Galantamine

drug
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Also known as (-)-galantamine(-)-galanthamineAcumor xlConsion xlElmino xlGalantaminaGalanthamineGalsya xlGalzemic xlGatalin xlGazylan xlLotprosin xlLuventa xlNSC-100058ReminylReminyl xlZeebral xlSID26751839SID26732575

Summary

Galantamine (CHEMBL659) is an approved small-molecule EC 3.1.1.7 (acetylcholinesterase) inhibitor (ATC N06DA04) targeting ACHE; indicated across 17 conditions including dementia and autism.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N06DA04
  • Targets: 1 (ACHE)
  • Indications: 17 conditions
  • Clinical trials: 64
  • Chemistry: 287.35 Da · C17H21NO3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL659
NameGalantamine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID9651
ChEBICHEBI:42944
ATCN06DA04
Molecular formulaC17H21NO3
Molecular weight287.35
InChIKeyASUTZQLVASHGKV-JDFRZJQESA-N

SMILES: CN1CC[C@@]23C=C[C@@H](C[C@@H]2OC4=C(C=CC(=C34)C1)OC)O

IUPAC name: (1S,12S,14R)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-ol

ChEBI definition: A benzazepine alkaloid isolated from certain species of daffodils.

Pharmacological roles (ChEBI): antidote to curare poisoning, EC 3.1.1.7 (acetylcholinesterase) inhibitor, cholinergic drug, EC 3.1.1.8 (cholinesterase) inhibitor.

Other ChEBI roles (chemical / environmental): plant metabolite.

Also known as: (-)-galantamine, (-)-galanthamine, Acumor xl, Consion xl, Elmino xl, Galantamina, Galantamine, Galanthamine, Galsya xl, Galzemic xl, Gatalin xl, Gazylan xl

Parent form; salt/anhydrous children: CHEMBL1555, CHEMBL3099484, CHEMBL4467191

Patent coverage: 8,565 distinct patent families (30,894 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 30,859 (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
ACHEacetylcholinesterase (Yt blood group)Inhibition6.39.6%P22303

Broader ChEMBL bioactivity targets: 11 (assay-derived). Sample: Prelamin-A/C, Cholinesterase, Acetylcholinesterase, Mu-type opioid receptor, Acetylcholinesterase, Acetylcholinesterase, Aldehyde dehydrogenase 1A1, Acetylcholinesterase, Acetylcholinesterase, Acetylcholinesterase.

Bioactivity

ChEMBL activities: 230 potent at pChembl ≥ 5 of 314 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
BCHE7.29IC5051nMCHEMBL_ACT_26036842
ACHE7.21Ki61.96nMCHEMBL_ACT_12071725
ACHE7.21Ki61.9nMCHEMBL_ACT_15013159
ACHE7IC50100nMCHEMBL_ACT_1143320
O422756.88IC50132nMCHEMBL_ACT_25618360
O422756.82IC50150nMCHEMBL_ACT_24708487
BCHE6.77IC50170nMCHEMBL_ACT_12405209
BCHE6.72Ki192.5nMCHEMBL_ACT_12071714
BCHE6.72Ki192.5nMCHEMBL_ACT_15013193
ACHE6.7IC50200nMCHEMBL_ACT_29288220
ACHE6.6Ki250nMCHEMBL_ACT_15631658
O422756.6IC50250nMCHEMBL_ACT_18343571
ACHE6.52IC50300nMCHEMBL_ACT_10850827
ACHE6.52IC50300nMCHEMBL_ACT_12633737
ACHE6.52IC50300nMCHEMBL_ACT_16597912
ACHE6.52IC50300nMCHEMBL_ACT_18793814
ACHE6.52Ki300nMCHEMBL_ACT_3423608
ACHE6.46IC50350nMCHEMBL_ACT_15762381
ACHE6.46IC50350nMCHEMBL_ACT_2341359
ACHE6.46IC50350nMCHEMBL_ACT_24998158
ACHE6.46IC50350nMCHEMBL_ACT_25083740
ACHE6.46IC50350nMCHEMBL_ACT_6180552
ACHE6.45IC50355nMCHEMBL_ACT_18124230
O422756.44IC50360nMCHEMBL_ACT_1991204
P040586.44IC50360nMCHEMBL_ACT_586329
O422756.44IC50360nMCHEMBL_ACT_600386
O422756.37Ki428nMCHEMBL_ACT_3408859
O422756.36Ki440nMCHEMBL_ACT_1676972
O422756.32IC50480nMCHEMBL_ACT_16664631
O422756.3IC50500nMCHEMBL_ACT_12389968

Target pathways

Aggregated over 1 target gene(s): ACHE.

