Galantamine
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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
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL659 |
| Name | Galantamine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 9651 |
| ChEBI | CHEBI:42944 |
| ATC | N06DA04 |
| Molecular formula | C17H21NO3 |
| Molecular weight | 287.35 |
| InChIKey | ASUTZQLVASHGKV-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).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| ACHE | acetylcholinesterase (Yt blood group) | Inhibition | 6.3 | 9.6% | 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):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| BCHE | 7.29 | IC50 | 51 | nM | CHEMBL_ACT_26036842 |
| ACHE | 7.21 | Ki | 61.96 | nM | CHEMBL_ACT_12071725 |
| ACHE | 7.21 | Ki | 61.9 | nM | CHEMBL_ACT_15013159 |
| ACHE | 7 | IC50 | 100 | nM | CHEMBL_ACT_1143320 |
| O42275 | 6.88 | IC50 | 132 | nM | CHEMBL_ACT_25618360 |
| O42275 | 6.82 | IC50 | 150 | nM | CHEMBL_ACT_24708487 |
| BCHE | 6.77 | IC50 | 170 | nM | CHEMBL_ACT_12405209 |
| BCHE | 6.72 | Ki | 192.5 | nM | CHEMBL_ACT_12071714 |
| BCHE | 6.72 | Ki | 192.5 | nM | CHEMBL_ACT_15013193 |
| ACHE | 6.7 | IC50 | 200 | nM | CHEMBL_ACT_29288220 |
| ACHE | 6.6 | Ki | 250 | nM | CHEMBL_ACT_15631658 |
| O42275 | 6.6 | IC50 | 250 | nM | CHEMBL_ACT_18343571 |
| ACHE | 6.52 | IC50 | 300 | nM | CHEMBL_ACT_10850827 |
| ACHE | 6.52 | IC50 | 300 | nM | CHEMBL_ACT_12633737 |
| ACHE | 6.52 | IC50 | 300 | nM | CHEMBL_ACT_16597912 |
| ACHE | 6.52 | IC50 | 300 | nM | CHEMBL_ACT_18793814 |
| ACHE | 6.52 | Ki | 300 | nM | CHEMBL_ACT_3423608 |
| ACHE | 6.46 | IC50 | 350 | nM | CHEMBL_ACT_15762381 |
| ACHE | 6.46 | IC50 | 350 | nM | CHEMBL_ACT_2341359 |
| ACHE | 6.46 | IC50 | 350 | nM | CHEMBL_ACT_24998158 |
| ACHE | 6.46 | IC50 | 350 | nM | CHEMBL_ACT_25083740 |
| ACHE | 6.46 | IC50 | 350 | nM | CHEMBL_ACT_6180552 |
| ACHE | 6.45 | IC50 | 355 | nM | CHEMBL_ACT_18124230 |
| O42275 | 6.44 | IC50 | 360 | nM | CHEMBL_ACT_1991204 |
| P04058 | 6.44 | IC50 | 360 | nM | CHEMBL_ACT_586329 |
| O42275 | 6.44 | IC50 | 360 | nM | CHEMBL_ACT_600386 |
| O42275 | 6.37 | Ki | 428 | nM | CHEMBL_ACT_3408859 |
| O42275 | 6.36 | Ki | 440 | nM | CHEMBL_ACT_1676972 |
| O42275 | 6.32 | IC50 | 480 | nM | CHEMBL_ACT_16664631 |
| O42275 | 6.3 | IC50 | 500 | nM | CHEMBL_ACT_12389968 |
Target pathways
Aggregated over 1 target gene(s): ACHE.
