◎ Sugi Atlas

Atlas / Drug / Proglumide

Proglumide

drug
On this page

Also known as BinosideCR-242Dl-proglumideGastrotopicMidelidMilidNSC-757841NulsaProglumidaPromidUlcutinW-5219XydeXylamideSID26747589SID50106676SID56463359SID90341320SID144204108

Summary

Proglumide (CHEMBL316561) is an approved small-molecule cholinergic antagonist (ATC A02BX06) targeting CCKAR; indicated across 5 conditions including peptic ulcer disease and gastroesophageal reflux disease.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: A02BX06
  • Targets: 1 (CCKAR)
  • Indications: 5 conditions
  • Clinical trials: 4
  • Chemistry: 334.4 Da · C18H26N2O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL316561
NameProglumide
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID4922
ChEBICHEBI:32058
ATCA02BX06
Molecular formulaC18H26N2O4
Molecular weight334.4
InChIKeyDGMKFQYCZXERLX-UHFFFAOYSA-N

SMILES: CCCN(CCC)C(=O)C(CCC(=O)O)NC(=O)C1=CC=CC=C1

IUPAC name: 4-benzamido-5-(dipropylamino)-5-oxopentanoic acid

ChEBI definition: A racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for treatment of stomach ulcers, but has been replaced by newer drugs.

Pharmacological roles (ChEBI): cholinergic antagonist, anti-ulcer drug, cholecystokinin antagonist, gastrointestinal drug, δ-opioid receptor agonist, opioid analgesic.

Other ChEBI roles (chemical / environmental): drug metabolite, xenobiotic metabolite.

Also known as: Binoside, CR-242, Dl-proglumide, Gastrotopic, Midelid, Milid, NSC-757841, Nulsa, Proglumida, Proglumide, Promid, Ulcutin

Parent form; salt/anhydrous children: CHEMBL1345380

Patent coverage: 1,199 distinct patent families (3,510 SureChEMBL compound mentions), from 1 matched compound structure(s). 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 receptorAntagonist2.20%P32238

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Endonuclease 4, Beta-lactamase, Histamine H2 receptor.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P008115.1Potency7943nMCHEMBL_ACT_4695511

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

5 indications (2 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
peptic ulcer disease4MONDO:0004247HP:0004398
gastroesophageal reflux disease4MONDO:0007186EFO:0003948
metabolic dysfunction-associated steatohepatitis1MONDO:0007027EFO:1001249
exocrine pancreatic carcinoma1MONDO:0005192EFO:0002618
cirrhosis of liver0MONDO:0005155EFO:0001422

Clinical trials

Total trials: 4.

Phase distribution

PhaseTrials
PHASE1/PHASE21
PHASE21
PHASE11
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05551858PHASE1/PHASE2ACTIVE_NOT_RECRUITINGRole of a CCK Receptor Antagonist Proglumide in Management of Chronic Pancreatitis
NCT05827055PHASE2ACTIVE_NOT_RECRUITINGProglumide and Chemotherapy for Metastatic Pancreatic Cancer
NCT04152473PHASE1COMPLETEDSafety and Tolerability of Oral Proglumide for NASH
NCT04814602EARLY_PHASE1COMPLETEDSingle-dose PK Assessment of Oral Proglumide in Those With Hepatic Impairment

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