Nepadutant(Nepadutant) - 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

作用方式

拮抗剂

作用机制

NK2R拮抗剂(神经激肽-2-受体拮抗剂)

治疗领域

遗传病与畸形消化系统疾病

在研适应症-

非在研适应症

绞痛喂养不耐受胃肠道疾病

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

权益机构-

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构/序列

分子式C45H58N10O13

InChIKeyNGCNKEZHGRXHNL-WVWQGFTISA-N

CAS号183747-35-5

Sequence Code 16642011

来源: *****

关联

7

项与 Nepadutant 相关的临床试验

NCT01532518

/ Completed临床2期

A Multicenter, Open Label, Ascending 7 Day-Repeated Dose Study to Investigate Efficacy, Safety and Pharmacokinetics of Nepadutant In Infants With Feeding Intolerance

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.

开始日期2011-08-01

申办/合作机构

A. Menarini Industrie Farmaceutiche Riunite Srl

NCT01309009

/ Withdrawn临床2期

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.

开始日期2011-02-01

申办/合作机构

A. Menarini Industrie Farmaceutiche Riunite Srl

EUCTR2010-022706-41-IT

/ Not yet recruitingN/A

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

开始日期2010-11-08

申办/合作机构

Menarini Ricerche SpA

100 项与 Nepadutant 相关的临床结果

登录后查看更多信息

100 项与 Nepadutant 相关的转化医学

登录后查看更多信息

100 项与 Nepadutant 相关的专利（医药）

登录后查看更多信息

81

项与 Nepadutant 相关的文献（医药）

2025-02-01·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

作者: 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.

2021-06-14·Chemistry – An Asian Journal3区 · 化学

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

3区 · 化学

Article

作者: 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.

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: 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 项与 Nepadutant 相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	Nepadutant	-	DB12538

研发状态

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
喂养不耐受	临床2期	美国	A. Menarini Industrie Farmaceutiche Riunite Srl	2011-08-01
绞痛	临床2期	瑞典	A. Menarini Industrie Farmaceutiche Riunite Srl	2010-11-01
绞痛	临床2期	波兰	A. Menarini Industrie Farmaceutiche Riunite Srl	2010-11-01
绞痛	临床2期	俄罗斯	A. Menarini Industrie Farmaceutiche Riunite Srl	2010-11-01
绞痛	临床2期	德国	A. Menarini Industrie Farmaceutiche Riunite Srl	2010-11-01
绞痛	临床2期	俄罗斯	A. Menarini Industrie Farmaceutiche Riunite Srl	2010-11-01
绞痛	临床2期	波兰	A. Menarini Industrie Farmaceutiche Riunite Srl	2010-11-01
绞痛	临床2期	德国	A. Menarini Industrie Farmaceutiche Riunite Srl	2010-11-01
绞痛	临床2期	瑞典	A. Menarini Industrie Farmaceutiche Riunite Srl	2010-11-01
胃肠道疾病	临床2期	美国	A. Menarini Industrie Farmaceutiche Riunite Srl	2008-03-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01258153 (no-cry, CTgov)	临床2期	绞痛	115	Nepadutant oral solution (Nepadutant Low Dose)	夢糧廠願艱蓋觸鹽鬱糧(製願廠積淵製鑰夢鹹蓋) = 遞鹽遞艱艱齋齋範構衊觸網製構淵積醖範鑰憲 (齋簾蓋鬱鹽糧壓鹽襯壓, 繭膚醖餘積鏇鏇遞範艱 ~ 艱築鹹醖廠齋衊積窪網) 更多	-	2015-06-10
				Nepadutant oral solution (Nepadutant High Dose)	夢糧廠願艱蓋觸鹽鬱糧(製願廠積淵製鑰夢鹹蓋) = 顧範積選願選蓋衊鏇艱觸網製構淵積醖範鑰憲 (齋簾蓋鬱鹽糧壓鹽襯壓, 淵淵獵糧壓鬱衊餘積憲 ~ 積蓋鑰衊積構鬱遞網膚) 更多
NCT00655083 (of Nepadutant in Infants \| Oral absorption, CTgov)	临床1期	绞痛 \| 胃肠道疾病	21	Nepadutant (Nepadutant 0.1 mg/kg)	鬱鏇選鹽夢簾窪鹹鹹憲(鏇遞顧艱醖衊醖蓋齋簾) = 簾糧鏇選範膚艱窪築廠醖鏇簾醖膚遞獵餘憲膚 (簾簾襯遞網衊淵顧餘鹹, 網廠鹹鏇餘艱範憲築醖 ~ 醖鬱壓簾製廠衊鏇壓糧) 更多	-	2010-08-25
				Nepadutant (Nepadutant 0.5 mg/kg)	鬱鏇選鹽夢簾窪鹹鹹憲(鏇遞顧艱醖衊醖蓋齋簾) = 範淵膚遞襯積築廠獵鏇醖鏇簾醖膚遞獵餘憲膚 (簾簾襯遞網衊淵顧餘鹹, 鏇製醖廠壓鹽餘鏇窪構 ~ 憲醖遞窪鹽蓋襯糧觸積) 更多