Top Reactome pathways

11 total, by targets touching each:

PathwayTargetsGenes
Neurotransmitter clearance1ACHE
Transmission across Chemical Synapses1ACHE
Neuronal System1ACHE
Metabolism1ACHE
Synthesis of PC1ACHE
Glycerophospholipid biosynthesis1ACHE
Phospholipid metabolism1ACHE
Peptide hormone metabolism1ACHE
Metabolism of proteins1ACHE
Synthesis, secretion, and deacylation of Ghrelin1ACHE
Metabolism of lipids1ACHE

Dominant GO biological processes

GO termTargets
acetylcholine catabolic process in synaptic cleft1
regulation of receptor recycling1
osteoblast development1
acetylcholine catabolic process1
cell adhesion1
nervous system development1
synapse assembly1
receptor internalization1
negative regulation of synaptic transmission, cholinergic1
amyloid precursor protein metabolic process1
positive regulation of protein secretion1
retina development in camera-type eye1
acetylcholine receptor signaling pathway1
positive regulation of cold-induced thermogenesis1

Indications & clinical

Indications

17 indications (1 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
dementia4MONDO:0001627HP:0000726
autism3MONDO:0005260EFO:0003758
vascular dementia3MONDO:0004648EFO:0004718
anxiety3MONDO:0011918EFO:0005230
Lewy body dementia3MONDO:0007488EFO:0006792
depressive disorder3MONDO:0002050MONDO:0002050
Alzheimer disease3MONDO:0004975MONDO:0004975
nicotine dependence2MONDO:0008575EFO:0003768
cocaine dependence2MONDO:0005186EFO:0002610
HIV infectious disease2MONDO:0005109EFO:0000764
schizoaffective disorder2MONDO:0005487EFO:0005411
obesity disorder1MONDO:0011122EFO:0001073
subarachnoid hemorrhage1MONDO:0005099EFO:0000713
orthostatic hypotension1MONDO:0005469EFO:0005252

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 64.

Phase distribution

PhaseTrials
PHASE418
Not specified13
PHASE310
PHASE29
PHASE19
PHASE2/PHASE33
PHASE1/PHASE22

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00035204PHASE4COMPLETEDA Study of the Effects on Sleep, Attention, and Gastrointestinal Tolerance of Galantamine and Donepezil in Patients With Alzheimer’s Disease
NCT00164242PHASE4COMPLETEDTreatment of Tardive Dyskinesia With Galantamine
NCT00176423PHASE4COMPLETEDEfficacy Study of Galantamine for Cognitive Impairments in Schizophrenia
NCT00195845PHASE4COMPLETEDA Double-Blind, Placebo-Controlled Study of Galantamine to Improve Cognitive Dysfunction in Bipolar Disorder
NCT00219869PHASE4UNKNOWNGalantamine in the Treatment of Post-Traumatic Headache
NCT00226824PHASE4TERMINATEDSafety Study of Galantamine in Tic Disorders
NCT00227994PHASE4COMPLETEDAcetylcholinesterase Inhibitors to Improve Cognitive Function and Overall Rehabilitation After a Stroke
NCT00232349PHASE4TERMINATEDEfficacy of Galantamine to Treat Schizophrenia
NCT00320736PHASE4COMPLETEDGalantamine for Cognition in People With Schizophrenia
NCT00423969PHASE4TERMINATEDGalantamine Augmentation of Escitalopram for Treatment of Depression
NCT00523666PHASE4UNKNOWNDiffusion Tensor Weighted MRI in Alzheimer’s Disease Modifying Treatment Effects of Galantamine (Reminyl®)
NCT00626613PHASE4UNKNOWNThe Relationship Between Risperdal Treatment and Quality of Life in Patients With Alzheimer’s Disease and Behavioural and Psychological Symptoms of Dementia (BPSD)
NCT00741598PHASE4COMPLETEDEfficacy and Safety of Galantamine for Improving Dysfunction in People With Bipolar Disorder
NCT00814658PHASE4COMPLETEDThe Use of Galantamine (Reminyl ER) in Patients With MIXed Dementia: Effects on Cognition and Quality of Life
NCT01054976PHASE4COMPLETEDThe Efficacy of Galantamine Treatment on Attention in Patients With Alzheimer’s Disease
NCT01181921PHASE4TERMINATEDThe CIRCADIAN Study: Evaluation of Modulating Effect of Galantamine on Circadian Rhythm in Patients With Mild to Moderate Alzheimer’s Disease
NCT01478633PHASE4COMPLETEDEvaluation of Efficacy and Safety of Galantamine in Patients With Dementia of Alzheimer’s Type Who Failed to Benefit From Donepezil
NCT02283242PHASE4COMPLETEDGalantamine Effects in Patients With Metabolic Syndrome
NCT07003386PHASE2/PHASE3RECRUITINGExploration of the Efficacy and Mechanism of Galantamine (an Extract From Lycoris Aurea) in Treating Ischemic Stroke
NCT00000172PHASE3COMPLETEDEvaluation of Galantamine in the Treatment of Alzheimer’s Disease
NCT00035191PHASE3COMPLETEDA Placebo-controlled Trial to Evaluate the Safety and Efficacy of Galantamine in the Treatment of Vascular Dementia
NCT00230997PHASE3COMPLETEDSafety and Efficacy of Galantamine in Patients With Dementia With Lewy Bodies
NCT00252603PHASE3COMPLETEDGalantamine Versus Placebo in Childhood Autism
NCT00301574PHASE3COMPLETEDAn Efficacy and Safety Study of Galantamine for the Treatment of Patients With Alzheimer’s Disease.
NCT00304629PHASE3COMPLETEDLong-term Safety and Efficacy of Galantamine in Alzheimer’s Disease
NCT00309725PHASE3COMPLETEDA Cardiac Safety Study of Galantamine in the Treatment of Alzheimer’s Disease.
NCT00463879PHASE2/PHASE3COMPLETEDGalantamine for Cognitive Deficits in Schizophrenia
NCT00679627PHASE3TERMINATEDA Study of Galantamine Used to Treat Patients With Mild to Moderate Alzheimer’s Disease
NCT00814801PHASE3COMPLETEDAn Efficacy and Safety Study of Galantamine for the Treatment of Patients With Alzheimer’s Disease
NCT02098824PHASE2/PHASE3UNKNOWNSymptomatic Treatment of Vascular Cognitive Impairment
NCT02374567PHASE3TERMINATEDPharmacovigilance in Gerontopsychiatric Patients
NCT04769206PHASE1/PHASE2RECRUITINGEnhancing Parasympathetic Activity to Improve Endothelial Dysfunction, Vascular Oxidative Stress in African Americans
NCT00509067PHASE2COMPLETEDUse of Galantamine and CDP-choline (Citicoline) to Treat Adults With Schizophrenia
NCT00809835PHASE2COMPLETEDGalantamine to Enhance Cognitive Behavioral Therapy for Cocaine Abuse
NCT01012167PHASE2COMPLETEDOxytocin or Galantamine Versus Placebo for the Treatment of Negative Symptoms and Cognitive Impairments in Schizophrenia
NCT01100775PHASE2COMPLETEDEffects of Galantamine on Cognition
NCT01416948PHASE2TERMINATEDCognitive REmediation After Trauma Exposure Trial = CREATE Trial
NCT01508494PHASE2COMPLETEDCognitive Rehabilitation and Galantamine for Post Stroke Cognitive Impairment
NCT01669538PHASE2COMPLETEDEffect of Galantamine on Short-term Abstinence
NCT01677754PHASE2COMPLETEDA Study of RO4602522 in Participants With Moderate Severity Alzheimer Disease on Background Alzheimer Disease Therapy

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 4 clinical and 38 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

