Page last updated: 2024-11-04

trimebutine

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

Description

Trimebutine: Proposed spasmolytic with possible local anesthetic action used in gastrointestinal disorders. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5573
CHEMBL ID190044
CHEBI ID94458
SCHEMBL ID25705
MeSH IDM0021980

Synonyms (79)

Synonym
AC-18004
AKOS005557702
2-(dimethylamino)-2-phenylbutyl 3,4,5-tris(methyloxy)benzoate
39133-31-8
trimebutine
S2085
beta-(dimethylamino)-beta-ethylphenethyl alcohol 3,4,5-trimethoxybenzoate (ester)
einecs 254-309-2
2-dimethylamino-2-phenylbutyl 3,4,5-trimethoxybenzoat
trimebutine [inn:ban:dcf]
trimebutino [inn-spanish]
trimebutinum [inn-latin]
benzoic acid, 3,4,5-trimethoxy-, 2-(dimethylamino)-2-phenylbutyl ester
trimebutine (inn)
D08639
trimebutina (tn)
CHEMBL190044
[2-(dimethylamino)-2-phenylbutyl] 3,4,5-trimethoxybenzoate
STK624973
2-(dimethylamino)-2-phenylbutyl 3,4,5-trimethoxybenzoate
NCGC00018269-02
A824421
3,4,5-trimethoxybenzoic acid [2-(dimethylamino)-2-phenylbutyl] ester
58997-89-0
unii-qz1oj92e5r
trimebutino
qz1oj92e5r ,
trimebutinum
3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutyl ester
FT-0630604
CCG-221203
HY-B0380
BBL028253
SCHEMBL25705
KS-5233
trimebutine [inn]
trimebutine [mi]
.beta.-(dimethylamino)-.beta.-ethylphenethyl alcohol 3,4,5-trimethoxybenzoate (ester)
trimebutine [who-dd]
trimebutina
T3049
(.+/-.)-2-(dimethylamino)-2-phenylbutyl 3,4,5-trimethoxybenzoate
benzoic acid, 3,4,5-trimethoxy-, 2-(dimethylamino)-2-phenylbutyl ester, (.+/-.)-
2-(dimethylamino)-2-phenylbutyl 3,4,5-trimethoxybenzoate #
trimebutine free base
(z)-2-butenedioic acid;3,4,5-trimethoxybenzoic acid [2-(dimethylamino)-2-phenylbutyl] ester
cid_5388977
maleic acid;3,4,5-trimethoxybenzoic acid [2-(dimethylamino)-2-phenyl-butyl] ester
bdbm83417
(z)-but-2-enedioic acid;[2-(dimethylamino)-2-phenyl-butyl] 3,4,5-trimethoxybenzoate
W-111163
AB00513736_18
AB00513736_19
DTXSID4023707
DB09089
mebutin
trimebutine base
CHEBI:94458
HMS3651M10
trimebutine, analytical standard
trimebutine; 3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutyl ester; (+/-)-trimebutine; brl-9476
SBI-0207059.P001
HMS3715B08
SW197522-2
FT-0675577
mfcd00133873
Q2569888
BCP10621
SB18897
HMS3884D05
D92653
3,4,5-trimethoxybenzoic acid 2-[dimethylamino]-2-phenylbutyl ester
(+)-trimebutine
(-)-trimebutine
benzoic acid, 3,4,5-trimethoxy-, 2-(dimethylamino)-2-phenylbutyl ester, (+)-
benzoic acid, 3,4,5-trimethoxy-, 2-(dimethylamino)-2-phenylbutyl ester, (-)-
2-(dimethylamino)-2-phenylbutyl3,4,5-trimethoxybenzoate
2-(dimethylamino)-2-phenylbutyl(-)-3,4,5-trimethoxybenzoate
EN300-18531315

Research Excerpts

Overview

Trimebutine maleate is a prokinetic drug that hastens gastric emptying, by inducing the release of gastrointestinal agents such as motilin and gastrin. It is an opiate modulator of the gastrointestinal motility that interacts with enkephalinergic receptors.

ExcerptReferenceRelevance
"Trimebutine maleate is a prokinetic drug that hastens gastric emptying, by inducing the release of gastrointestinal agents such as motilin and gastrin."( The trimebutine effect on Helicobacter pylori-related gastrointestinal tract and brain disorders: A hypothesis.
Boziki, M; Deretzi, G; Doulberis, M; Fludaras, I; Gavalas, E; Grigoriadis, N; Karafoulidou, E; Katsinelos, P; Kesidou, E; Koukoufiki, A; Kountouras, J; Liatsos, C; Papaefthymiou, A; Polyzos, SA; Simeonidou, C; Sofou, E; Taloumtzis, C; Theotokis, P; Touloumtzi, M; Vardaka, E, 2021
)
1.9
"Trimebutine is a weak opioid receptor agonist used in the treatment of IBS."( A nitro-arginine derivative of trimebutine (NO2-Arg-Trim) attenuates pain induced by colorectal distension in conscious rats.
Caliendo, G; Distrutti, E; Fiorucci, S; Mencarelli, A; Renga, B; Santagada, V; Severino, B, 2009
)
1.36
"Trimebutine is an opioid derivative with exclusive action on receptors of the Meissner and Auerbach plexus throughout the digestive tube."( Rizatriptan vs. rizatriptan plus trimebutine for the acute treatment of migraine: a double-blind, randomized, cross-over, placebo-controlled study.
Bigal, ME; Filho, PF; Krymchantowski, AV, 2006
)
1.34
"Trimebutine maleate is a prokinetic agent that acts directly on the smooth muscle of the GI tract. "( Pharmacokinetic and bioequivalence evaluation of two formulations of 100 mg trimebutine maleate (Recutin and Polybutin) in healthy male volunteers using the LC-MS/MS method.
Jeon, YC; Jhee, OH; Kang, JS; Lee, MH; Lee, SH; Lee, YS; Shaw, LM, 2007
)
2.01
"Trimebutine is an opiate modulator of the gastrointestinal motility that interacts with enkephalinergic receptors."( Effects of trimebutine on sphincter of Oddi motility in patients with post-cholecystectomy pain.
Abou, E; Barthet, M; Berdah, S; Bouvier, M; Grimaud, JC; Mambrini, P; Pecout, C; Salducci, J; Viviand, X, 1998
)
2.13
"Trimebutine possibly acts as a stimulator of peripheral receptors of the enkephalinergic nervous system."( [Effects of trimebutine on motility of the small intestine in humans].
Chaussade, S; Couturier, D; Grandjouan, S, 1989
)
1.38

Effects

Trimebutine maleate has been used extensively, since the late 1960's, for the treatment of functional gastrointestinal disorders, including irritable bowel syndrome (IBS) It has been effective in some IBS patients by modulating colonic motility.

ExcerptReferenceRelevance
"Nor-trimebutine has a blocking activity on sodium channels and a potent local anesthetic effect."( Effect of nor-trimebutine on neuronal activation induced by a noxious stimulus or an acute colonic inflammation in the rat.
Bonaz, B; Mouchet, P; Sinniger, V, 2005
)
1.17
"Trimebutine maleate has been used extensively, since the late 1960's, for the treatment of functional gastrointestinal disorders, including irritable bowel syndrome (IBS). "( Trimebutine: a state-of-the-art review.
Salvioli, B, 2019
)
3.4
"Trimebutine has been shown to act on peripheral opioid receptors."( Trimebutine: abuse, addiction and overdose.
, 2013
)
2.55
"Trimebutine has been used for treatment of both hypermotility and hypomotility disorders of the gastrointestinal (GI) tract, such as irritable bowel syndrome. "( Trimebutine as a modulator of gastrointestinal motility.
Kim, BJ; Lee, HT, 2011
)
3.25
"Nor-trimebutine has a blocking activity on sodium channels and a potent local anesthetic effect."( Effect of nor-trimebutine on neuronal activation induced by a noxious stimulus or an acute colonic inflammation in the rat.
Bonaz, B; Mouchet, P; Sinniger, V, 2005
)
1.17
"Trimebutine has been effective in some IBS patients by modulating colonic motility."( Efficacy of trimebutine therapy in patients with gastroesophageal reflux disease and irritable bowel syndrome.
Boura, P; Chatzopoulos, D; Kalis, A; Kountouras, J; Venizelos, J; Zavos, C,
)
1.23

