Page last updated: 2024-12-11

men 11420

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID9876321
CHEMBL ID1908318
MeSH IDM0280213

Synonyms (13)

Synonym
cyclo(n-(2-acetamido-2-deoxy-beta-d-glucopyranosyl)-l-asparaginyl-l-alpha-aspartyl-l-tryptophyl-l-phenylalanyl-l-2,3-diaminopropionyl-l-leucyl),cyclic(2-5)-peptide
nepadutant [inn]
men-11,420
men 11420
nepadutant
183747-35-5
cyclo(n-(2-acetamido-2-deoxy-beta-d-glucopyranosyl)-l-asparginyl-l-alpha-aspartyl-l-tryptophyl-l-phenylalanyl-l-2,3-diaminopropionyl-l-leucyl), cyclic(2-5)-peptide.
unii-xw59tyl1xh
xw59tyl1xh ,
CHEMBL1908318
cyclo(n-(2-acetamido-2-deoxy-.beta.-d-glucopyranosyl)-l-asparaginyl-l-.alpha.-aspartyl-l-tryptophyl-l-phenylalanyl-l-2,3-diaminopropionyl-l-leucyl),cyclic(2-5)-peptide
DB12538
n-[(2r,3r,4r,5s,6r)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]-2-[(1s,4s,7s,10s,13s,16s)-4-benzyl-7-(1h-indol-3-ylmethyl)-16-(2-methylpropyl)-3,6,9,12,15,18,21-heptaoxo-2,5,8,11,14,17,20-heptazabicyclo[8.8.4]docosan-13-yl]acetamide

Research Excerpts

Overview

Mens 11420 (nepadutant) is a potent, selective and competitive antagonist of tachykinin NK2 receptors.

ExcerptReferenceRelevance
"1. MEN 11420 (nepadutant) is a potent, selective and competitive antagonist of tachykinin NK2 receptors. "( A novel tachykinin NK2 receptor antagonist prevents motility-stimulating effects of neurokinin A in small intestine.
Hellström, PM; Lördal, M; Maggi, CA; Navalesi, G; Theodorsson, E, 2001
)
0.93

Treatment

ExcerptReferenceRelevance
"Treatment with MEN 11420 significantly reduced the acute bronchoconstriction induced by antigen, in terms of lung resistance."( Effect of antagonists for NK(2)and B(2) receptors on antigen-induced airway responses in allergic rabbits.
Douglas, GJ; Matsumoto, T; Page, CP; Paul, W; Whalley, ET; Woisin, FE, 2000
)
0.65

Pharmacokinetics

ExcerptReferenceRelevance
" The mean plasma half-life (44 min) and AUC value (285 micrograms."( Pharmacokinetics of the bicyclic peptide tachykinin NK2 receptor antagonist MEN 11420 (nepadutant) in rats.
Criscuoli, M; Guelfi, M; Lippi, A; Maggi, CA; Santicioli, P, 1998
)
0.53
"Tachykinin NK2 receptor antagonists could reduce motility and symptoms during gastrointestinal diseases characterized by local inflammation such as diarrhea or colitis; however, how these conditions change pharmacodynamic and pharmacokinetic characteristics of NK2 receptor antagonists is unknown."( Nepadutant pharmacokinetics and dose-effect relationships as tachykinin NK2 receptor antagonist are altered by intestinal inflammation in rodent models.
Bueno, L; Carini, F; Crea, A; Criscuoli, M; D'Aranno, V; Fioramonti, J; Giuliani, S; Lecci, A; Maggi, CA; Marinoni, E; Tramontana, M, 2001
)
0.31

