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Rebamipide

drug
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Also known as MucostaNSC-758955OPC-12759ProamipideRebamipidaRebatorSID26749027SID144205013SID174006202SID170465891

Summary

Rebamipide (CHEMBL1697771) is a phase-3 clinical-stage small molecule (ATC A02BX14) targeting CCKAR; indicated across 11 conditions including dry eye syndrome and peptic ulcer disease.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • ATC class: A02BX14
  • Targets: 1 (CCKAR)
  • Indications: 11 conditions
  • Clinical trials: 38
  • Chemistry: 370.8 Da · C19H15ClN2O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1697771
NameRebamipide
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID5042
ATCA02BX14
Molecular formulaC19H15ClN2O4
Molecular weight370.8
InChIKeyALLWOAVDORUJLA-UHFFFAOYSA-N

SMILES: C1=CC=C2C(=C1)C(=CC(=O)N2)CC(C(=O)O)NC(=O)C3=CC=C(C=C3)Cl

IUPAC name: 2-[(4-chlorobenzoyl)amino]-3-(2-oxo-1H-quinolin-4-yl)propanoic acid

Also known as: Mucosta, NSC-758955, OPC-12759, Proamipide, Rebamipida, Rebamipide, Rebator, SID26749027, REBAMIPIDE, SID144205013, SID174006202, SID170465891

Patent coverage: 1,011 distinct patent families (3,752 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,748 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
CCKARCCK1 receptorFull agonist4.40%P32238

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Ubiquitin-associated and SH3 domain-containing protein B.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 5 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
UBASH3B5.7Ki2000nMCHEMBL_ACT_25965922
UBASH3B5.7Ki2000nMCHEMBL_ACT_25965923
UBASH3B5.52IC503000nMCHEMBL_ACT_25965895
UBASH3B5.43IC503700nMCHEMBL_ACT_25965920
UBASH3B5.43IC503700nMCHEMBL_ACT_25965921

Target pathways

Aggregated over 1 target gene(s): CCKAR.

Top Reactome pathways

7 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction1CCKAR
Signaling by GPCR1CCKAR
Class A/1 (Rhodopsin-like receptors)1CCKAR
Peptide ligand-binding receptors1CCKAR
GPCR downstream signalling1CCKAR
G alpha (q) signalling events1CCKAR
GPCR ligand binding1CCKAR

Dominant GO biological processes

GO termTargets
neuron migration1
G protein-coupled receptor signaling pathway1
phospholipase C-activating G protein-coupled receptor signaling pathway1
axonogenesis1
forebrain development1
cellular response to hormone stimulus1
cholecystokinin signaling pathway1
regulation of hormone secretion1
signal transduction1

Indications & clinical

Indications

11 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
dry eye syndrome3MONDO:0006733EFO:1000906
peptic ulcer disease3MONDO:0004247HP:0004398
gastritis3MONDO:0004966EFO:0000217
chronic gastritis3MONDO:0005001EFO:0000337
ankylosing spondylitis3MONDO:0005306EFO:0003898
gastroesophageal reflux disease3MONDO:0007186EFO:0003948
gastric ulcer3MONDO:0001126EFO:0009454
rheumatoid arthritis3MONDO:0008383EFO:0000685
osteoarthritis3MONDO:0005178MONDO:0005178
ulcerative colitis2MONDO:0005101EFO:0000729
head and neck cancer2MONDO:0005627EFO:0006859

Clinical trials

Total trials: 38.

