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Colchicine

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Also known as (-)-colchicineColchcineColchicine component of col-probenecidColchicine component of colbenemidColchicine component of mitigareColchicine component of proben-cColchicinumColchineosColchisolColcrysGloperbaLodocoMitigareNSC-757colchichinecoichicineSID11114044SID17389095SID17389096

Summary

Colchicine (CHEMBL107) is an approved small-molecule anti-inflammatory agent (ATC M04AC01) targeting BRD4, TUBB, and GLRA1; indicated across 42 conditions including gout and familial mediterranean fever.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: M04AC01
  • Targets: 6 (BRD4, TUBB, GLRA1…)
  • Indications: 42 conditions
  • Clinical trials: 231
  • Chemistry: 399.4 Da · C22H25NO6

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL107
NameColchicine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID6167
ChEBICHEBI:27882
ATCM04AC01
Molecular formulaC22H25NO6
Molecular weight399.4
InChIKeyIAKHMKGGTNLKSZ-INIZCTEOSA-N

SMILES: CC(=O)N[C@H]1CCC2=CC(=C(C(=C2C3=CC=C(C(=O)C=C13)OC)OC)OC)OC

IUPAC name: N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide

ChEBI definition: A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.

Pharmacological roles (ChEBI): mutagen, anti-inflammatory agent, gout suppressant.

Also known as: (-)-colchicine, Colchcine, Colchicine, Colchicine component of col-probenecid, Colchicine component of colbenemid, Colchicine component of mitigare, Colchicine component of proben-c, Colchicinum, Colchineos, Colchisol, Colcrys, Gloperba

Patent coverage: 35,013 distinct patent families (93,932 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 93,858 (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
BRD4bromodomain containing 4Inhibition4.794.7% (common-essential)O60885
TUBBtubulin beta class IInhibition7.96P07437
GLRA1glycine receptor α1 subunitAntagonist3.50.3%P23415
GLRA2glycine receptor α2 subunitAntagonist4.20.4%P23416
Glycine Receptor (All subtypes)Inhibition
TAS2R4TAS2R4Agonist2.990%Q9NYW5
TAS2R46TAS2R46Agonist2.82.2%P59540

Broader ChEMBL bioactivity targets: 30 (assay-derived). Sample: Prelamin-A/C, Ferritin light chain, Thrombopoietin, Geminin, Endonuclease 4, Ras-related protein Rab-9A, 5-hydroxytryptamine receptor 2B, Thyrotropin receptor, Beta-lactamase, Solute carrier family 22 member 3.

Bioactivity

ChEMBL activities: 146 potent at pChembl ≥ 5 of 162 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P025508.79Ki1.61nMCHEMBL_ACT_12159388
TUBB4A8.52IC503nMCHEMBL_ACT_25872982
P025508.17IC506.7nMCHEMBL_ACT_16562094
LMNA8.05Potency8.9nMCHEMBL_ACT_3626577
GMNN7.4Potency39.8nMCHEMBL_ACT_5061236
P159177.3Potency50.1nMCHEMBL_ACT_4659592
TUBB4A7.24Kd58nMCHEMBL_ACT_18357215
LMNA7.15Potency70.8nMCHEMBL_ACT_4402409
P159177Potency100nMCHEMBL_ACT_4633042
SLC22A36.92Ki120nMCHEMBL_ACT_11002258
LMNA6.9Potency125.9nMCHEMBL_ACT_3645019
TUBB4A6.72IC50190nMCHEMBL_ACT_22750673
TUBB4A6.7EC50200nMCHEMBL_ACT_22930733
TUBB4A6.44IC50360nMCHEMBL_ACT_15203083
TUBB4A6.3IC50500nMCHEMBL_ACT_1766796
THPO6.3Potency501.2nMCHEMBL_ACT_4805572
THPO6.3Potency501.2nMCHEMBL_ACT_5070323
Q279576.12EC50750nMCHEMBL_ACT_12563896
Q6B8566.11Ki780nMCHEMBL_ACT_539983
Q6B8566.1IC50800nMCHEMBL_ACT_1044136
Q6B8566.1IC50800nMCHEMBL_ACT_1098989
Q6B8566.1IC50800nMCHEMBL_ACT_329353
P025506.1IC50800nMCHEMBL_ACT_380041
CYP2D66.1Potency794.3nMCHEMBL_ACT_4969891
CYP2D66.1AC50794.3nMCHEMBL_ACT_6050298
Q6B8566.1IC50800nMCHEMBL_ACT_906404
Q6B8566.1IC50800nMCHEMBL_ACT_943855
Q6B8566.1IC50800nMCHEMBL_ACT_988362
P084826.05Potency891.3nMCHEMBL_ACT_4803398
TUBB4A5.98IC501050nMCHEMBL_ACT_2003745