Top Reactome pathways
11 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Neurotransmitter clearance | 1 | ACHE |
| Transmission across Chemical Synapses | 1 | ACHE |
| Neuronal System | 1 | ACHE |
| Metabolism | 1 | ACHE |
| Synthesis of PC | 1 | ACHE |
| Glycerophospholipid biosynthesis | 1 | ACHE |
| Phospholipid metabolism | 1 | ACHE |
| Peptide hormone metabolism | 1 | ACHE |
| Metabolism of proteins | 1 | ACHE |
| Synthesis, secretion, and deacylation of Ghrelin | 1 | ACHE |
| Metabolism of lipids | 1 | ACHE |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| acetylcholine catabolic process in synaptic cleft | 1 |
| regulation of receptor recycling | 1 |
| osteoblast development | 1 |
| acetylcholine catabolic process | 1 |
| cell adhesion | 1 |
| nervous system development | 1 |
| synapse assembly | 1 |
| receptor internalization | 1 |
| negative regulation of synaptic transmission, cholinergic | 1 |
| amyloid precursor protein metabolic process | 1 |
| positive regulation of protein secretion | 1 |
| retina development in camera-type eye | 1 |
| acetylcholine receptor signaling pathway | 1 |
| positive regulation of cold-induced thermogenesis | 1 |
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).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| dementia | 4 | MONDO:0001627 | HP:0000726 |
| autism | 3 | MONDO:0005260 | EFO:0003758 |
| vascular dementia | 3 | MONDO:0004648 | EFO:0004718 |
| anxiety | 3 | MONDO:0011918 | EFO:0005230 |
| Lewy body dementia | 3 | MONDO:0007488 | EFO:0006792 |
| depressive disorder | 3 | MONDO:0002050 | MONDO:0002050 |
| Alzheimer disease | 3 | MONDO:0004975 | MONDO:0004975 |
| nicotine dependence | 2 | MONDO:0008575 | EFO:0003768 |
| cocaine dependence | 2 | MONDO:0005186 | EFO:0002610 |
| HIV infectious disease | 2 | MONDO:0005109 | EFO:0000764 |
| schizoaffective disorder | 2 | MONDO:0005487 | EFO:0005411 |
| obesity disorder | 1 | MONDO:0011122 | EFO:0001073 |
| subarachnoid hemorrhage | 1 | MONDO:0005099 | EFO:0000713 |
| orthostatic hypotension | 1 | MONDO:0005469 | EFO: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
| Phase | Trials |
|---|---|
| PHASE4 | 18 |
| Not specified | 13 |
| PHASE3 | 10 |
| PHASE2 | 9 |
| PHASE1 | 9 |
| PHASE2/PHASE3 | 3 |
| PHASE1/PHASE2 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00035204 | PHASE4 | COMPLETED | A Study of the Effects on Sleep, Attention, and Gastrointestinal Tolerance of Galantamine and Donepezil in Patients With Alzheimer’s Disease |
| NCT00164242 | PHASE4 | COMPLETED | Treatment of Tardive Dyskinesia With Galantamine |
| NCT00176423 | PHASE4 | COMPLETED | Efficacy Study of Galantamine for Cognitive Impairments in Schizophrenia |
| NCT00195845 | PHASE4 | COMPLETED | A Double-Blind, Placebo-Controlled Study of Galantamine to Improve Cognitive Dysfunction in Bipolar Disorder |
| NCT00219869 | PHASE4 | UNKNOWN | Galantamine in the Treatment of Post-Traumatic Headache |
| NCT00226824 | PHASE4 | TERMINATED | Safety Study of Galantamine in Tic Disorders |
| NCT00227994 | PHASE4 | COMPLETED | Acetylcholinesterase Inhibitors to Improve Cognitive Function and Overall Rehabilitation After a Stroke |
| NCT00232349 | PHASE4 | TERMINATED | Efficacy of Galantamine to Treat Schizophrenia |
| NCT00320736 | PHASE4 | COMPLETED | Galantamine for Cognition in People With Schizophrenia |
| NCT00423969 | PHASE4 | TERMINATED | Galantamine Augmentation of Escitalopram for Treatment of Depression |
| NCT00523666 | PHASE4 | UNKNOWN | Diffusion Tensor Weighted MRI in Alzheimer’s Disease Modifying Treatment Effects of Galantamine (Reminyl®) |