MoleculeSourceStatusShared targets
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)ACHE
PAZOPANIBChEMBL + PubChemPhase 4 (approved)ACHE
TADALAFILChEMBL + PubChemPhase 4 (approved)ACHE
ALFUZOSINChEMBLPhase 4 (approved)ACHE
ARIPIPRAZOLEChEMBLPhase 4 (approved)ACHE
BERBERINEChEMBLPhase 4 (approved)ACHE
BOSUTINIBChEMBLPhase 4 (approved)ACHE
BROMOCRIPTINEChEMBLPhase 4 (approved)ACHE
BUTENAFINEChEMBLPhase 4 (approved)ACHE
CABERGOLINEChEMBLPhase 4 (approved)ACHE
CAFFEINEChEMBLPhase 4 (approved)ACHE
CANNABIDIOLChEMBLPhase 4 (approved)ACHE
CITALOPRAMChEMBLPhase 4 (approved)ACHE
CLOTRIMAZOLEChEMBLPhase 4 (approved)ACHE
DECAMETHONIUMChEMBLPhase 4 (approved)ACHE
DECAMETHONIUM BROMIDEChEMBLPhase 4 (approved)ACHE
DEQUALINIUMChEMBLPhase 4 (approved)ACHE
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)ACHE
DISULFIRAMChEMBLPhase 4 (approved)ACHE
DOFETILIDEChEMBLPhase 4 (approved)ACHE
DONEPEZILChEMBLPhase 4 (approved)ACHE
DYCLONINEChEMBLPhase 4 (approved)ACHE
EBASTINEChEMBLPhase 4 (approved)ACHE
ECONAZOLEChEMBLPhase 4 (approved)ACHE
EDROPHONIUMChEMBLPhase 4 (approved)ACHE
EDROPHONIUM CHLORIDEChEMBLPhase 4 (approved)ACHE
EPIRUBICINChEMBLPhase 4 (approved)ACHE
ETHOPROPAZINEChEMBLPhase 4 (approved)ACHE
ETHYLESTRENOLChEMBLPhase 4 (approved)ACHE
FENOFIBRATEChEMBLPhase 4 (approved)ACHE
FLAVOXATEChEMBLPhase 4 (approved)ACHE
FLUOXETINEChEMBLPhase 4 (approved)ACHE
GALLAMINEChEMBLPhase 4 (approved)ACHE
HEXACHLOROPHENEChEMBLPhase 4 (approved)ACHE
HEXAFLUORENIUMChEMBLPhase 4 (approved)ACHE
ILOPERIDONEChEMBLPhase 4 (approved)ACHE
IRINOTECANChEMBLPhase 4 (approved)ACHE
ISOFLUROPHATEChEMBLPhase 4 (approved)ACHE
LEVALLORPHANChEMBLPhase 4 (approved)ACHE
LORLATINIBChEMBLPhase 4 (approved)ACHE
LURASIDONEChEMBLPhase 4 (approved)ACHE
MELPHALANChEMBLPhase 4 (approved)ACHE
MEMANTINEChEMBLPhase 4 (approved)ACHE
MEPTAZINOLChEMBLPhase 4 (approved)ACHE
METHOXSALENChEMBLPhase 4 (approved)ACHE
MICONAZOLEChEMBLPhase 4 (approved)ACHE
MINAPRINEChEMBLPhase 4 (approved)ACHE
NAFTOPIDILChEMBLPhase 4 (approved)ACHE
NEFAZODONEChEMBLPhase 4 (approved)ACHE
NEOSTIGMINEChEMBLPhase 4 (approved)ACHE
NEOSTIGMINE METHYLSULFATEChEMBLPhase 4 (approved)ACHE
NICERGOLINEChEMBLPhase 4 (approved)ACHE
NIZATIDINEChEMBLPhase 4 (approved)ACHE
ORLISTATChEMBLPhase 4 (approved)ACHE
OXICONAZOLEChEMBLPhase 4 (approved)ACHE
PALBOCICLIBChEMBLPhase 4 (approved)ACHE
PENTAMIDINEChEMBLPhase 4 (approved)ACHE
PENTOXIFYLLINEChEMBLPhase 4 (approved)ACHE
PERICIAZINEChEMBLPhase 4 (approved)ACHE
PHYSOSTIGMINEChEMBLPhase 4 (approved)ACHE