Bioavailability

ExcerptReferenceRelevance
" The absolute bioavailability of MEN 11420 after intranasal (1 mg/kg) or ip (1 mg/kg) administration was virtually complete."( Pharmacokinetics of the bicyclic peptide tachykinin NK2 receptor antagonist MEN 11420 (nepadutant) in rats.
Criscuoli, M; Guelfi, M; Lippi, A; Maggi, CA; Santicioli, P, 1998
)
0.81
" In the castor oil model, the oral/intraduodenal bioavailability of nepadutant was also determined."( Nepadutant pharmacokinetics and dose-effect relationships as tachykinin NK2 receptor antagonist are altered by intestinal inflammation in rodent models.
Bueno, L; Carini, F; Crea, A; Criscuoli, M; D'Aranno, V; Fioramonti, J; Giuliani, S; Lecci, A; Maggi, CA; Marinoni, E; Tramontana, M, 2001
)
0.31
" Nepadutant did not affect the basal intestinal propulsion and showed a good oral bioavailability and long duration of action."( Influence of tachykinin NK2 receptors on intestinal sensitivity and motility in newborn rats.
Evangelista, S; Girod, V; Giuliani, S; Maggi, CA; Manzini, S; Robelet, S; Tramontana, M, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)KD/Ki0.00740.00740.02000.0400AID68771
Substance-K receptorHomo sapiens (human)KD/Ki0.46230.00040.03491.0700AID163136; AID163138; AID202474; AID202475; AID202476; AID217944; AID219264; AID219265; AID219266; AID219919; AID219920; AID219925; AID219926; AID219929; AID219932; AID219934; AID219935; AID43022; AID68754; AID68756; AID68771; AID80500; AID93319
Histamine H2 receptorCavia porcellus (domestic guinea pig)KD/Ki0.01150.01150.04570.0800AID80500
E-selectinRattus norvegicus (Norway rat)KD/Ki0.00150.00150.00250.0035AID202476
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Processvia Protein(s)Taxonomy
negative regulation of endothelial cell proliferationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte chemotaxis involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte migration involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
humoral immune responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of bone mineralizationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
dendritic cell migrationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
glucose homeostasisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of fat cell differentiationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of insulin secretionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of vascular wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory response to woundingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cytokine production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cellular response to oxidative stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene A4 biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of sprouting angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cellPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxin biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
muscle contractionSubstance-K receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-K receptorHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionSubstance-K receptorHomo sapiens (human)
intestine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionSubstance-K receptorHomo sapiens (human)
operant conditioningSubstance-K receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-K receptorHomo sapiens (human)
positive regulation of monoatomic ion transportSubstance-K receptorHomo sapiens (human)
positive regulation of smooth muscle contractionSubstance-K receptorHomo sapiens (human)
response to electrical stimulusSubstance-K receptorHomo sapiens (human)
prolactin secretionSubstance-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
arachidonate 5-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
iron ion bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
protein bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
hydrolase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
tachykinin receptor activitySubstance-K receptorHomo sapiens (human)
protein bindingSubstance-K receptorHomo sapiens (human)
substance K receptor activitySubstance-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
extracellular regionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular spacePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelope lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nucleoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
cytosolPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear matrixPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear membranePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
secretory granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
perinuclear region of cytoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
ficolin-1-rich granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
plasma membraneSubstance-K receptorHomo sapiens (human)
sperm flagellumSubstance-K receptorHomo sapiens (human)
sperm headSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
plasma membraneSubstance-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID43025Binding affinity against C167A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand; UB is Undetectable Binding2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID144213Binding affinity against N110A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand; UB is Undetectable Binding2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219264Binding affinity against wild type human Wild-type tachykinin receptor 2 (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID217947Binding affinity against W263A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand; UB is Undetectable Binding2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219929Binding affinity against Y269A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID68771Binding affinity against F293A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219920Binding affinity against Y169A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID80500Binding affinity against H198A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219926Binding affinity against Y266F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID217944Binding affinity against W263A human neurokinin-2 receptor (hNK-2R) using [3H]SR-48,968 as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219932Binding affinity against Y269F human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219919Binding affinity against Y107A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219934Binding affinity against Y289F human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219928Binding affinity against Y266F human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand; UB is Undetectable Binding2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219265Binding affinity against wild-type human Wild-type tachykinin receptor 2 (hNK-2R) using [125I]-NKA as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219935Binding affinity against Y289T human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID208388Binding affinity against T171A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand; UB is undetectable binding2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID93319Binding affinity against I202F human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID43022Binding affinity against C167A human neurokinin-2 receptor (hNK-2R) using [3H]SR-48,968 as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219925Binding affinity against Y206F human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID68756Binding affinity against F168A human neurokinin-2 receptor (hNK-2R) using [3H]-nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID219266Binding affinity against wild-type human Wild-type tachykinin receptor 2 (hNK-2R) using [3H]-SR-48,968 as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID163138Binding affinity against Q166A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID163136Binding affinity against Q109A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID202474Binding affinity against S164A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID202476Binding affinity against S170A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID68754Binding affinity against F112A human neurokinin-2 receptor (hNK-2R) using [3H]nepadutant as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
AID202475Binding affinity against S170A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (49)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's15 (30.61)18.2507
2000's32 (65.31)29.6817
2010's2 (4.08)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.32