Phase distribution

PhaseTrials
PHASE412
PHASE311
PHASE26
Not specified5
PHASE1/PHASE22
PHASE12

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07397949PHASE4NOT_YET_RECRUITINGRebamipide Versus Diquafosol for Perioperative Dry Eye in Cataract Surgery
NCT00233389PHASE4COMPLETEDPost-marketing Clinical Study of Rebamipide in Patients With Gastric Ulcer
NCT00272467PHASE4COMPLETEDHealing Effects of Rebamipide and Omeprazole in Helicobacter Pylori-positive Gastric Ulcer After Eradication Therapy
NCT00641004PHASE4COMPLETEDRandomized Double-Blind Clinical Trial of Rebamipide vs Esomeprazole in the Treatment of NSAID-induced Gastropathy
NCT01817556PHASE4COMPLETEDA Study to Evaluate the Efficacy and of Stillen Tab. and to Demonstrate the Non-inferiority of Stillen Tab.
NCT02134405PHASE4UNKNOWNRebamipide in Combination With Esomeprazole in the Management of Asian Patients With Functional Dyspepsia
NCT02393430PHASE4COMPLETEDClinical Effect of Rebamipide on Chronic Gastritis
NCT02755753PHASE4COMPLETEDA Study to Evaluate REbamiPide as an Adjuvant Regimen to Heal erosIve Reflux Esophagitis
NCT03608761PHASE4COMPLETEDComparison Between Rebamipide 2% Versus Autologous Serum
NCT04885751PHASE4UNKNOWNCompare the Effect of Eupatilin and Rebamipide on the Prevention of Gastroenteropathy
NCT07354230PHASE4COMPLETEDGastroprotective Efficacy of Rebamipide in Patients With Atrial Fibrillation Treated With DOACs
NCT07397936PHASE4COMPLETEDRebamipide Versus Diquafosol and Cyclosporine for Perioperative Dry Eye in Cataract Surgery
NCT00201955PHASE3COMPLETEDStudy of Rebamipide Eye Drops to Treat Dry Eye
NCT00201981PHASE3COMPLETEDStudy of Rebamipide Eye Drops to Treat Dry Eye
NCT00576706PHASE3COMPLETEDPReventive Efficacy and Safety of rEbamipide on Nsaid Induced Mucosal Toxicity
NCT00996788PHASE3COMPLETEDAnti Free Radical & Anti Inflammatory Effect & Safety of Rebamipide in Chronic Gastritis
NCT01150162PHASE3COMPLETEDMucosta in Gastric Ulcer Treatment, Effectiveness and Safety Evaluation
NCT01632137PHASE3COMPLETEDEfficacy and Safety of Rebamipide in Subjects With Dry Eye Syndrome
NCT01660256PHASE3COMPLETEDConfirmatory Study of OPC-12759 Ophthalmic Solution
NCT01813812PHASE3UNKNOWNA Study to Evaluate the Efficacy and Safety of DA-6034 and to Demonstrate the Non-inferiority of DA-6034
NCT04066530PHASE3COMPLETEDA Study to Evaluate the Efficacy and Safety of AD-203
NCT04189705PHASE3COMPLETEDA Study to Evaluate the Efficacy and Safety of MCT-SR in Patients With Gastritis
NCT04649697PHASE3UNKNOWNRebamipide (Regular & Nanoparticulated) vs. Clobetasol in Management of Methotrexate-Induced Oral Ulceration in Rheumatoid Arthritis Patients
NCT00233363PHASE2COMPLETEDExploratory Study for Dry Mouth in Patients With Sjögren’s Syndrome
NCT00234078PHASE2COMPLETEDDose-response Study of OPC-12759 Ophthalmic Suspension
NCT00463151PHASE2COMPLETEDAn Exploratory Study of Rebamipide in Patients With Active Ulcerative Colitis
NCT01027013PHASE2COMPLETEDSafety and Efficacy Study of Rebamipide 2% Ophthalmic Suspension in Patients With Dry Eye
NCT01057147PHASE2COMPLETEDSafety and Efficacy Study of Rebamipide 2% Ophthalmic Suspension in Subjects With Dry Eye - Effects on Central Cornea
NCT03437785PHASE2COMPLETEDClinical Trial to Evaluate the Efficacy and Safety of CKD-495 Tablet
NCT05166304PHASE1/PHASE2COMPLETEDRebamipide in Patients With Active Rheumatoid Arthritis
NCT06084624PHASE1/PHASE2UNKNOWNEvaluation of Topical Rebamipide Versus Topical Betamethasone for Management of Oral Ulcers in Behcet’s Disease
NCT01549743PHASE1COMPLETEDThe Pharmacokinetic Interaction Between Celecoxib and Rebamipide
NCT02106130PHASE1COMPLETEDA Drug Interaction Study of Mosapride and Rebamipide
NCT00862628Not specifiedUNKNOWNThe Effect of Rebamipide for Non-steroidal Anti-inflammatory Drugs (NSAID) - Induced Small-intestinal Injuries
NCT01167101Not specifiedCOMPLETEDIs Rebamipide Effective on the Healing of Iatrogenic Gastric Ulcer After Endoscopic Mucosal Resection?
NCT01759108Not specifiedUNKNOWNRebamipide AND Sjögren Syndrome
NCT02243618Not specifiedCOMPLETEDThe Effect of Proton Pump Inhibitor and Polaprezinc Combination Therapy for Healing of Endoscopic Submucosal Dissection-induced Ulcer
NCT04550858Not specifiedUNKNOWNh.Pylori Ttt With Rebamipide

