Page last updated: 2024-11-04

opc 12759

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Description

rebamipide: structure in first source; RN refers to (+-)-isomer; inhibits gastric xanthine oxidase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5042
CHEMBL ID1697771
CHEBI ID93814
SCHEMBL ID221527
MeSH IDM0149727

Synonyms (120)

Synonym
AC-6841
90098-04-7
ccris 3585
rebamipide [inn:jan]
(+-)-1,2-dihydro-alpha-((4-chlorobenzoyl)amino)-2-oxo-4-quinolinepropanoic acid
rebamipidum [inn-latin]
(+-)-2-(4-chlorobenzoylamino)-3-(2(1h)-quinolinon-4-yl)propionic acid
opc 12759
4-quinolinepropanoic acid, 1,2-dihydro-alpha-((4-chlorobenzoyl)amino)-2-oxo-, (+-)-
AB01275518-01
BRD-A15909516-001-02-5
gtpl871
proamipide
pramipide
mucosta
opc-12759
opc-759
rebamipide
BSPBIO_003559
111911-87-6
D01121
mucosta (tn)
rebamipide (jp17/inn)
NCGC00095161-02
NCGC00095161-01
KBIO3_002880
SPECTRUM2_000039
SPECTRUM3_001959
SPBIO_000137
SPECTRUM1505310
HMS2090L13
FT-0655225
HMS1922B20
2-[(4-chlorobenzoyl)amino]-3-(2-oxo-1h-quinolin-4-yl)propanoic acid
2-[(4-chlorophenyl)carbonylamino]-3-(2-oxidanylidene-1h-quinolin-4-yl)propanoic acid
2-[[(4-chlorophenyl)-oxomethyl]amino]-3-(2-oxo-1h-quinolin-4-yl)propanoic acid
A802443
A843443
nsc-758955
CHEMBL1697771
rebator
NCGC00095161-03
AKOS005721106
n-[(4-chlorophenyl)carbonyl]-3-(2-hydroxyquinolin-4-yl)alanine
STK577121
BBL011328
R0085
2-(4-chlorobenzamido)-3-[2(1h)-quinolinon-4-yl]propionic acid
nsc758955
pharmakon1600-01505310
tox21_111460
dtxsid8045937 ,
cas-90098-04-7
dtxcid6025937
nsc 758955
lr583v32zr ,
unii-lr583v32zr
rebamipidum
2-(4-chlorobenzoylamino)-3-(1,2-dihydro-2-oxo-4-quinolyl)propionic acid
CCG-39619
AKOS005501649
STL146407
n-[(4-chlorophenyl)carbonyl]-3-(2-oxo-1,2-dihydroquinolin-4-yl)alanine
rebamipide hydrate
FT-0630971
NCGC00095161-04
S2032
SCHEMBL221527
4-quinolinepropanoic acid, .alpha.-((4-chlorobenzoyl)amino)-1,2-dihydro-2-oxo-
139344-42-6
rebamipide [jan]
rebamipide [mi]
rebamipide [who-dd]
rebamipide [inn]
(+/-)-.alpha.-(p-chlorobenzamido)-1,2-dihydro-2-oxo-4-quinolinepropionic acid
HY-B0360
2-(4-chlorobenzoylamino)-3-(2-quinolon-4-yl)propionic acid
ALLWOAVDORUJLA-UHFFFAOYSA-N
2-(4-chlorobenzoylamino)-3-[2(1h)-quinolinon-4-yl]propionic acid
2-(4-chlorobenzoylamino)-3-(2-oxo-1,2-dihydroquinolin-4-yl)propionic acid
NCGC00095161-05
tox21_111460_1
2-(4-chlorobenzoylamino)-3-[2(1h)-quinolinon-4-yl] propionic acid
MLS006011883
smr003309276
Q-201660
AB01275518_03
AB01275518_02
4-quinolinepropanoicacid,a-[(4-chlorobenzoyl)amino]-1,2-dihydro-2-oxo-
mfcd00866895
opc12759
AC-7588
sr-05000001520
SR-05000001520-2
2-(4-chlorobenzamido)-3-(2-oxo-1,2-dihydroquinolin-4-yl)propanoic acid
CHEBI:93814
HMS3655L11
SR-05000001520-1
SR-05000001520-3
SBI-0207054.P001
HMS3714A15
SW199113-2
DB11656
BCP07230
2-[(4-chlorobenzoyl)amino]-3-(2-hydroxyquinolin-4-yl)propanoic acid
dispersered72
VS-02924
2-[(4-chlorophenyl)formamido]-3-(2-oxo-1,2-dihydroquinolin-4-yl)propanoic acid
(+/-)-2-(4-chlorobenzoylamino)-3-(2(1h)-quinolinon-4-yl)-propionic acid
Q7301602
BRD-A15909516-001-03-3
SY057250
2-(4-chlorobenzamido)-3-(2-oxo-1,2-dihydro-4-quinolyl)propanoic acid
A900081
4-quinolinepropanoicacid, a-[(4-chlorobenzoyl)amino]-1,2-dihydro-2-oxo-
BC164330
2-(4-chlorobenzamido)-3-(2-oxo-1,2-dihydroquinolin-4-yl)propanoicacid
4-quinolinepropanoic acid,a-[(4-chlorobenzoyl)amino]-1,2-dihydro-2-oxo-, (a+/-)-
EN300-19651969
Z2289798874

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"To develop the safe formulation that can safely improve bioavailability of poorly absorbable drugs and that is practically available, we prepared the suppositories of rebamipide, a poorly soluble and poorly absorbable antiulcer drug, by employing the combinatorial use of sodium laurate (C12), an absorption enhancer, with taurine (Tau) or L-glutamine (L-Gln), an adjuvant exerting the cytoprotective action."( Development of suppository formulation safely improving rectal absorption of rebamipide, a poorly absorbable drug, by utilizing sodium laurate and taurine.
Higaki, K; Kamada, N; Kimura, T; Minami, T; Miyake, M; Mukai, T; Odomi, M; Ogawara, K; Oka, Y; Toguchi, H, 2004
)
0.32
" No difference in the incidence of adverse events was seen between the two groups, confirming the safety of rebamipide."( Efficacy and safety of rebamipide for the treatment of dry mouth symptoms in patients with Sjögren's syndrome: a double-blind placebo-controlled multicenter trial.
Kawakami, A; Koni, I; Nishinarita, M; Nishiyama, S; Ohta, S; Oka, H; Sawada, S; Sugai, S; Sugiyama, E; Takahashi, H; Takei, M; Umehara, H; Yamaji, K, 2009
)
0.35
"Use of nonsteroidal anti-inflammatory drugs (NSAIDs) is primarily limited by renal and gastrointestinal adverse effects."( Effects of rebamipide on nephrotoxicity associated with selected NSAIDs in rats.
Bullins, KW; Denham, JW; Hanley, AV; Hanley, GA; Harirforoosh, S; Panus, PC; Wood, RC; Wyatt, JE, 2013
)
0.39
" No serious adverse events were observed in either group."( Efficacy and safety of proton pump inhibitors (PPIs) plus rebamipide for endoscopic submucosal dissection-induced ulcers: a meta-analysis.
Cao, Z; Dong, W; Guo, X; Liu, M; Song, J; Wang, J; Ye, C; Yu, S; Zhang, J, 2014
)
0.4
" When the possibility of poor compliance and the potential adverse effects of misoprostol are considered, rebamipide appears to be a clinically effective and safe alternative."( Preventive efficacy and safety of rebamipide in nonsteroidal anti-inflammatory drug-induced mucosal toxicity.