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.32 (24.57)
Research Supply Index3.95 (2.92)
Research Growth Index4.27 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (4.08%)5.53%
Reviews2 (4.08%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other45 (91.84%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Multicenter, Open Label, Ascending 7 Day-Repeated Dose Study to Investigate Efficacy, Safety and Pharmacokinetics of Nepadutant In Infants With Feeding Intolerance [NCT01532518]Phase 227 participants (Actual)Interventional2011-08-31Completed
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 [NCT01309009]Phase 20 participants (Actual)Interventional2011-02-28Withdrawn
Double-blind, Randomised, Placebo-controlled, Parallel Group Study to Evaluate the Efficacy and Safety of Oral Administration of Nepadutant in Infant Colic [NCT01258153]Phase 2115 participants (Actual)Interventional2010-11-30Completed
Pilot Study to Evaluate the Oral Absorption, Safety, and Tolerability of Nepadutant Administered as Single Oral Doses to Infants With Colic and Other Functional Gastrointestinal Disorders [NCT00655083]Phase 121 participants (Actual)Interventional2008-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00655083 (4) [back to overview]Drug Concentration Measurement in the Urine Collected by Diapers Along 24 Hours Post Dose and One Week After Dose in All Treated Infants and by Age and Dose Subgroups.
NCT00655083 (4) [back to overview]Number of Adverse Events After Administration of Single Oral Doses up to 0.5 mg/kg of Nepadutant in Infants.
NCT00655083 (4) [back to overview]Drug Concentration Measurement in the Urine Collected by Diapers Along 24 Hours Post Dose and One Week After Dose in All Treated Infants and by Age and Dose Subgroups.
NCT00655083 (4) [back to overview]Number of Adverse Events After Administration of Single Oral Doses up to 0.5 mg/kg of Nepadutant in Infants.
NCT01258153 (6) [back to overview]Absolute Change in the Overall Parental Judgment After the First Dose of Treatment Versus Baseline
NCT01258153 (6) [back to overview]Absolute Change in the Overall Parental Judgment After Treatment Discontinuation Versus Baseline
NCT01258153 (6) [back to overview]Absolute Change in the Overall Parental Judgment at the End of Treatment Versus Baseline
NCT01258153 (6) [back to overview]Percentage of 'Responder' Babies at the End of Treatment Period.
NCT01258153 (6) [back to overview]Safety and Tolerability Will be Assessed in Terms of Frequency and Severity of AEs as Well as Frequency of Clinically Significant Changes in Physical Examination and Lab Test.
NCT01258153 (6) [back to overview]Absolute Change of the Mean Daily Crying and Fussing Time for Three Consecutive Days While on Treatment Versus Baseline.
NCT01532518 (10) [back to overview]A Population Pharmacokinetic Analysis to Characterize the Plasma Concentration-time Course for Nepadutant in Infant With Colics From NIC-04
NCT01532518 (10) [back to overview]A Population Pharmacokinetic Analysis to Characterize the Plasma Concentration-time Course for Nepadutant in Infant With Colics From NIC-04
NCT01532518 (10) [back to overview]A Population Pharmacokinetic Analysis to Characterize the Plasma Concentration-time Course for Nepadutant in Infant With Colics From NIC-04
NCT01532518 (10) [back to overview]A Population Pharmacokinetic Analysis to Characterize the Plasma Concentration-time Course for Nepadutant in Infant With Colics From NIC-04
NCT01532518 (10) [back to overview]I-GERQ-R Score Changes vs Baseline (Visit 2) by First Dose Level (0.1mg/kg and 0.5mg/kg).
NCT01532518 (10) [back to overview]I-GERQ-R Score Changes vs Visit 3 by Second Dose Level (0.5mg/kg and 1mg/kg).
NCT01532518 (10) [back to overview]The Absolute Differences of I-GERQ-R Total Score at V3 (End of First Week of Treatment) Respect to the Baseline (V2).
NCT01532518 (10) [back to overview]The Absolute Differences of I-GERQ-R Total Score at V4 (End of 2nd Week of Treatment) Respect to V3 (End of 1st Week of Treatment).
NCT01532518 (10) [back to overview]The Absolute Differences of I-GERQ-R Total Score at V5 (Follow-up) Respect to V2 (Baseline).
NCT01532518 (10) [back to overview]Incidence and Severity of AEs_ Number of Adverse Events by Treatment Dose Level

Drug Concentration Measurement in the Urine Collected by Diapers Along 24 Hours Post Dose and One Week After Dose in All Treated Infants and by Age and Dose Subgroups.