| NCT00626613 | PHASE4 | UNKNOWN | The Relationship Between Risperdal Treatment and Quality of Life in Patients With Alzheimer’s Disease and Behavioural and Psychological Symptoms of Dementia (BPSD) |
| NCT00741598 | PHASE4 | COMPLETED | Efficacy and Safety of Galantamine for Improving Dysfunction in People With Bipolar Disorder |
| NCT00814658 | PHASE4 | COMPLETED | The Use of Galantamine (Reminyl ER) in Patients With MIXed Dementia: Effects on Cognition and Quality of Life |
| NCT01054976 | PHASE4 | COMPLETED | The Efficacy of Galantamine Treatment on Attention in Patients With Alzheimer’s Disease |
| NCT01181921 | PHASE4 | TERMINATED | The CIRCADIAN Study: Evaluation of Modulating Effect of Galantamine on Circadian Rhythm in Patients With Mild to Moderate Alzheimer’s Disease |
| NCT01478633 | PHASE4 | COMPLETED | Evaluation of Efficacy and Safety of Galantamine in Patients With Dementia of Alzheimer’s Type Who Failed to Benefit From Donepezil |
| NCT02283242 | PHASE4 | COMPLETED | Galantamine Effects in Patients With Metabolic Syndrome |
| NCT07003386 | PHASE2/PHASE3 | RECRUITING | Exploration of the Efficacy and Mechanism of Galantamine (an Extract From Lycoris Aurea) in Treating Ischemic Stroke |
| NCT00000172 | PHASE3 | COMPLETED | Evaluation of Galantamine in the Treatment of Alzheimer’s Disease |
| NCT00035191 | PHASE3 | COMPLETED | A Placebo-controlled Trial to Evaluate the Safety and Efficacy of Galantamine in the Treatment of Vascular Dementia |
| NCT00230997 | PHASE3 | COMPLETED | Safety and Efficacy of Galantamine in Patients With Dementia With Lewy Bodies |
| NCT00252603 | PHASE3 | COMPLETED | Galantamine Versus Placebo in Childhood Autism |
| NCT00301574 | PHASE3 | COMPLETED | An Efficacy and Safety Study of Galantamine for the Treatment of Patients With Alzheimer’s Disease. |
| NCT00304629 | PHASE3 | COMPLETED | Long-term Safety and Efficacy of Galantamine in Alzheimer’s Disease |
| NCT00309725 | PHASE3 | COMPLETED | A Cardiac Safety Study of Galantamine in the Treatment of Alzheimer’s Disease. |
| NCT00463879 | PHASE2/PHASE3 | COMPLETED | Galantamine for Cognitive Deficits in Schizophrenia |
| NCT00679627 | PHASE3 | TERMINATED | A Study of Galantamine Used to Treat Patients With Mild to Moderate Alzheimer’s Disease |
| NCT00814801 | PHASE3 | COMPLETED | An Efficacy and Safety Study of Galantamine for the Treatment of Patients With Alzheimer’s Disease |
| NCT02098824 | PHASE2/PHASE3 | UNKNOWN | Symptomatic Treatment of Vascular Cognitive Impairment |
| NCT02374567 | PHASE3 | TERMINATED | Pharmacovigilance in Gerontopsychiatric Patients |
| NCT04769206 | PHASE1/PHASE2 | RECRUITING | Enhancing Parasympathetic Activity to Improve Endothelial Dysfunction, Vascular Oxidative Stress in African Americans |
| NCT00509067 | PHASE2 | COMPLETED | Use of Galantamine and CDP-choline (Citicoline) to Treat Adults With Schizophrenia |
| NCT00809835 | PHASE2 | COMPLETED | Galantamine to Enhance Cognitive Behavioral Therapy for Cocaine Abuse |
| NCT01012167 | PHASE2 | COMPLETED | Oxytocin or Galantamine Versus Placebo for the Treatment of Negative Symptoms and Cognitive Impairments in Schizophrenia |
| NCT01100775 | PHASE2 | COMPLETED | Effects of Galantamine on Cognition |
| NCT01416948 | PHASE2 | TERMINATED | Cognitive REmediation After Trauma Exposure Trial = CREATE Trial |
| NCT01508494 | PHASE2 | COMPLETED | Cognitive Rehabilitation and Galantamine for Post Stroke Cognitive Impairment |
| NCT01669538 | PHASE2 | COMPLETED | Effect of Galantamine on Short-term Abstinence |
| NCT01677754 | PHASE2 | COMPLETED | A 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).