Target pathways

Aggregated over 6 target gene(s): BRD4, TUBB, GLRA1, GLRA2, TAS2R4, TAS2R46.

Top Reactome pathways

35 total, by targets touching each:

PathwayTargetsGenes
Neurotransmitter receptors and postsynaptic signal transmission2GLRA1, GLRA2
Signal Transduction2TAS2R4, TAS2R46
Disease2BRD4, TUBB
Signaling by GPCR2TAS2R4, TAS2R46
GPCR downstream signalling2TAS2R4, TAS2R46
G alpha (i) signalling events2TAS2R4, TAS2R46
Class C/3 (Metabotropic glutamate/pheromone receptors)2TAS2R4, TAS2R46
GPCR ligand binding2TAS2R4, TAS2R46
Infectious disease2BRD4, TUBB
Potential therapeutics for SARS2BRD4, TUBB
SARS-CoV Infections2BRD4, TUBB
Sensory Perception2TAS2R4, TAS2R46
Sensory perception of taste2TAS2R4, TAS2R46
Sensory perception of sweet, bitter, and umami (glutamate) taste2TAS2R4, TAS2R46
Viral Infection Pathways2BRD4, TUBB
Cell Cycle1TUBB
Innate Immune System1TUBB
Immune System1TUBB
Organelle biogenesis and maintenance1TUBB
Regulation of PLK1 Activity at G2/M Transition1TUBB
Loss of Nlp from mitotic centrosomes1TUBB
Recruitment of mitotic centrosome proteins and complexes1TUBB
Loss of proteins required for interphase microtubule organization from the centrosome1TUBB
Centrosome maturation1TUBB
Recruitment of NuMA to mitotic centrosomes1TUBB
Mitotic G2-G2/M phases1TUBB
Cilium Assembly1TUBB
Anchoring of the basal body to the plasma membrane1TUBB
Neutrophil degranulation1TUBB
Mitotic Prometaphase1TUBB

Dominant GO biological processes

GO termTargets
monoatomic ion transport2
chloride transport2
neuropeptide signaling pathway2
cellular response to amino acid stimulus2
cellular response to zinc ion2
cellular response to ethanol2
chloride transmembrane transport2
monoatomic ion transmembrane transport2
excitatory postsynaptic potential2
detection of chemical stimulus involved in sensory perception of bitter taste2
signal transduction2
G protein-coupled receptor signaling pathway2
sensory perception of taste2
chromatin remodeling1
regulation of transcription by RNA polymerase II1