Nepadutant was measured in the 24-h urine collection post both doses (0.1 and 0.5 mg/kg dose), in the age stratum 18-24 weeks, using urinary collection/extraction from pre-weighed special fiber based diapers. (NCT00655083)
Timeframe: 24 hours

Interventionng (Mean)
Nepadutant 0.1 mg/kg1127

[back to top]

Number of Adverse Events After Administration of Single Oral Doses up to 0.5 mg/kg of Nepadutant in Infants.

Number of adverse events (AE) reported by dose and age stratum 18-24 weeks. (NCT00655083)
Timeframe: one week

InterventionAdverse Events (Number)
Nepadutant 0.1 mg/kg3

[back to top]

Drug Concentration Measurement in the Urine Collected by Diapers Along 24 Hours Post Dose and One Week After Dose in All Treated Infants and by Age and Dose Subgroups.

Nepadutant was measured in the 24-h urine collection post both doses (0.1 and 0.5 mg/kg dose), in the age strata 6-<12 and 12-<18 weeks, using urinary collection/extraction from pre-weighed special fiber based diapers. (NCT00655083)
Timeframe: 24 hours

,
Interventionng (Mean)
6- <12 week old12- < 18 week old
Nepadutant 0.1 mg/kg50412095
Nepadutant 0.5 mg/kg64743727

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Number of Adverse Events After Administration of Single Oral Doses up to 0.5 mg/kg of Nepadutant in Infants.

Number of adverse events (AE) reported by dose and age stratum 6-<12 and 12-<18 weeks. (NCT00655083)
Timeframe: one week

,
InterventionAdverse Events (Number)
6- <12 week old12- < 18 week old
Nepadutant 0.1 mg/kg01
Nepadutant 0.5 mg/kg31

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Absolute Change in the Overall Parental Judgment After the First Dose of Treatment Versus Baseline

"On a daily basis parents expressed an overall judgement on the study treatment effect based on a 6 rate categorical scale from 0 to 5 (where 0 is for Not at all and 5 is Extremely.~The question was How frustrating to you was your baby's crying today?)" (NCT01258153)
Timeframe: 1 day

InterventionScore range 0-5 (Mean)
Nepadutant Low Dose-0.38
Nepadutant High Dose-0.68
Placebo-0.34

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Absolute Change in the Overall Parental Judgment After Treatment Discontinuation Versus Baseline

"On a daily basis parents expressed an overall judgement on the study treatment effect based on a 6 rate categorical scale from 0 to 5 (where 0 is for Not at all and 5 is Extremely.~The question was How frustrating to you was your baby's crying today?)" (NCT01258153)
Timeframe: 10 days

InterventionScore range 0-5 (Mean)
Nepadutant Low Dose-1.35
Nepadutant High Dose-1.78
Placebo-1.39

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Absolute Change in the Overall Parental Judgment at the End of Treatment Versus Baseline

"On a daily basis parents expressed an overall judgement on the study treatment effect based on a 6 rate categorical scale from 0 to 5 (where 0 is for Not at all and 5 is Extremely.~The question was How frustrating to you was your baby's crying today?)" (NCT01258153)
Timeframe: 1 week

InterventionScore range 0-5 (Mean)
Nepadutant Low Dose-1.24
Nepadutant High Dose-1.75
Placebo-1.23

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Percentage of 'Responder' Babies at the End of Treatment Period.

Response is defined as a decrease of at least 50% of crying and fussing time during the last 3 days on treatment vs baseline. (NCT01258153)
Timeframe: baseline and one week

InterventionResponders Rate (% of responders babies) (Number)
Nepadutant Low Dose36.8
Nepadutant High Dose55.3
Placebo19.4

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Safety and Tolerability Will be Assessed in Terms of Frequency and Severity of AEs as Well as Frequency of Clinically Significant Changes in Physical Examination and Lab Test.

Safety and tolerability will be assessed for the Safety Population (all patients who received the study drug) in terms of frequency and severity of AEs as well as frequency of clinically significant changes in physical examination and lab test. (NCT01258153)
Timeframe: up to four weeks

InterventionAdverse events (Number)
Nepadutant Low Dose9
Nepadutant High Dose6
Placebo5

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Absolute Change of the Mean Daily Crying and Fussing Time for Three Consecutive Days While on Treatment Versus Baseline.

