Delving into the Latest Updates on Ibodutant with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

NK2R

Mechanism

NK2R antagonists(Neurokinin 2 receptor antagonists)

Therapeutic Areas

Digestive System DisordersOther Diseases

Active Indication-

Inactive Indication

DiarrheaIrritable Bowel SyndromeIrritable bowel syndrome with diarrhea

Originator Organization

A. Menarini Industrie Farmaceutiche Riunite SRL

Active Organization-

Inactive Organization

A. Menarini Industrie Farmaceutiche Riunite SRLRottendorf Pharma GmbH

A. Menarini Asia-Pacific Holdings Pte Ltd.

+ [2]

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

Structure

Molecular FormulaC37H48N4O4S

InChIKeyYQYSVMKCMIUCHY-WJOKGBTCSA-N

CAS Registry522664-63-7

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.

Start Date01 Oct 2015

Sponsor / Collaborator

A. Menarini Industrie Farmaceutiche Riunite SRL

NCT02107196 / CompletedPhase 3

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.

Start Date01 Mar 2014

Sponsor / Collaborator

A. Menarini Industrie Farmaceutiche Riunite SRL

NCT02120027 / TerminatedPhase 3

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.

Start Date01 Feb 2014

Sponsor / Collaborator

A. Menarini Industrie Farmaceutiche Riunite SRL

100 Clinical Results associated with Ibodutant

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100 Translational Medicine associated with Ibodutant

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100 Patents (Medical) associated with Ibodutant

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17

Literatures (Medical) associated with Ibodutant

03 Mar 2024·Expert Opinion on Investigational Drugs

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

Review

Author: 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.

01 Oct 2020·Journal of Pharmacology and Experimental TherapeuticsQ3 · MEDICINE

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

Q3 · MEDICINE

Article

Author: 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.

01 Feb 2019·Journal of physiology and pharmacology : an official journal of the Polish Physiological SocietyQ4 · MEDICINE

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

Q4 · MEDICINE

Review

Author: 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 Deals associated with Ibodutant

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Ibodutant	-	DB12042

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Irritable bowel syndrome with diarrhea	Phase 3	PL	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	SE	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	LV	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	CZ	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	DE	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	DE	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	PL	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	LV	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	SE	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014
Irritable bowel syndrome with diarrhea	Phase 3	CZ	A. Menarini Industrie Farmaceutiche Riunite SRL	01 Feb 2014

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01303224 (Pubmed \| Gut) Manual	Phase 2	Irritable bowel syndrome with diarrhea	559	ibodutant	(jmujorkvfv) = krhdrapodx vhonawxwto (vgqiumvhcz )	Positive	01 Aug 2017
				Placebo	(jmujorkvfv) = orswmjnzwi vhonawxwto (vgqiumvhcz )
NCT02120027 (IRIS-4, CTgov)	Phase 3	Irritable bowel syndrome with diarrhea	558	Ibodutant 10 mg (Ibodutant 10 mg)	mlpukjywjd(mxykvscnkf) = kaptdwfpwg mdcwduiuvs (ixsdmjtpig, gvwcfthbel - iamundsxsd) View more	-	18 Jan 2017
				Placebo (Placebo)	mlpukjywjd(mxykvscnkf) = wiajvwsplw mdcwduiuvs (ixsdmjtpig, uublpfsttf - iuojrrwqzv) View more
NCT02107196 (IRIS-3, CTgov)	Phase 3	Irritable bowel syndrome with diarrhea \| Diarrhea	535	Ibodutant 10 mg (Ibodutant 10 mg)	duosuilgnr(jsccehnjfl) = slrjhgkltb fyvuxrtgon (jeuflcyegx, wcimxgjjyu - yhzkravevb) View more	-	27 Sep 2016
				Placebo (Placebo)	duosuilgnr(jsccehnjfl) = uxqskbpfvf fyvuxrtgon (jeuflcyegx, pjuthcokkq - hahhbutros) View more
NCT01303224 (IRIS-2, CTgov)	Phase 2	Irritable bowel syndrome with diarrhea	565	Placebo	ejlbahfepy(rhuccycrat) = clrfeyzpsd wqmkowujfv (mchchzpgdv, dnfjzprnhs - sufxiohjgv) View more	-	25 Mar 2013
NCT00761007 (IRIS, CTgov)	Phase 2	Irritable Bowel Syndrome	554	Ibodutant (Ibodutant 10 mg)	bnhbemjvnt(imeygohyeb) = batblmfqvg mxtxwskwle (wgnwuyoikx, lcxgmwcylm - lqqobumgiq) View more	-	01 Oct 2010
				Ibodutant (Ibodutant 30 mg)	bnhbemjvnt(imeygohyeb) = yxrlvninpl mxtxwskwle (wgnwuyoikx, uvdkuxyfur - ozwrncbrzp) View more