Cho, CS; Kang, YM; Kim, JH; Kim, SK; Lee, DH; Lee, SK; Lee, ST; Lee, YC; Park, SH; Park, W; Park, YW; Rew, JS; Yoo, WH, 2014
)
0.4
" No serious adverse events were observed in any of the patients in either group."( Efficacy and safety of 1-week Helicobacter pylori eradication therapy and 7-week rebamipide treatment after endoscopic submucosal dissection of early gastric cancer in comparison with 8-week PPI standard treatment: a randomized, controlled, prospective, m
Azuma, T; Higuchi, K; Iguchi, M; Machida, H; Morita, Y; Naito, Y; Takeuchi, T; Takeuchi, Y; Tamada, T; Tominaga, K; Uedo, N; Yagi, N; Yamao, J; Yazumi, S, 2015
)
0.42
" Serious adverse events were not observed in either group."( Efficacy and safety of 1-week Helicobacter pylori eradication therapy and 7-week rebamipide treatment after endoscopic submucosal dissection of early gastric cancer in comparison with 8-week PPI standard treatment: a randomized, controlled, prospective, m
Azuma, T; Higuchi, K; Iguchi, M; Machida, H; Morita, Y; Naito, Y; Takeuchi, T; Takeuchi, Y; Tamada, T; Tominaga, K; Uedo, N; Yagi, N; Yamao, J; Yazumi, S, 2015
)
0.42
" The incidences of adverse events potentially related to the study drug were 16%, 26%, and 13% in the placebo, rebamipide 2%, and rebamipide 4% groups, respectively."( Efficacy and safety of rebamipide liquid for chemoradiotherapy-induced oral mucositis in patients with head and neck cancer: a multicenter, randomized, double-blind, placebo-controlled, parallel-group phase II study.
Beppu, T; Fujii, M; Fujii, T; Fujimoto, Y; Hasegawa, Y; Hirano, S; Iwae, S; Kojima, H; Matsushima, Y; Matsuura, K; Monden, N; Naka, Y; Nishimori, H; Ogawa, T; Okami, K; Ota, I; Sasaki, K; Tahara, M; Takahashi, S; Tanaka, K; Ueda, S; Ueda, T; Yokota, T, 2017
)
0.46
"The present phase II study suggests that mouth washing with rebamipide may be effective and safe for patients with HNC receiving chemoradiotherapy, and 4% liquid is the optimal dose of rebamipide."( Efficacy and safety of rebamipide liquid for chemoradiotherapy-induced oral mucositis in patients with head and neck cancer: a multicenter, randomized, double-blind, placebo-controlled, parallel-group phase II study.
Beppu, T; Fujii, M; Fujii, T; Fujimoto, Y; Hasegawa, Y; Hirano, S; Iwae, S; Kojima, H; Matsushima, Y; Matsuura, K; Monden, N; Naka, Y; Nishimori, H; Ogawa, T; Okami, K; Ota, I; Sasaki, K; Tahara, M; Takahashi, S; Tanaka, K; Ueda, S; Ueda, T; Yokota, T, 2017
)
0.46
" Adverse events were recorded by patients in specially developed diaries."( Efficacy and safety of the use of rebamipide in the scheme of triple eradication therapy of Helicobacter pylori infection: a prospective randomized comparative study.
Andreev, DN; Dicheva, DT; Maev, IV; Partzvania-Vinogradova, EV; Samsonov, AA, 2018
)
0.48
" The incidence of adverse events between the groups was comparable: 22."( Efficacy and safety of the use of rebamipide in the scheme of triple eradication therapy of Helicobacter pylori infection: a prospective randomized comparative study.
Andreev, DN; Dicheva, DT; Maev, IV; Partzvania-Vinogradova, EV; Samsonov, AA, 2018
)
0.48
"This study aimed to detect safety signals of rebamipide and search for adverse events (AEs) of rebamipide that are more common than those of other drugs for peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD) in the elderly population."( Frequently reported adverse events of rebamipide compared to other drugs for peptic ulcer and gastroesophageal reflux disease.
Jang, E; Jeong, JE; Kim, MG; Lee, JY; Park, M, 2022
)
0.72
"The only side effect was dysgeusia (10% patients)."( Efficacy and safety of topical 2% rebamipide ophthalmic suspension in dry eye disease at tertiary care centre.
Jain, K; Jaju, M; Yadav, D, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic parameters were determined using a noncompartmental method."( Pharmacokinetics and bioequivalence of two formulations of rebamipide 100-mg tablets: a randomized, single-dose, two-period, two-sequence crossover study in healthy Korean male volunteers.
Cho, HY; Lee, YB; Park, GK; Yoon, H, 2009
)
0.35
" No significant sequence, subject, formulation, or period effects were detected for any pharmacokinetic parameter."( Pharmacokinetics and bioequivalence of two formulations of rebamipide 100-mg tablets: a randomized, single-dose, two-period, two-sequence crossover study in healthy Korean male volunteers.