Indications & clinical

Indications

42 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
gout4MONDO:0005393EFO:0004274
familial Mediterranean fever4MONDO:0018088MONDO:0018088
myocardial infarction3MONDO:0005068EFO:0000612
atrial fibrillation3MONDO:0004981EFO:0000275
pericarditis3MONDO:0005904EFO:0007427
proliferative vitreoretinopathy3MONDO:0700115EFO:1001129
primary biliary cholangitis3MONDO:0005388EFO:1001486
vasculitis3MONDO:0018882EFO:0006803
ST-elevation myocardial infarction3MONDO:0041656EFO:0008585
severe acute respiratory syndrome3MONDO:0005091EFO:0000694
lung disorder3MONDO:0005275EFO:0003818
coronary artery disorder3MONDO:0005010EFO:0001645
heart failure3MONDO:0005252EFO:0003144
asthma3MONDO:0004979MONDO:0004979
cardiovascular disorder3MONDO:0004995EFO:0000319
plasma cell myeloma3MONDO:0009693EFO:0001378
ischemia reperfusion injury3MONDO:0005203EFO:0002687
canker sore2MONDO:0005318EFO:0003938
acute coronary syndrome2MONDO:0005542EFO:0005672
Behcet disease2MONDO:0007191EFO:0003780
vascular disorder2MONDO:0005385EFO:0004264
diabetic kidney disease2MONDO:0005016EFO:0000401
chronic hepatitis C virus infection2MONDO:0005354EFO:0004220
heart disorder2MONDO:0005267EFO:0003777
cholangiocarcinoma2MONDO:0019087EFO:0005221
viral pneumonia2MONDO:0006012EFO:0007541
chronic kidney disease2MONDO:0005300EFO:0003884
hypertensive disorder2MONDO:0005044EFO:0000537
atherosclerosis2MONDO:0005311EFO:0003914
amyotrophic lateral sclerosis2MONDO:0004976MONDO:0004976
osteoarthritis, knee2MONDO:0005416EFO:0004616
cirrhosis of liver1MONDO:0005155EFO:0001422
neoplasm1MONDO:0005070EFO:0000616
peripheral arterial disease0MONDO:0005386EFO:0004265

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

Clinical trials

Total trials: 231.

Phase distribution

PhaseTrials
PHASE358
PHASE255
PHASE447
PHASE127
Not specified27
PHASE2/PHASE310
EARLY_PHASE14
PHASE1/PHASE23