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

101 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)CCKAR
ATAZANAVIRChEMBL + PubChemPhase 4 (approved)CCKAR
RIFAMPINChEMBL + PubChemPhase 4 (approved)CCKAR
AMSACRINEChEMBLPhase 4 (approved)CCKAR
BEPRIDILChEMBLPhase 4 (approved)CCKAR
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)CCKAR
CANNABIDIOLChEMBLPhase 4 (approved)CCKAR
CHLORDIAZEPOXIDEChEMBLPhase 4 (approved)CCKAR
CHLORHEXIDINEChEMBLPhase 4 (approved)CCKAR
DASATINIBChEMBLPhase 4 (approved)CCKAR
DAUNORUBICINChEMBLPhase 4 (approved)CCKAR
DESERPIDINEChEMBLPhase 4 (approved)CCKAR
ERLOTINIBChEMBLPhase 4 (approved)CCKAR
FLUVASTATINChEMBLPhase 4 (approved)CCKAR
HYDROXOCOBALAMINChEMBLPhase 4 (approved)CCKAR
INDOCYANINE GREEN ACID FORMChEMBLPhase 4 (approved)CCKAR
LETERMOVIRChEMBLPhase 4 (approved)CCKAR
LURASIDONEChEMBLPhase 4 (approved)CCKAR
NEFAZODONEChEMBLPhase 4 (approved)CCKAR
NIMESULIDEChEMBLPhase 4 (approved)CCKAR
NITAZOXANIDEChEMBLPhase 4 (approved)CCKAR
OSIMERTINIBChEMBLPhase 4 (approved)CCKAR
PACLITAXELChEMBLPhase 4 (approved)CCKAR
PIMOZIDEChEMBLPhase 4 (approved)CCKAR
RAMATROBANChEMBLPhase 4 (approved)CCKAR
RIFAXIMINChEMBLPhase 4 (approved)CCKAR
RIMONABANTChEMBLPhase 4 (approved)CCKAR
RITONAVIRChEMBLPhase 4 (approved)CCKAR
SINCALIDEChEMBLPhase 4 (approved)CCKAR
SUNITINIBChEMBLPhase 4 (approved)CCKAR
TELMISARTANChEMBLPhase 4 (approved)CCKAR
TELOTRISTATChEMBLPhase 4 (approved)CCKAR
TELOTRISTAT ETHYLChEMBLPhase 4 (approved)CCKAR
TIPRANAVIRChEMBLPhase 4 (approved)CCKAR
CE-326597ChEMBLPhase 2CCKAR
DEVAZEPIDEChEMBLPhase 2CCKAR
DIPERODONChEMBLPhase 2CCKAR
LINTITRIPTChEMBLPhase 2CCKAR
LOXIGLUMIDEChEMBLPhase 2CCKAR
NETAZEPIDEChEMBLPhase 2CCKAR
PIRENOXINEChEMBLPhase 2CCKAR
AbirateronePubChemApprovedCCKAR
acetylcysteinePubChemApprovedCCKAR
Aclidinium BromidePubChemApprovedCCKAR
AcyclovirPubChemApprovedCCKAR
AllopurinolPubChemApprovedCCKAR
AlmotriptanPubChemApprovedCCKAR
AlogliptinPubChemApprovedCCKAR
aminolevulinic acidPubChemApprovedCCKAR
AnagrelidePubChemApprovedCCKAR
ApixabanPubChemApprovedCCKAR
ApremilastPubChemApprovedCCKAR
AprepitantPubChemApprovedCCKAR
BinimetinibPubChemApprovedCCKAR
BosentanPubChemApprovedCCKAR
CapsaicinPubChemApprovedCCKAR
chenodiolPubChemApprovedCCKAR
CinacalcetPubChemApprovedCCKAR
ClofarabinePubChemApprovedCCKAR
ClozapinePubChemApprovedCCKAR

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot