Delving into the Latest Updates on Nepadutant with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

NK2R

Action

antagonists

Mechanism

NK2R antagonists(Neurokinin 2 receptor antagonists)

Therapeutic Areas

Congenital DisordersDigestive System Disorders

Active Indication-

Inactive Indication

ColicFeeding intoleranceGastrointestinal Diseases

Originator Organization

A. Menarini Industrie Farmaceutiche Riunite Srl

Active Organization-

Inactive Organization

A. Menarini Industrie Farmaceutiche Riunite Srl

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC45H58N10O13

InChIKeyNGCNKEZHGRXHNL-WVWQGFTISA-N

CAS Registry183747-35-5

Sequence Code 16642011

Source: *****

The present pilot study is aimed to obtain preliminary data on the effect of three ascending oral dose levels of nepadutant on the relief of symptoms associated with feeding intolerance. In addition, the assessment of drug exposure (PK assessment) will provide additional information on the dose-effect relationship, thus supporting the dose selection and dosing schedule in the future studies.

Start Date01 Aug 2011

Sponsor / Collaborator

A. Menarini Industrie Farmaceutiche Riunite Srl

NCT01309009

/ WithdrawnPhase 2

Double-blind, Randomised, Placebo-controlled, Parallel Group Pilot Study to Evaluate the Efficacy and Safety of Oral Administration of Nepadutant in Infant Colic Babies Not Responder to Conventional Treatments

This phase IIa study is designed as a multi-centre, single country, randomised, double-blind, placebo controlled study in three parallel groups, with the aim to evaluate the efficacy and safety of Nepadutant given at two oral doses once daily for seven days in comparison to placebo in the treatment of infantile colic.

Start Date01 Feb 2011

Sponsor / Collaborator

A. Menarini Industrie Farmaceutiche Riunite Srl

EUCTR2010-022706-41-IT

/ Not yet recruitingNot Applicable

Double-blind, randomised, placebo-controlled, parallel group pilot study to evaluate the efficacy and safety of oral administration of Nepadutant in infant colic babies not responder to conventional treatments - NOCRY-a

Start Date08 Nov 2010

Sponsor / Collaborator

Menarini Ricerche SpA

100 Clinical Results associated with Nepadutant

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100 Translational Medicine associated with Nepadutant

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100 Patents (Medical) associated with Nepadutant

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81

Literatures (Medical) associated with Nepadutant

01 Feb 2025·British Journal of Clinical Pharmacology

Population pharmacokinetic and dose–response models of nepadutant, a selective antagonist of the NK₂ receptors, in infants with colic

Article

Author: Jönsson, Siv ; Tagliavini, Alessia ; Pellacani, Andrea ; Piana, Chiara ; Werkstetter, Katharina ; Koletzko, Sibylle ; Capriati, Angela ; Mazzei, Paolo ; Bouchene, Salim ; Jonsson, E. Niclas ; Borella, Elisa ; Karlsson, Mats O.

AimsThe aim of the current analyses was to develop a population pharmacokinetic model for nepadutant in infants with colic, and a pharmacokinetic‐pharmacodynamic model based on observations of duration of crying and fussing following oral nepadutant administration in infants (3–25 weeks) with colic.MethodsThe models were developed based on data obtained at baseline and following treatment with placebo, nepadutant 0.1 mg/kg or nepadutant 0.5 mg/kg administered for 7 days. A continuous response variable, duration of crying and fussing in minutes within 2 h interval, was assembled based on records from “baby's day” diary.ResultsThe pharmacokinetics of nepadutant was described by a one‐compartment model with first‐order absorption and elimination with body weight as a structural covariate incorporated allometrically. For an infant weighing 5.3 kg, the estimated apparent clearance was 68.6 L/h (12% relative standard error) and exhibited large variability (78% coefficient of variation). The pharmacokinetic‐pharmacodynamic model described (i) a circadian rhythm in the response with lowest and highest observations at 4 a.m. and 9 p.m., respectively, (ii) a placebo effect increasing and flattening out with time in an exponential manner, and (iii) a statistically significant (P < .01) linearly increasing response with dose. The observed and model predicted relative change in response from baseline was −35% and −28% (95% prediction interval −36%; −19%) following placebo, and −44% and −36% (−46%; −27%) after 0.5 mg/kg.ConclusionsPopulation pharmacokinetic and dose–response models were successfully developed characterizing the available nepadutant pharmacokinetics and duration of crying and fussing data in infants.

14 Jun 2021·Chemistry – An Asian JournalQ3 · CHEMISTRY

Atomistic De‐novo Inhibitor Generation‐Guided Drug Repurposing for SARS‐CoV‐2 Spike Protein with Free‐Energy Validation by Well‐Tempered Metadynamics

Q3 · CHEMISTRY

Article

Author: Singh, Reman K. ; Chowdhury, Rituparno ; Sai Sreyas Adury, Venkata ; Vijay, Amal ; Mukherjee, Arnab

AbstractComputational drug design is increasingly becoming important with new and unforeseen diseases like COVID‐19. In this study, we present a new computational de novo drug design and repurposing method and applied it to find plausible drug candidates for the receptor binding domain (RBD) of SARS‐CoV‐2 (COVID‐19). Our study comprises three steps: atom‐by‐atom generation of new molecules around a receptor, structural similarity mapping to existing approved and investigational drugs, and validation of their binding strengths to the viral spike proteins based on rigorous all‐atom, explicit‐water well‐tempered metadynamics free energy calculations. By choosing the receptor binding domain of the viral spike protein, we showed that some of our new molecules and some of the repurposable drugs have stronger binding to RBD than hACE2. To validate our approach, we also calculated the free energy of hACE2 and RBD, and found it to be in an excellent agreement with experiments. These pool of drugs will allow strategic repurposing against COVID‐19 for a particular prevailing conditions.

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: Malkiewicz, A ; Fichna, J ; 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 Nepadutant

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Nepadutant	-	DB12538

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Feeding intolerance	Phase 2	United States	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Aug 2011
Colic	Phase 2	Sweden	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Nov 2010
Colic	Phase 2	Poland	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Nov 2010
Colic	Phase 2	Russia	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Nov 2010
Colic	Phase 2	Germany	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Nov 2010
Colic	Phase 2	Russia	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Nov 2010
Colic	Phase 2	Poland	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Nov 2010
Colic	Phase 2	Germany	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Nov 2010
Colic	Phase 2	Sweden	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Nov 2010
Gastrointestinal Diseases	Phase 2	United States	A. Menarini Industrie Farmaceutiche Riunite Srl	01 Mar 2008

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01258153 (no-cry, CTgov)	Phase 2	Colic	115	Nepadutant oral solution (Nepadutant Low Dose)	yinlhpppzi(cqpakegcee) = iptzpsrakn ymorbknvoy (ymwfszjtdg, tznjinevhp - wwagsnzbue) View more	-	10 Jun 2015
				Nepadutant oral solution (Nepadutant High Dose)	yinlhpppzi(cqpakegcee) = pknhpcjhkc ymorbknvoy (ymwfszjtdg, ygtrmvpeqf - hmxsdzlnzz) View more
NCT00655083 (of Nepadutant in Infants \| Oral absorption, CTgov)	Phase 1	Colic \| Gastrointestinal Diseases	21	Nepadutant (Nepadutant 0.1 mg/kg)	wftweorsnu(ttkdevsfzw) = ylxonkffzz edscqnqarc (svkiiouboe, ihvyobvnoc - lwohwefcsg) View more	-	25 Aug 2010
				Nepadutant (Nepadutant 0.5 mg/kg)	wftweorsnu(ttkdevsfzw) = fzgdhddlbh edscqnqarc (svkiiouboe, lymhehrbuo - wysnfwyfdd) View more