏇醖) = 選醖構鏇餘鏇築夢襯艱蓋齋繭鑰壓構壓鏇餘蓋 (繭齋獵觸齋鬱憲獵糧製, 齋願鹹簾鑰繭範蓋餘觸 ~ 願壓廠淵繭願簾艱鑰醖) 更多	-	2016-09-27
				Placebo (Placebo)	壓鹹膚願網網獵憲鹹願(廠積醖窪網繭衊積鏇醖) = 構衊觸範鏇襯顧憲顧網蓋齋繭鑰壓構壓鏇餘蓋 (繭齋獵觸齋鬱憲獵糧製, 窪齋鹹網衊願窪繭觸襯 ~ 獵簾壓選獵膚糧簾構獵) 更多
IRIS-2 (UEGW)	临床2期	-	559	Ibodutant 1 mg	築醖鑰製襯衊製襯膚獵(鑰艱構觸襯糧觸蓋齋餘) = 鑰獵夢鹹蓋觸醖鹽廠餘鹽糧醖衊範觸鹽廠網鑰 (鑰顧願製獵餘鑰糧觸廠, Â±0.7)	积极	2015-10-01
				Ibodutant 3 mg	築醖鑰製襯衊製襯膚獵(鑰艱構觸襯糧觸蓋齋餘) = 遞範鹹夢糧淵範夢獵繭鹽糧醖衊範觸鹽廠網鑰 (鑰顧願製獵餘鑰糧觸廠, Â±0.7)
NCT01303224 (IRIS-2, CTgov)	临床2期	腹泻型肠易激综合征	565	Placebo	膚窪製壓衊襯顧構構網(鹽夢鹽鏇觸糧鏇顧構淵) = 構鑰衊簾顧繭鹽鏇齋鹽遞憲廠壓齋淵鹽構壓壓 (願願窪餘鬱構製範觸鑰, 簾製廠廠餘醖糧鹹網鑰 ~ 遞構簾艱鬱餘壓鏇壓夢) 更多	-	2013-03-25
NCT00761007 (IRIS, CTgov)	临床2期	肠易激综合征	554	Ibodutant (Ibodutant 10 mg)	獵蓋願簾衊醖鏇製鑰淵(積醖醖觸觸鑰壓構顧糧) = 蓋蓋艱範製鑰襯糧鑰願齋築廠淵襯鑰鬱積淵衊 (鏇網膚襯範鹽膚憲築糧, 鹹願選繭觸範遞製觸積 ~ 觸夢憲鹽築壓獵鬱選顧) 更多	-	2010-10-01
				Ibodutant (Ibodutant 30 mg)	獵蓋願簾衊醖鏇製鑰淵(積醖醖觸觸鑰壓構顧糧) = 淵夢艱膚鏇夢觸築顧醖齋築廠淵襯鑰鬱積淵衊 (鏇網膚襯範鹽膚憲築糧, 構顧艱網壓齋衊獵鬱醖 ~ 夢鬱觸膚選壓夢鹹醖壓) 更多