"Efficacy assessment to be measured through baby's day diary recorded for three consecutive days while on treatment (i.e. starting from 6 pm on Day 4 and continued for 72 hours) vs baseline (i.e. starting from 6 pm on Day -4 until 1st treatment administration)." (NCT01258153)
Timeframe: Baseline and one week

,,
InterventionMinutes (Mean)
BaselineEnd of TreatmentChange
Nepadutant High Dose273.6154.4-119.2
Nepadutant Low Dose284.57185.8-96.9
Placebo283.91192.7-91.2

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A Population Pharmacokinetic Analysis to Characterize the Plasma Concentration-time Course for Nepadutant in Infant With Colics From NIC-04

PopPK Volume estimated with a one compartment model with first order absorption and elimination. NOTE: for this measure, no inter-individual variability was estimated, therefore the value for each cohort corresponds to the typical value. (NCT01532518)
Timeframe: 0.5, 1, 2, 3 hours post Single Dose and 24 hours post Repeated Dose

InterventionL (Mean)
Cohort 1, 2, and 322.5

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A Population Pharmacokinetic Analysis to Characterize the Plasma Concentration-time Course for Nepadutant in Infant With Colics From NIC-04

The population pharmacokinetic analyses is presented. PopPK Clearance estimated with a one compartment model with first order absorption and elimination. (NCT01532518)
Timeframe: 0.5, 1, 2, 3 hours post Single Dose and 24 hours post Repeated Dose

InterventionL/h (Mean)
Cohort11.24
Cohort 21.31
Cohort 31.64

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A Population Pharmacokinetic Analysis to Characterize the Plasma Concentration-time Course for Nepadutant in Infant With Colics From NIC-04

The population pharmacokinetic analyses is presented. PopPK Ka estimated with a one compartment model with first order absorption and elimination. NOTE: for this measure, no inter-individual variability was estimated, therefore the value for each cohort corresponds to the typical value. (NCT01532518)
Timeframe: 0.5, 1, 2, 3 hours post Single Dose and 24 hours post Repeated Dose

Intervention1/h (Mean)
Cohort 1, 2 and 3206

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A Population Pharmacokinetic Analysis to Characterize the Plasma Concentration-time Course for Nepadutant in Infant With Colics From NIC-04

The population pharmacokinetic analyses is presented. The PopPK parameter fraction of the dose absorbed (F1) is estimated with a one compartment model with first order absorption and elimination.The results are presented fraction of the absorbed dose with 95% CI of the parameter estimate value (NCT01532518)
Timeframe: 0.5, 1, 2, 3 hours post Single Dose and 24 hours post Repeated Dose

Interventionfraction of dose absorbed (Mean)
Cohort 10.0275
Cohort 20.0342
Cohort 30.0346

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I-GERQ-R Score Changes vs Baseline (Visit 2) by First Dose Level (0.1mg/kg and 0.5mg/kg).

"Change in Infant Gastroesophageal Reflux Questionnaire Revised (I-GERQ-R) Score. Assessing the I-GERQ-R score changes vs baseline (Visit 2) by first dose level (0.1mg/kg and 0.5mg/kg). Infant Gastroesophageal Reflux Questionnaire Revised (I-GERQ-R ), with a minimum-maximum score of 0-42 (minimum for diagnosis >15). The higher values reflect worse outcome. The questionnaire comprised 12 items as questions quantifying aspects of regurgitation (3 questions), crying (3 questions), feeding refusal (2 questions), apnea/cyanosis (2 questions), hiccups and arching. Questions with 4 possible options have a score ranging from 0 to 3; questions with 5 possible options have a score ranging from 0 to 4.~The scores of each item are summed, so the total score is presented." (NCT01532518)
Timeframe: Baseline (V2) and end of 1st week of treatment(V3)

Interventionscore on a scale (Mean)
Low Dose Level (0.1mg/kg)-6.8
Medium Dose Level 0.5mg/kg-7.6

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I-GERQ-R Score Changes vs Visit 3 by Second Dose Level (0.5mg/kg and 1mg/kg).