Cho, HY; Lee, YB; Park, GK; Yoon, H, 2009
)
0.35
" There was no evidence that rebamipide pharmacokinetic parameters were influenced by genetic polymorphisms in the ABCB1 gene (exons 21 and 26)."( Pharmacokinetics and bioequivalence of two formulations of rebamipide 100-mg tablets: a randomized, single-dose, two-period, two-sequence crossover study in healthy Korean male volunteers.
Cho, HY; Lee, YB; Park, GK; Yoon, H, 2009
)
0.35
"This study was conducted primarily to improve the solubility of rebamipide, a poorly water-soluble anti-ulcer drug, using novel ternary solid dispersion (SD) systems and secondly to evaluate the effect of solubility enhancement on its pharmacokinetic (PK) and pharmacodynamic (PD) profile."( Physicochemical, pharmacokinetic and pharmacodynamic evaluations of novel ternary solid dispersion of rebamipide with poloxamer 407.
Chi, SC; Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2013
)
0.39
" In this study, we investigated the pharmacokinetic drug interactions of rebamipide with two selected NSAIDs, celecoxib or diclofenac."( Pharmacokinetic interactions between rebamipide and selected nonsteroidal anti-inflammatory drugs in rats.
Cooper, DL; Harirforoosh, S; Wood, RC; Wyatt, JE, 2014
)
0.4
"In this study, the population pharmacokinetic (PK) analysis of rebamipide (Reba) in healthy male Korean subjects was analyzed using the nonlinear mixed effects modeling method."( Population pharmacokinetic analysis of rebamipide in healthy Korean subjects with the characterization of atypical complex absorption kinetics.
Cho, HY; Lee, YB; Ngo, L; Tran, P; Yoo, HD, 2017
)
0.46
"Despite similar in vitro dissolution profiles, in vivo pharmacokinetic results revealed a partial difference between F4 and reference tablets."( Immediate-release tablet formulation of rebamipide and a pharmacokinetic study in healthy human subjects.
Choi, YW; Goo, YT; Hong, SH; Kim, CH; Kim, MJ; Lee, TH; Sin, GH; Won, YH, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"The present study evaluated the therapeutic effects of rebamipide alone and in combination with cimetidine on experimental gastritis established by the administration of 5 mM sodium taurocholate (TCA) for 6 months in rats."( Therapeutic effects of oral rebamipide and in combination with cimetidine on experimental gastritis in rats.
Fujimura, J; Haruma, K; Kajiyama, G; Kishimoto, S; Kobayashi, H; Machino, H; Sakurai, K; Shimamoto, T; Shimizu, S; Yamasaki, K, 1992
)
0.28

Bioavailability

ExcerptReferenceRelevance
" In conclusion, the combinatorial use of C12 with Tau or L-Gln could lead to a novel formulation improving the bioavailability of poorly absorbable drugs without any serious local damages."( Combinatorial use of sodium laurate with taurine or L-glutamine enhances colonic absorption of rebamipide, poorly absorbable antiulcer drug, without any serious histopathological mucosal damages.
Higaki, K; Kimura, T; Minami, T; Miyake, M; Odomi, M; Ogawara, K; Oka, Y; Toguchi, H, 2003
)
0.32
"To develop the safe formulation that can safely improve bioavailability of poorly absorbable drugs and that is practically available, we prepared the suppositories of rebamipide, a poorly soluble and poorly absorbable antiulcer drug, by employing the combinatorial use of sodium laurate (C12), an absorption enhancer, with taurine (Tau) or L-glutamine (L-Gln), an adjuvant exerting the cytoprotective action."( Development of suppository formulation safely improving rectal absorption of rebamipide, a poorly absorbable drug, by utilizing sodium laurate and taurine.
Higaki, K; Kamada, N; Kimura, T; Minami, T; Miyake, M; Mukai, T; Odomi, M; Ogawara, K; Oka, Y; Toguchi, H, 2004
)
0.32
" This study was conducted to examine if the rebamipide lysinate salt form would exhibit improved solubility profiles and higher oral bioavailability compared with rebamipide free acid."( Oral absorption and pharmacokinetics of rebamipide and rebamipide lysinate in rats.
Han, HS; Jun, YS; Kim, CH; Lee, KC; Rho, JI; Shin, BS; Yoo, SD; Yoon, CH, 2004
)
0.32
" Although Tau tended to attenuate the absorption-enhancing effect of C12, several C12-Tau suppositories kept high bioavailability values, which were much higher than control."( Optimization of suppository preparation containing sodium laurate and taurine that can safely improve rectal absorption of rebamipide.
Higaki, K; Kamada, N; Kato, Y; Kimura, T; Minami, T; Miyake, M; Mukai, T; Odomi, M; Ogawara, K; Oka, Y; Toguchi, H; Yamazaki, H, 2006
)
0.33
" Consequently, the bioavailability of rebamipide is under 10% in humans."( Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2011
)
0.37
" The bioavailability and efficacy of RBM solid dispersion were evaluated in a rat model."( Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2011
)
0.37
" Bioavailability and efficacy of rebamipide were increased significantly by solubility enhancement of the drug."( Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2011
)
0.37
" PK and PD studies in Sprague-Dawley rats revealed that the bioavailability of the drug using optimal SD was about twofold higher than that of reference product, and the irritation area of stomach was significantly reduced in the ulcer-induced rat model using optimal SD as compared to the reference product."( Physicochemical, pharmacokinetic and pharmacodynamic evaluations of novel ternary solid dispersion of rebamipide with poloxamer 407.
Chi, SC; Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2013
)
0.39
"The purpose of this study was to improve the gastric solubility and bioavailability of rebamipide (RBM) by preparing the RBM solid dispersion tablet (RBM-SDT) from solid dispersion powder prepared by spray-drying technique."( Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability.
Choi, HG; Choi, IS; Choi, JY; Kim, JO; Pradhan, R; Tran, TH; Yong, CS, 2015
)
0.42
"Rebamipide (RBP) is a potent anti-ulcer and anti-oxidative agent, which is a BCS class IV drug with a low oral bioavailability of less than 10%."( Capmul MCM/Solutol HS15-Based Microemulsion for Enhanced Oral Bioavailability of Rebamipide.
Cho, HJ; Kim, DD; Kim, KT; Lee, JY; Park, JH; Yoon, IS, 2017
)
0.46
"Rebamipide has low oral bioavailability (10%) due to its low solubility and permeability."( Lipid Nanoemulsions of Rebamipide: Formulation, Characterization, and In Vivo Evaluation of Pharmacokinetic and Pharmacodynamic Effects.
Guda, S; Narala, A; Veerabrahma, K, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Rebamipide, classified into BCS class IV, is one of those drugs which provide very low bioavailability and/or the difficulty of formulation for oral administration."( Improvement of lipid solubility and oral bioavailability of a poorly water- and poorly lipid-soluble drug, rebamipide, by utilizing its counter ion and SNEDDS preparation.
Higaki, K; Maruyama, M; Masuda, K; Ogawara, KI; Okawa, S; Sumimoto, Y, 2021
)
0.62
"In this study, a novel rebamipide-loaded spray-dried microsphere (RSM) with enhanced drug solubility and oral bioavailability has been developed utilizing meglumine, an alkalizing agent."( Development of rebamipide-loaded spray-dried microsphere using distilled water and meglumine: physicochemical characterization and pharmacokinetics in rats.
Cho, JH; Choi, HG; Ko, DW, 2021
)
0.62
"Rebamipide (REB) a potent anti-ulcer agent, has not been exploited to its full potential, owing to it extremely poor solubility, leading to highly diminutive bioavailability (<10%)."( Engineering a Remedy to Modulate and Optimize Biopharmaceutical Properties of Rebamipide by Synthesizing New Cocrystal: In Silico and Experimental Studies.
Chadha, R; Dureja, J; Jindal, A; Karan, M; Singh, R; Tomar, S, 2021
)
0.62
"5 folds enhancement in relative bioavailability and remarkable amplification in anti-ulcer, anti-inflammatory and the antioxidant potential of these cocrystals were observed."( Engineering a Remedy to Modulate and Optimize Biopharmaceutical Properties of Rebamipide by Synthesizing New Cocrystal: In Silico and Experimental Studies.
Chadha, R; Dureja, J; Jindal, A; Karan, M; Singh, R; Tomar, S, 2021
)
0.62
" Unexpectedly, despite enhanced dissolution rate in a controlled manner, a designed bilayer tablet had no dose- and dosage form dependent in vivo bioavailability in beagle dogs as compared with IR 100 mg RBM reference tablet."( Design and evaluation of in vivo bioavailability in beagle dogs of bilayer tablet consisting of immediate release nanosuspension and sustained release layers of rebamipide.
Cao, QR; Cui, JH; Jin, G; Jung, M; Lee, BJ; Ngo, HV; Park, C; Wang, J, 2022
)
0.72
"To develop an immediate-release tablet preparation containing rebamipide (RBM) and perform the bioavailability assessment in the healthy human subjects."( Immediate-release tablet formulation of rebamipide and a pharmacokinetic study in healthy human subjects.
Choi, YW; Goo, YT; Hong, SH; Kim, CH; Kim, MJ; Lee, TH; Sin, GH; Won, YH, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" Given intraperitoneally at the single dosing range of 10-100 mg/kg, OPC-12759 inhibited the formation of these acute gastric ulcer models."( Effect of OPC-12759, a novel antiulcer agent, on chronic and acute experimental gastric ulcer, and gastric secretion in rats.
Imaizumi, T; Ishiyama, H; Kanbe, T; Yabuuchi, Y; Yamasaki, K, 1989
)
0.28
" The dose-response relationship of indomethacin for inhibition of prostaglandin formation and rebamipide-induced protection correlated well and 5 mg/kg indomethacin completely prevented the protective effect of rebamipide."( Stimulation of prostaglandin biosynthesis mediates gastroprotective effect of rebamipide in rats.
Kleine, A; Kluge, S; Peskar, BM, 1993
)
0.29
" Sixty patients received 40 mg of omeprazole twice a day, 1500 mg of amoxicillin three times a day, and 300 mg of rebamipide three times a day (group OAR); the other 60 patients received the same dosage of omeprazole and amoxicillin but no rebamipide for two weeks (group OA)."( Effect of rebamipide on Helicobacter pylori infection in patients with peptic ulcer.
Ando, K; Arakawa, T; Harihara, S; Higuchi, K; Ito, H; Kobayashi, K; Kuroki, T; Nebiki, H; Uchida, T, 1998
)
0.3
" The competitive antagonistic action was further confirmed by the finding that rebamipide caused a parallel shift to the right in the dose-response curve of O2 production induced by fMLP."( Rebamipide suppresses formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide production by inhibiting fMLP-receptor binding in human neutrophils.
Azuma, A; Imagawa, K; Ishiyama, H; Kikuchi, M; Nagano, C; Sekiguchi, K, 2001
)
0.31
"Twenty patients with the active distal type of UC in whom corticosteroid treatment had been unsuccessful were treated with rectal administration of Rebamipide twice a day for 3 weeks, during which corticosteroid dosage was kept constant."( Rebamipide enema therapy as a treatment for patients with active distal ulcerative colitis.
Ando, T; Furuta, R; Goto, H; Ina, K; Ishiguro, K; Kusugami, K; Maeda, O; Watanabe, O, 2007
)
0.34
" Enemas containing 150 mg rebamipide per dosing were administered after morning bowel movement, and always prior to bedtime, twice daily for 4 weeks."( Rebampide enema therapy as a treatment for patients with chronic radiation proctitis: initial treatment or when other methods of conservative management have failed.
Cho, M; Heo, J; Kang, DH; Kim, GH; Kim, TO; Lee, SM; Song, GA, 2008
)
0.35
" The colonic and plasma concentrations were analyzed by high performance liquid chromatography (HPLC) to evaluate colon-targeting action after oral administration of various dosage forms, and rebamipide with absorption enhancers in chitosan dosage forms."( Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier.
Akira, Y; Duan, L; Huang, BB; Li, GF; Luo, JH; Nobuaki, K, 2008
)
0.35
" Vital signs (temperature, blood pressure, and heart rate) were measured before and after dosing in both periods."( Pharmacokinetics and bioequivalence of two formulations of rebamipide 100-mg tablets: a randomized, single-dose, two-period, two-sequence crossover study in healthy Korean male volunteers.
Cho, HY; Lee, YB; Park, GK; Yoon, H, 2009
)
0.35
"After taking into account the physiochemical properties of RBM (solubility, melting point, dosage etc."( Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2011
)
0.37
"A randomized, double-masked, multicenter, placebo-controlled, parallel-group, dose-response phase II study."( Rebamipide (OPC-12759) in the treatment of dry eye: a randomized, double-masked, multicenter, placebo-controlled phase II study.
Awamura, S; Kinoshita, S; Nakamichi, N; Oshiden, K; Suzuki, H; Yokoi, N, 2012
)
0.38
" The grade of gastric mucosal injuries was evaluated by esophagogastroduodenoscopy before and after dosing (on day 0 and day 14), and the grade of gastric mucosal injury was assessed according to the modified Lanza score."( A randomized, double-blind, placebo-controlled study of rebamipide for gastric mucosal injury taking aspirin with or without clopidogrel.
Fukui, H; Hida, N; Hori, K; Miwa, H; Nakamura, S; Ogawa, T; Ohda, Y; Okugawa, T; Oshima, T; Tomita, T; Tozawa, K; Watari, J, 2014
)
0.4
" The proposed methods have been successfully applied to the analysis of REB in pharmaceutical dosage forms without interference from other dosage form excipients."( Stability-indicating determination of rebamipide in the presence of its acid degradation products.
Abbas, SS; El-Bardicy, MG; Essam, HA; Zaazaa, HE,
)
0.13
" The optimized RBM-SD was formulated in tablet dosage form, containing approximately 2 % sodium lauryl sulphate and poloxamer F68 as wetting agents."( Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability.
Choi, HG; Choi, IS; Choi, JY; Kim, JO; Pradhan, R; Tran, TH; Yong, CS, 2015
)
0.42
"Rats were given either vehicle or rebamipide (30 mg/kg) orally twice daily for two days, then on the third day respective groups were dosed with either vehicle, celecoxib (40 mg/kg), or diclofenac (10 mg/kg) in addition to a respective dose of vehicle or rebamipide."( Celecoxib or diclofenac hepatic status in the presence or absence of rebamipide.
Denham, JW; Harirforoosh, S; Murrell, DE; Panus, PC; Rahmasari, Y, 2015
)
0.42
" The pretreatment period, dosing frequency, and dose dependency of rebamipide were examined."( Intra-oral administration of rebamipide liquid prevents tongue injuries induced by X-ray irradiation in rats.
Nakashima, T; Sakurai, K; Uematsu, N, 2017
)
0.46
" These methods are useful for analysis of REB in pharmaceutical dosage form."( Development and Validation of Four Spectrophotometric Methods for Assay of Rebamipide and its Impurity: Application to Tablet Dosage Form.
Alqarni, MA; El Ghobashy, MR; Farid, NF; Moatamed, RS; Naguib, IA, 2022
)
0.72
" Unexpectedly, despite enhanced dissolution rate in a controlled manner, a designed bilayer tablet had no dose- and dosage form dependent in vivo bioavailability in beagle dogs as compared with IR 100 mg RBM reference tablet."( Design and evaluation of in vivo bioavailability in beagle dogs of bilayer tablet consisting of immediate release nanosuspension and sustained release layers of rebamipide.
Cao, QR; Cui, JH; Jin, G; Jung, M; Lee, BJ; Ngo, HV; Park, C; Wang, J, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
[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 (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency35.19730.001310.157742.8575AID1259252; AID1259253
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency6.30960.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (45)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1661047Solubility of the compound in water
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1346809Rat CCK1 receptor (Cholecystokinin receptors)2004European journal of pharmacology, Nov-28, Volume: 505, Issue:1-3
Pharmacological characterization of rebamipide: its cholecystokinin CCK1 receptor binding profile and effects on Ca2+ mobilization and amylase release in rat pancreatic acinar cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (446)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (1.12)18.7374
1990's62 (13.90)18.2507
2000's138 (30.94)29.6817
2010's196 (43.95)24.3611
2020's45 (10.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 14.70

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 Index14.70 (24.57)
Research Supply Index6.29 (2.92)
Research Growth Index5.81 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (14.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials86 (18.94%)5.53%
Reviews35 (7.71%)6.00%
Case Studies11 (2.42%)4.05%
Observational1 (0.22%)0.25%
Other321 (70.70%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]