Treatment

ExcerptReferenceRelevance
"Treatment with trimebutine maleate resulted in reduction in duration of the lag period and less retention of food at 100 minutes (p < 0.0005)."( The effect of trimebutine maleate on gastric emptying in patients with non-ulcer dyspepsia.
Aktas, A; Bayhan, H; Caner, B; Mentes, T; Narin, Y; Ozturk, F, 1999
)
1

Pharmacokinetics

The method is accurate, sensitive and suitable for pharmacokinetic study of trimebutine maleate. This method has been successfully applied to the pharmacokinetics study in rabbit blood following oral administration of 200 mg/kg.

ExcerptReferenceRelevance
" The non-compartmental method was used for pharmacokinetic analysis."( Pharmacokinetics and bioequivalence of two trimebutine formulations in healthy volunteers using desmethyl-trimebutine levels.
Cahiez, G; Chomard, JM; Donazzolo, C; Houin, G; Labaune, JP; Lavit, M; Martin, A; Michel, F; Saivin, S, 2000
)
0.57
" The method was employed to pharmacokinetic analysis of trimebutine maleate."( [HPCE determination of trimebutine maleate in rat plasma and its pharmacokinetics].
Li, FM; Yu, LN, 2001
)
0.87
" The pharmacokinetic results were AUC0-infinity = 8 micrograms."( [HPCE determination of trimebutine maleate in rat plasma and its pharmacokinetics].
Li, FM; Yu, LN, 2001
)
0.62
"The method is accurate, sensitive and suitable for pharmacokinetic study of trimebutine maleate."( [HPCE determination of trimebutine maleate in rat plasma and its pharmacokinetics].
Li, FM; Yu, LN, 2001
)
0.85
" The main pharmacokinetic parameters of T1/2, Tmax and Cmax were (9."( [Pharmacokinetics and bioequivalence of trimebutine dispersive tablet in healthy subjects].
Ding, L; Huang, X; Jiang, H; Liu, GY; Yang, J; Zhang, ZX, 2004
)
0.59
" This method has been successfully applied to the pharmacokinetic study of trimebutine maleate in rabbit blood following oral administration of 200 mg/kg."( Pharmacokinetic study of trimebutine maleate in rabbit blood using in vivo microdialysis coupled to capillary electrophoresis.
Wang, L; Yang, W; Zhang, Z, 2005
)
0.86
" Several pharmacokinetic (PK) parameters (including AUC(t), AUC(infinity), C(max), T(max), T(1/2), and K(e)) were determined from the plasma concentrations of nor-TMB of both formulations."( Pharmacokinetic and bioequivalence evaluation of two formulations of 100 mg trimebutine maleate (Recutin and Polybutin) in healthy male volunteers using the LC-MS/MS method.
Jeon, YC; Jhee, OH; Kang, JS; Lee, MH; Lee, SH; Lee, YS; Shaw, LM, 2007
)
0.57

Bioavailability

ExcerptReferenceRelevance
" The confidence interval approach was used for comparison of the formulations according to the EU guidance note on bioavailability and bioequivalence on Cmax, AUC0-t and AUC0-infinity, log transformed."( Pharmacokinetics and bioequivalence of two trimebutine formulations in healthy volunteers using desmethyl-trimebutine levels.
Cahiez, G; Chomard, JM; Donazzolo, C; Houin, G; Labaune, JP; Lavit, M; Martin, A; Michel, F; Saivin, S, 2000
)
0.57
" The oral bioavailability of drugs in the TMCTs was then evaluated and compared to the simultaneous oral administration of trimebutine maleate-loaded and mosapride citrate-loaded commercial products in the beagle dog."( Development of a novel combination tablet containing trimebutine maleate and mosapride citrate for the treatment of functional dyspepsia.
Cho, KH; Choi, HG; Choi, YK; Kang, JH; Park, YJ; Yong, CS, 2010
)
0.82

Dosage Studied

Trimebutine (3-30 microM) caused a parallel rightward shift of the dose-response curve for the contractile response to a higher concentration range of Ca2+ under high-K+ conditions in a noncompetitive manner.

ExcerptRelevanceReference
" In mechanical experiments using the taenia cecum, trimebutine (3-30 microM) caused a parallel rightward shift of the dose-response curve for the contractile response to a higher concentration range of Ca2+ under high-K+ conditions in a noncompetitive manner."( Allosteric interaction of trimebutine maleate with dihydropyridine binding sites.
Kurosawa, H; Nagasaki, M; Naito, K; Tamaki, H, 1990
)
0.83
" At similar dosage NDTMB had less pronounced inhibitory effects on gastric activity fronts and in contrast with TMB, the inhibitory effect on the colonic motility was observed as soon as the infusion of NDTMB started."( Effects of orally vs. parenterally administrated trimebutine on gastrointestinal and colonic motility in dogs.
Buéno, L; Hondé, C; Junien, JL; Pascaud, X, 1987
)
0.53
" TM-906 noncompetitively antagonized the contractile response to methacholine, and it caused a parallel shift of dose-response curves for the contractile response to CaCl2 to higher concentrations."( Effects of trimebutine maleate (TM-906) on the smooth muscles of isolated guinea pig gallbladder.
Magaribuchi, T; Takenaga, H; Tamaki, H, 1984
)
0.66
"001) more effective than placebo, but not significantly so when the dosage level was halved."( A three-part controlled study of trimebutine in the treatment of irritable colon syndrome.
Lüttecke, K, 1980
)
0.54
" The method was successfully applied to the quantitation of TMB in granule dosage form (Debridat) and recoveries between 98."( Determination of trimebutine in pharmaceuticals by differential pulse voltammetry at a glassy carbon electrode.
Adhoum, N; Monser, L, 2005
)
0.67
"HCl) and trimebutine (TB) drugs as electron donor with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ), tetracyanoethylene (TCNE) and 7,7,8,8-tetracyanoquinodimethane (TCNQ) as π-acceptors in acetonitrile were investigated spectrophotometrically to determine the cited drugs in pure and dosage forms."( Analytical studies on the charge transfer complexes of loperamide hydrochloride and trimebutine drugs. Spectroscopic and thermal characterization of CT complexes.
El-Din, GM; Elqudaby, HM; Mohamed, GG, 2014
)
1.04
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
trihydroxybenzoic acid
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)10.00000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID1283269Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID250135Inhibition of compound against MES-SA/DX5 cell line was determined using P-glycoprotein assay2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
A pharmacophore hypothesis for P-glycoprotein substrate recognition using GRIND-based 3D-QSAR.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1283260Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as increase in lanosterol levels at 100 nM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1283272Change in cholesterol level in Dhcr7-deficient mouse Neuro2a cells at 100 nM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1283259Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as increase in desmosterol levels at 100 nM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (183)

TimeframeStudies, This Drug (%)All Drugs %
pre-199063 (34.43)18.7374
1990's41 (22.40)18.2507
2000's40 (21.86)29.6817
2010's26 (14.21)24.3611
2020's13 (7.10)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 89.21

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index89.21 (24.57)
Research Supply Index5.45 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index160.08 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (89.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials38 (19.59%)5.53%
Reviews12 (6.19%)6.00%
Case Studies12 (6.19%)4.05%
Observational1 (0.52%)0.25%
Other131 (67.53%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (7)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Impact of Bacillus Clausii Administration on Irritable Bowel Syndrome Patients - a Pilot Study [NCT03359499]Phase 2/Phase 380 participants (Actual)Interventional2017-08-12Completed
Trimebutine Maleate (NEWBUTIN SR 300 mg Tab) as a Prophylactic Anti-emetic Drug for Patients Who Underwent Arthroscopic Rotator Cuff Repair: a Randomized Controlled Study [NCT01984931]Phase 345 participants (Anticipated)Interventional2013-10-31Recruiting
A Phase 1b Clinical Study on the Analgesic Effect of GIC-1001 and GIC-1002 on Visceral Pain Under Rectal Distension and Rectal Sensory Threshold Using the Barostat Method in Male and Female Healthy Volunteers. [NCT02276768]Phase 190 participants (Actual)Interventional2014-10-31Completed
The Clinical Efficacy and Safety of Trimebutine Maleate Combined With Rabeprazole in Patients With Grade A or B Reflux Esophagitis Whose Symptoms Refractory to Rabeprazole [NCT02986685]Phase 40 participants (Actual)Interventional2016-11-30Withdrawn(stopped due to Lack of funds)
Additive Effect of Trimebutine on the Development of Adverse Events Related to the Helicobacter Pylori Eradication Medications; an Open-label, Randomized Controlled Trial [NCT04403087]Phase 4132 participants (Actual)Interventional2021-05-01Completed
Effect of Trimebutine on Postoperative Pain After Milligan-Morgan Hemorrhoidectomy: A Randomized Controlled Trial [NCT03036111]42 participants (Anticipated)Interventional2017-02-01Suspended(stopped due to Unavailability of Triembutine maleate)
A Randomized, Double-Blind, Placebo-Controlled, Phase 2a Proof-of-Concept Study of GIC-1001 for the Management of Visceral Pain in Subjects Undergoing Sedation-Free, Full Colonoscopy [NCT01926444]Phase 2308 participants (Actual)Interventional2013-07-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01926444 (7) [back to overview]Colonoscopy Completion Rate (%)
NCT01926444 (7) [back to overview]Time to Caecum
NCT01926444 (7) [back to overview]Total Examination Time (Colonoscopy)
NCT01926444 (7) [back to overview]Measurements of Visceral Pain, Using a 100-mm Visual Analog Scale (VAS)
NCT01926444 (7) [back to overview]Safety-Plasma Concentrations of Trimebutine and N-Desmethyl-Trimebutine
NCT01926444 (7) [back to overview]Endoscopist's Perception of Colonoscopy- Adequacy of Analgesia, Difficulty of Insertion and Withdrawal
NCT01926444 (7) [back to overview]Endoscopist's Perception of Colonoscopy- Amount of Colonic Spasm on Insertion and Withdrawal

Colonoscopy Completion Rate (%)

Qualitative outcome: colonoscopy completion is defined as a procedure performed entirely, from initial anal insertion, reaching of caecum, and complete removal of the scope. Completion rate is then the number of patient (%) with a complete colonoscopy (up to the caecum) divided by the number of trial participants. (NCT01926444)
Timeframe: Number of patients during trial with a complete colonoscopy, where the scope has reached the caecum during the colonoscopy. Range of duration of colonoscopy 5.00- 50.10 minutes.

InterventionParticipants (Count of Participants)
GIC-1001 Low Dose56
GIC-1001 Mid-dose52
GIC-1001 , High Dose51
GIC-1001 Matching Placebo101

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Time to Caecum

Time to Caecum is the time taken by the physician to reach the caecum with the colonoscope, from the insertion in the anus. Time to Caecum was measured during colonoscopy, for which total duration of colonoscopy ranged between a minimum of 5.00 and a maximum of 50.10 minutes. (NCT01926444)
Timeframe: From the time of introduction of the colonoscope, to removal of colonoscope. Range of duration of colonoscopy 5.00- 50.10 minutes.

Interventionminutes (Mean)
GIC-1001 Low Dose8.47
GIC-1001 Mid-dose6.51
GIC-1001 , High Dose9.22
GIC-1001 Matching Placebo8.04

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Total Examination Time (Colonoscopy)

Defined as the time from endoscope insertion to complete removal of the endoscope; measured in minutes (NCT01926444)
Timeframe: From the time of introduction of the colonoscope, to removal of colonoscope. Range of duration of colonoscopy 5.00- 50.10 minutes.

Interventionminutes (Mean)
GIC-1001 Low Dose15.82
GIC-1001 Mid-dose13.05
GIC-1001 , High Dose15.52
GIC-1001 Matching Placebo14.61

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Measurements of Visceral Pain, Using a 100-mm Visual Analog Scale (VAS)

The Primary Outcomes Measure was the pain VAS 100-mm AUC (0mm = no pain; 100mm = worst pain), constructed from serial pain VAS measurements performed during colonoscopy. At least 8 pain VAS measurements were made, and the length of the colonoscope inserted (or removed on the way out) was recorded at every measurement. The X-axis of the VAS versus anatomical locations was defined accordingly: each VAS value corresponded to a relative length of inserted colonoscope (d/2Lc) of the X axis, where d was the actual length of the inserted colonoscope and 2Lc represented twice the total length of the colon examined (Lc). Before scope insertion the X value equaled zero. Once the caecum was reached, the X value was 0.5. Upon complete removal of the endoscope, the X value was 1. This allowed standardization of colonic length between study subjects. Visceral pain AUC (mm) was calculated from all serial measurements, where the length of inserted colonoscope determined the VAS measurement's location (NCT01926444)
Timeframe: Assessed at different anatomical locations: (1) before colonoscopy, (2) insertion of scope in anus, (3) at rectosigmoid flexure, (4) at splenic flexure, (5) at hepatic flexure, (6) at caecum, (7) at splenic flexure on way back, (8) after colonoscopy.

,,,
Interventionmm (Mean)
AUC- censorsed (standardized); FASAUC LOCF (standardized); FASAUC- censorsed (standardized); PPAUC LOCF (standardized); PP
GIC-1001 , High Dose23.3127.7324.6124.8
GIC-1001 Low Dose22.2725.520.7920.96
GIC-1001 Matching Placebo22.2227.5522.0322.00
GIC-1001 Mid-dose18.9323.4417.617.63

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Safety-Plasma Concentrations of Trimebutine and N-Desmethyl-Trimebutine

A pharmacokinetic (PK) analysis was carried out on the first 24 patients randomized, equally distributed between treatment groups; 18 patients were assigned to active treatment (NCT01926444)
Timeframe: Day 4 prior to colonoscopy.

,,
Interventionng/mL (Mean)
Plasma Concentration- TrimebutinePlasma Concentration-N-Desmethyl-Trimebutine
GIC-1001 , High Dose16.22389.18
GIC-1001 Low Dose5.17174.5
GIC-1001 Mid-dose8.80440.98

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Endoscopist's Perception of Colonoscopy- Adequacy of Analgesia, Difficulty of Insertion and Withdrawal

Endoscopist's perception of the adequacy of analgesia, difficulty of insertion and withdrawal measured on a five-point Likert scale: Strongly Agree, Agree, Agree nor Disagree, Disagree, Strongly Disagree (NCT01926444)
Timeframe: From the time of introduction of the colonoscope, to removal of colonoscope. Range of duration of colonoscopy 5.00- 50.10 minutes.

InterventionParticipants (Count of Participants)
Adequate Analgesia72219363Adequate Analgesia72219364Adequate Analgesia72219365Adequate Analgesia72219366Difficult Insertion72219366Difficult Insertion72219363Difficult Insertion72219364Difficult Insertion72219365Difficult Withdrawal72219365Difficult Withdrawal72219366Difficult Withdrawal72219363Difficult Withdrawal72219364
Strongly AgreeAgreeAgree nor DisagreeDisagreeStrongly Disagree
GIC-1001 Low Dose20
GIC-1001 Mid-dose18
GIC-1001 , High Dose16
GIC-1001 Matching Placebo33
GIC-1001 Low Dose14
GIC-1001 Mid-dose21
GIC-1001 , High Dose17
GIC-1001 Matching Placebo30
GIC-1001 Low Dose8
GIC-1001 Mid-dose3
GIC-1001 Matching Placebo10
GIC-1001 Low Dose9
GIC-1001 Mid-dose6
GIC-1001 , High Dose11
GIC-1001 Matching Placebo16
GIC-1001 Low Dose5
GIC-1001 Mid-dose4
GIC-1001 , High Dose5
GIC-1001 Matching Placebo12
GIC-1001 Low Dose3
GIC-1001 Mid-dose2
GIC-1001 , High Dose3
GIC-1001 Matching Placebo5
GIC-1001 Low Dose7
GIC-1001 , High Dose7
GIC-1001 Matching Placebo24
GIC-1001 Low Dose6
GIC-1001 Mid-dose5
GIC-1001 , High Dose4
GIC-1001 Low Dose22
GIC-1001 Mid-dose19
GIC-1001 , High Dose21
GIC-1001 Low Dose18
GIC-1001 Mid-dose20
GIC-1001 , High Dose18
GIC-1001 Matching Placebo31
GIC-1001 Low Dose0
GIC-1001 Mid-dose0
GIC-1001 Mid-dose1
GIC-1001 , High Dose2
GIC-1001 Matching Placebo2
GIC-1001 , High Dose0
GIC-1001 Matching Placebo1
GIC-1001 Low Dose19
GIC-1001 , High Dose15
GIC-1001 Matching Placebo29
GIC-1001 Low Dose37
GIC-1001 Mid-dose32
GIC-1001 , High Dose36
GIC-1001 Matching Placebo68

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Endoscopist's Perception of Colonoscopy- Amount of Colonic Spasm on Insertion and Withdrawal

Endoscopist's perception of the amount of colonic spasm on insertion and withdrawal measured on five-point Likert scale according to the following: Strongly Agree, Agree, Agree nor Disagree, Disagree, Strongly Disagree (NCT01926444)
Timeframe: From the time of introduction of the colonoscope, to removal of colonoscope. Range of duration of colonoscopy 5.00- 50.10 minutes.

InterventionParticipants (Count of Participants)
Colonic Spasm insertion72219365Colonic Spasm insertion72219366Colonic Spasm insertion72219363Colonic Spasm insertion72219364Colonic Spasm WIthdrawal72219364Colonic Spasm WIthdrawal72219365Colonic Spasm WIthdrawal72219363Colonic Spasm WIthdrawal72219366
AbsentPresent and minimal # (1 spasm)Present and moderate #(2-3 spasms)Present and high # (4-5 spasms)Present and very high (>5 spasms)
GIC-1001 Low Dose33
GIC-1001 Mid-dose33
GIC-1001 , High Dose33
GIC-1001 Matching Placebo59
GIC-1001 Mid-dose7
GIC-1001 , High Dose11
GIC-1001 Matching Placebo20
GIC-1001 Low Dose8
GIC-1001 Mid-dose10
GIC-1001 , High Dose6
GIC-1001 Matching Placebo11
GIC-1001 Mid-dose2
GIC-1001 , High Dose1
GIC-1001 Matching Placebo9
GIC-1001 Matching Placebo2
GIC-1001 Low Dose41
GIC-1001 Mid-dose40
GIC-1001 , High Dose45
GIC-1001 Matching Placebo83
GIC-1001 Low Dose11
GIC-1001 Mid-dose8
GIC-1001 Matching Placebo14
GIC-1001 Mid-dose4
GIC-1001 , High Dose2
GIC-1001 Matching Placebo3
GIC-1001 Low Dose2
GIC-1001 , High Dose0
GIC-1001 Matching Placebo1
GIC-1001 Low Dose0
GIC-1001 Mid-dose0
GIC-1001 Matching Placebo0

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