"Change in Infant Gastroesophageal Reflux Questionnaire Revised (I-GERQ-R) Score. Assessing the I-GERQ-R score changes vs Visit 3 by second dose level (0.5mg/kg and 1mg/kg).~Infant Gastroesophageal Reflux Questionnaire Revised (I-GERQ-R ), with a minimum-maximum score of 0-42 (minimum for diagnosis >15). The higher values reflect worse outcome. The questionnaire comprised 12 items as questions quantifying aspects of regurgitation (3 questions), crying (3 questions), feeding refusal (2 questions), apnea/cyanosis (2 questions), hiccups and arching. Questions with 4 possible options have a score ranging from 0 to 3; questions with 5 possible options have a score ranging from 0 to 4.~The scores of each item are summed, so the total score is presented." (NCT01532518)
Timeframe: end of first week of treatment (V3) and end of second week of treatment (V4)

InterventionScore as sum of units (Mean)
Medium Dose Level (0.5mg/kg)-1.4
High Dose Level 1mg/kg-4.9

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The Absolute Differences of I-GERQ-R Total Score at V3 (End of First Week of Treatment) Respect to the Baseline (V2).

"Results obtained at V2 serve as baseline values for the assessment of effects at V3 (i.e. end of first week of treatment).~Infant Gastroesophageal Reflux Questionnaire Revised (I-GERQ-R ), with a minimum-maximum score of 0-42 (minimum for diagnosis >15). The higher values reflect worse outcome. The questionnaire comprised 12 items as questions quantifying aspects of regurgitation (3 questions), crying (3 questions), feeding refusal (2 questions), apnea/cyanosis (2 questions), hiccups and arching. Questions with 4 possible options have a score ranging from 0 to 3; questions with 5 possible options have a score ranging from 0 to 4.~The scores of each item are summed, so the total score is presented." (NCT01532518)
Timeframe: Baseline (V2) and end of first week of treatment (V3)

Interventionscore on a scale (Mean)
Cohort 3-6.8
Cohort 2-7.6
Cohort 1-6.8

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The Absolute Differences of I-GERQ-R Total Score at V4 (End of 2nd Week of Treatment) Respect to V3 (End of 1st Week of Treatment).

"The results obtained at V3 are used as baseline for the second week treatment period (V4).~Infant Gastroesophageal Reflux Questionnaire Revised (I-GERQ-R ), with a minimum-maximum score of 0-42 (minimum for diagnosis >15). The higher values reflect worse outcome. The questionnaire comprised 12 items as questions quantifying aspects of regurgitation (3 questions), crying (3 questions), feeding refusal (2 questions), apnea/cyanosis (2 questions), hiccups and arching. Questions with 4 possible options have a score ranging from 0 to 3; questions with 5 possible options have a score ranging from 0 to 4.~The scores of each item are summed, so the total score is presented." (NCT01532518)
Timeframe: V3 (end of 1st week of treatment) and V4 (end of 2nd week of treatment)

InterventionScore as sum of units (Mean)
Cohort 3-15.2
Cohort 2-11.9
Cohort 1-8.6

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The Absolute Differences of I-GERQ-R Total Score at V5 (Follow-up) Respect to V2 (Baseline).

"Results obtained at V2 serve as baseline values for follow-up assessment 2 weeks after the last administered dose (V5) Infant Gastroesophageal Reflux Questionnaire Revised (I-GERQ-R ), with a minimum-maximum score of 0-42 (minimum for diagnosis >15). The higher values reflect worse outcome. The questionnaire comprised 12 items as questions quantifying aspects of regurgitation (3 questions), crying (3 questions), feeding refusal (2 questions), apnea/cyanosis (2 questions), hiccups and arching. Questions with 4 possible options have a score ranging from 0 to 3; questions with 5 possible options have a score ranging from 0 to 4.~The scores of each item are summed, so the total score is presented." (NCT01532518)
Timeframe: Baseline (V2) and follow up 2 weeks after the last administered dose (V5)

InterventionScore as sum of units (Mean)
Cohort 3-7.8
Cohort 2-11.1
Cohort 1-9.8

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Incidence and Severity of AEs_ Number of Adverse Events by Treatment Dose Level

The analysis is by treatment - Each infant was treated with two out of three ascending dose (0.1, 0.5 or 1.0 mg/kg), therefore counted in more than one dose level. (NCT01532518)
Timeframe: up to 4 weeks

,,
InterventionNumber of events (Number)
gastrointestinal disorderGeneral disorders and administration site conditioInfections and infestationsInjury, poisoning and procedural complicationsPsychiatric disordersRespiratory, thoracic and medistinal disordersSkin and subcutaneous tissue disorders
High Dose Level (1.0 mg/Kg)6171033
Low Dose Level(0.1mg/Kg)3010113
Medium Dose Level (0.5mg/Kg)4021011

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