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04875702PHASE4RECRUITINGTreat-to-Target Serum Urate Versus Treat-to-Avoid Symptoms in Gout
NCT05618353PHASE4RECRUITINGThe Peri-OPerative COlchicine to Reduce Negative Events (POPCORN) Trial
NCT05850091PHASE4RECRUITINGPolygenic Risk-based Detection of Subclinical Coronary Atherosclerosis and Intervention With Statin and Colchicine
NCT06090890PHASE4RECRUITINGAnti-inflammatory Therapy for Recurrent In-stent Restenosis
NCT06286423PHASE4RECRUITINGColchicine in Acutely Decompensated HFREF
NCT06396858PHASE4NOT_YET_RECRUITINGAnti-inflammatory and Anti-thrombotic Therapy With colcHicine and Low Dose Rivaroxaban for Major Adverse Cardiovascular Events Reduction in Ischemic Stroke
NCT06543082PHASE4RECRUITINGMACT (Mono Antiplatelet and Colchicine Therapy) Prospective Multicenter Study
NCT06765356PHASE4ACTIVE_NOT_RECRUITINGPragmatic Evaluation of a Pentaspline Pulsed Field Ablation System to Treat Atrial Fibrillation and Related Arrhythmias
NCT06798714PHASE4RECRUITINGThe Effect of Colchicine on the Occurrence of Atrial Fibrillation After Cardiac Surgery
NCT06802926PHASE4RECRUITINGPilot Trial of Colchicine for Graft Failure in CABG
NCT07287345PHASE4RECRUITINGColchicine’s Effect on Inflammatory Markers
NCT07462325PHASE4NOT_YET_RECRUITINGProteomic and Inflammatory Omics Changes With Colchicine Therapy in Coronary Heart Disease
NCT00179413PHASE4COMPLETEDStudy of Long-term Peg Intron vs. Colchicine in Non-responders.
NCT00235079PHASE4COMPLETEDStudy of Colchicine to Treat and Prevent Recurrent Pericarditis After Failure of Conventional Treatment.
NCT01084278PHASE4COMPLETEDHealthy and Renal Impairment Study of Colcrys (Colchicine, USP)
NCT01112982PHASE4COMPLETEDAn Assessment of Chronic Synovial-Based Inflammation and Its Role With Serum Urate Levels.
NCT01173107PHASE4COMPLETEDA Pilot Study for PK/PD Parameter of Colchicine in Chronic Kidney Disease Patient.
NCT01451645PHASE4COMPLETEDEfficacy and Safety of Colchicine for the Prevention of Gout Flares During the Initiation of Allopurinol
NCT01601132PHASE4COMPLETEDDrug Interaction Study of Colchicine and Theophylline
NCT01709981PHASE4COMPLETEDAnti-inflammatory Effects of Colchicine in PCI
NCT01906749PHASE4UNKNOWNColchicine for Acute Coronary Syndromes
NCT01994226PHASE4COMPLETEDColchicine Or Naproxen Treatment for ACute gouT
NCT02060552PHASE4COMPLETEDImmune Molecular and Inflammatory Cytokines Dysfunction Analysis in Gout Patients With Different Urate Levels
NCT02122484PHASE4COMPLETEDColchicine in Coronary Artery Bypass Graft (CABG)
NCT02140372PHASE4COMPLETEDAnti-platelet Effects of Colchicine in Healthy Volunteers
NCT02260206PHASE4COMPLETEDImpact of Colchicine Therapy on Arrhythmia Recurrence After Acute Pericardial Effusion
NCT02281305PHASE4UNKNOWNPost-MI PET Scan Imaging of Inflammation
NCT02500641PHASE4COMPLETEDIntensive Urate Lowering Therapy of Febuxostat Compared to Allopurinol on Cardiovascular Risk in Patients With Gout
NCT02602028PHASE4COMPLETEDThe Comparison of the Efficacy of Once and Twice Daily Colchicine Dosage in Pediatric Patients With FMF
NCT02926248PHASE4SUSPENDEDEffect of Colchicine on Range of Motion After Manipulation Under Anesthesia for the Stiff Total Knee Replacement
NCT03226899PHASE4TERMINATEDA Phase 4 Safety and Efficacy Study to Evaluate Lesinurad 200 mg in Participants With Gout and Renal Impairment
NCT04224545PHASE4COMPLETEDCOlchicine in Cardiac Surgery
NCT04382443PHASE4COMPLETEDOral Colchicine in Argentina to Prevent Restenosis
NCT04601883PHASE4COMPLETEDColchicine as Treatment for People With Hand Osteoarthritis
NCT04818489PHASE4UNKNOWNColchicine and Post-COVID-19 Pulmonary Fibrosis
NCT04848857PHASE4COMPLETEDColchicine for the Stability of Coronary Plaque in Acute Coronary Syndrome (COLOCT)
NCT04949516PHASE4COMPLETEDMono Antiplatelet and Colchicine Therapy
NCT05130892PHASE4COMPLETEDEffect of Inflammasome Inhibitor on hsCRP in Patients After PCI
NCT05168137PHASE4UNKNOWNEfficacy and Safety of Low-Dose Colchicine on Surrogate Markers of Cardiovascular Events in People Living With HIV Receiving Antiretroviral Therapy
NCT05246072PHASE4COMPLETEDEffect of Combined Use of Ivermectin and Colchicine in COVID-19 Patients

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 2 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.

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

MoleculeSourceStatusShared targets
ISOPROTERENOLChEMBLPhase 4 (approved)TAS2R4, TAS2R46
MOLIBRESIBChEMBLPhase 2BRD4, TUBB
ADAPALENEChEMBL + PubChemPhase 4 (approved)GLRA1
CANNABIDIOLChEMBL + PubChemPhase 4 (approved)GLRA2
CHOLECALCIFEROLChEMBL + PubChemPhase 4 (approved)GLRA1
CINACALCETChEMBL + PubChemPhase 4 (approved)GLRA1
DRONABINOLChEMBL + PubChemPhase 4 (approved)GLRA1
DUTASTERIDEChEMBL + PubChemPhase 4 (approved)GLRA1
GLYCINEChEMBL + PubChemPhase 4 (approved)GLRA1
MEFLOQUINEChEMBL + PubChemPhase 4 (approved)GLRA1
PIMOZIDEChEMBL + PubChemPhase 4 (approved)GLRA1
PODOFILOXChEMBL + PubChemPhase 4 (approved)TUBB
REGORAFENIBChEMBL + PubChemPhase 4 (approved)GLRA1
RISPERIDONEChEMBL + PubChemPhase 4 (approved)GLRA1
SULINDACChEMBL + PubChemPhase 4 (approved)GLRA1
TELMISARTANChEMBL + PubChemPhase 4 (approved)GLRA1
VINBLASTINEChEMBL + PubChemPhase 4 (approved)TUBB
ACETAMINOPHENChEMBLPhase 4 (approved)BRD4
ALPRAZOLAMChEMBLPhase 4 (approved)BRD4
ASTEMIZOLEChEMBLPhase 4 (approved)GLRA1
BELINOSTATChEMBLPhase 4 (approved)BRD4
DEXTROMETHORPHANChEMBLPhase 4 (approved)TAS2R46
DOCETAXELChEMBLPhase 4 (approved)TUBB
FEDRATINIBChEMBLPhase 4 (approved)BRD4
FLUSPIRILENEChEMBLPhase 4 (approved)GLRA1
LENALIDOMIDEChEMBLPhase 4 (approved)BRD4
LEVOFLOXACINChEMBLPhase 4 (approved)TUBB
NITROXOLINEChEMBLPhase 4 (approved)BRD4
NORFLOXACINChEMBLPhase 4 (approved)BRD4
NOSCAPINEChEMBLPhase 4 (approved)TUBB
PACLITAXELChEMBLPhase 4 (approved)TUBB
PANOBINOSTATChEMBLPhase 4 (approved)BRD4
ROMIDEPSINChEMBLPhase 4 (approved)BRD4
TIRBANIBULINChEMBLPhase 4 (approved)TUBB
VINCRISTINEChEMBLPhase 4 (approved)TUBB
VINORELBINEChEMBLPhase 4 (approved)TUBB
VORINOSTATChEMBLPhase 4 (approved)BRD4
APABETALONEChEMBLPhase 3BRD4
DINACICLIBChEMBLPhase 3BRD4
PATUPILONEChEMBLPhase 3TUBB
PELABRESIBChEMBLPhase 3BRD4
TACEDINALINEChEMBLPhase 3BRD4
VOLASERTIBChEMBLPhase 3BRD4
7-ETHYL-10-HYDROXYCAMPTOTHECINChEMBLPhase 2BRD4
ABT-751ChEMBLPhase 2TUBB
ALOBRESIBChEMBLPhase 2BRD4
AMREDOBRESIBChEMBLPhase 2BRD4
BI-2536ChEMBLPhase 2BRD4
BIRABRESIBChEMBLPhase 2BRD4
CLOXYQUINChEMBLPhase 2BRD4
DOLASTATIN-10ChEMBLPhase 2TUBB
EZOBRESIBChEMBLPhase 2BRD4
FRUCTOSEChEMBLPhase 2GLRA1
INDIBULINChEMBLPhase 2TUBB
MAYTANSINEChEMBLPhase 2TUBB
MIVEBRESIBChEMBLPhase 2BRD4
NOCODAZOLEChEMBLPhase 2TUBB
PARBENDAZOLEChEMBLPhase 2TUBB
SF-1126ChEMBLPhase 2BRD4
.gamma.-aminobutyric acidPubChemApprovedGLRA1

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