Related molecules
Related molecules
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:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | ACHE |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | ACHE |
| TADALAFIL | ChEMBL + PubChem | Phase 4 (approved) | ACHE |
| ALFUZOSIN | ChEMBL | Phase 4 (approved) | ACHE |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | ACHE |
| BERBERINE | ChEMBL | Phase 4 (approved) | ACHE |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | ACHE |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | ACHE |
| BUTENAFINE | ChEMBL | Phase 4 (approved) | ACHE |
| CABERGOLINE | ChEMBL | Phase 4 (approved) | ACHE |
| CAFFEINE | ChEMBL | Phase 4 (approved) | ACHE |
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | ACHE |
| CITALOPRAM | ChEMBL | Phase 4 (approved) | ACHE |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | ACHE |
| DECAMETHONIUM | ChEMBL | Phase 4 (approved) | ACHE |
| DECAMETHONIUM BROMIDE | ChEMBL | Phase 4 (approved) | ACHE |
| DEQUALINIUM | ChEMBL | Phase 4 (approved) | ACHE |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | ACHE |
| DISULFIRAM | ChEMBL | Phase 4 (approved) | ACHE |
| DOFETILIDE | ChEMBL | Phase 4 (approved) | ACHE |
| DONEPEZIL | ChEMBL | Phase 4 (approved) | ACHE |
| DYCLONINE | ChEMBL | Phase 4 (approved) | ACHE |
| EBASTINE | ChEMBL | Phase 4 (approved) | ACHE |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | ACHE |
| EDROPHONIUM | ChEMBL | Phase 4 (approved) | ACHE |
| EDROPHONIUM CHLORIDE | ChEMBL | Phase 4 (approved) | ACHE |
| EPIRUBICIN | ChEMBL | Phase 4 (approved) | ACHE |
| ETHOPROPAZINE | ChEMBL | Phase 4 (approved) | ACHE |
| ETHYLESTRENOL | ChEMBL | Phase 4 (approved) | ACHE |
| FENOFIBRATE | ChEMBL | Phase 4 (approved) | ACHE |
| FLAVOXATE | ChEMBL | Phase 4 (approved) | ACHE |
| FLUOXETINE | ChEMBL | Phase 4 (approved) | ACHE |
| GALLAMINE | ChEMBL | Phase 4 (approved) | ACHE |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | ACHE |
| HEXAFLUORENIUM | ChEMBL | Phase 4 (approved) | ACHE |
| ILOPERIDONE | ChEMBL | Phase 4 (approved) | ACHE |
| IRINOTECAN | ChEMBL | Phase 4 (approved) | ACHE |
| ISOFLUROPHATE | ChEMBL | Phase 4 (approved) | ACHE |
| LEVALLORPHAN | ChEMBL | Phase 4 (approved) | ACHE |
| LORLATINIB | ChEMBL | Phase 4 (approved) | ACHE |
| LURASIDONE | ChEMBL | Phase 4 (approved) | ACHE |
| MELPHALAN | ChEMBL | Phase 4 (approved) | ACHE |
| MEMANTINE | ChEMBL | Phase 4 (approved) | ACHE |
| MEPTAZINOL | ChEMBL | Phase 4 (approved) | ACHE |
| METHOXSALEN | ChEMBL | Phase 4 (approved) | ACHE |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | ACHE |
| MINAPRINE | ChEMBL | Phase 4 (approved) | ACHE |
| NAFTOPIDIL | ChEMBL | Phase 4 (approved) | ACHE |
| NEFAZODONE | ChEMBL | Phase 4 (approved) | ACHE |
| NEOSTIGMINE | ChEMBL | Phase 4 (approved) | ACHE |
| NEOSTIGMINE METHYLSULFATE | ChEMBL | Phase 4 (approved) | ACHE |
| NICERGOLINE | ChEMBL | Phase 4 (approved) | ACHE |
| NIZATIDINE | ChEMBL | Phase 4 (approved) | ACHE |
| ORLISTAT | ChEMBL | Phase 4 (approved) | ACHE |
| OXICONAZOLE | ChEMBL | Phase 4 (approved) | ACHE |
| PALBOCICLIB | ChEMBL | Phase 4 (approved) | ACHE |
| PENTAMIDINE | ChEMBL | Phase 4 (approved) | ACHE |
| PENTOXIFYLLINE | ChEMBL | Phase 4 (approved) | ACHE |
| PERICIAZINE | ChEMBL | Phase 4 (approved) | ACHE |
| PHYSOSTIGMINE | ChEMBL | Phase 4 (approved) | ACHE |
Related Atlas pages
- Genes: ACHE
- Diseases: dementia, autism, vascular dementia, anxiety, Lewy body dementia, depressive disorder, Alzheimer disease
- Drugs: Pazopanib, Tadalafil, Alfuzosin, Aripiprazole, Berberine, Bosutinib, Bromocriptine, Butenafine, Cabergoline, Caffeine, Cannabidiol, Citalopram, Clotrimazole, Decamethonium, Dequalinium, Diethylstilbestrol, Disulfiram, Dofetilide, Donepezil, Dyclonine, Ebastine, Econazole, Edrophonium, Epirubicin, Ethopropazine, Ethylestrenol, Fenofibrate, Flavoxate, Fluoxetine, Gallamine, Hexachlorophene, Hexafluorenium, Iloperidone, Irinotecan, Isoflurophate, Levallorphan, Lorlatinib, Lurasidone, Melphalan, Memantine, Meptazinol, Methoxsalen, Miconazole, Minaprine, Naftopidil, Nefazodone, Neostigmine, Nicergoline, Nizatidine, Orlistat, Oxiconazole, Palbociclib, Pentamidine, Pentoxifylline, Periciazine, Physostigmine