◎ Sugi Atlas

Atlas / Drug / Epigalocatechin Gallate

Epigalocatechin Gallate

drug
On this page

Also known as (-)-epigallocatechin gallate(-)epigallocatechingallate(-)epigallocatechin gallateepigallocatechin gallateSID26719730SID49681655SID26757738(-)-epi-gallocatechine gallateEpigallocatchechingallateSID144208666SID144213767(-)-epigallocatechingallateEpigallocatechingallateC0164942(-)-epigallo-catechin gallate(-)-Epigaloocatechin gallate(-)-Epigallocathechin gallateEpigallocatechin-gallate

Summary

Epigalocatechin Gallate (CHEMBL297453) is a phase-3 clinical-stage small-molecule antineoplastic agent targeting DYRK1A, EP300, and KAT2B; indicated across 40 conditions including anogenital human papillomavirus infection and lichen planus, oral.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 4 (DYRK1A, EP300, KAT2B…)
  • Indications: 40 conditions
  • Clinical trials: 21
  • Chemistry: 458.4 Da · C22H18O11

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL297453
NameEpigalocatechin Gallate
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID65064
ChEBICHEBI:4806
Molecular formulaC22H18O11
Molecular weight458.4
InChIKeyWMBWREPUVVBILR-WIYYLYMNSA-N

SMILES: C1[C@H]([C@H](OC2=CC(=CC(=C21)O)O)C3=CC(=C(C(=C3)O)O)O)OC(=O)C4=CC(=C(C(=C4)O)O)O

IUPAC name: [(2R,3R)-5,7-dihydroxy-2-(3,4,5-trihydroxyphenyl)-3,4-dihydro-2H-chromen-3-yl] 3,4,5-trihydroxybenzoate

ChEBI definition: A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (−)-epigallocatechin.

Pharmacological roles (ChEBI): antineoplastic agent, antioxidant, Hsp90 inhibitor, neuroprotective agent, geroprotector, apoptosis inducer.

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

Also known as: (-)-epigallocatechin gallate, Epigalocatechin gallate, (-)epigallocatechingallate, (-)epigallocatechin gallate, epigallocatechin gallate, Epigallocatechin gallate, (-)Epigallocatechin gallate, (-)-Epigallocatechin gallate, Epigallocatechin Gallate, SID26719730, SID49681655, SID26757738

Patent coverage: 9,012 distinct patent families (22,804 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 22,790 (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
DYRK1Adual specificity tyrosine phosphorylation regulated kinase 1AInhibition6.4810.5%Q13627
EP300EP300 lysine acetyltransferaseInhibition4.5233.3%Q09472
KAT2Blysine acetyltransferase 2BInhibition4.220.2%Q92831
TAS2R5TAS2R5Agonist4.910.1%Q9NYW4

Broader ChEMBL bioactivity targets: 88 (assay-derived). Sample: Dual specificity tyrosine-phosphorylation-regulated kinase 4, Tyrosyl-DNA phosphodiesterase 1, Pyruvate kinase PKM, Glucose-6-phosphate 1-dehydrogenase, Polymerase acidic protein, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Fructose-bisphosphate aldolase, ATP-dependent DNA helicase Q1, 4’-phosphopantetheinyl transferase ffp.

Bioactivity

ChEMBL activities: 104 potent at pChembl ≥ 5 of 140 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P158407.55Ki28nMCHEMBL_ACT_10982199
RPSA7.4Kd39.9nMCHEMBL_ACT_25495733
CLK17.14IC5071.6nMCHEMBL_ACT_25064327
PSMB57.07IC5086nMCHEMBL_ACT_19449315
P159177.01IC5097nMCHEMBL_ACT_24867625
ADAMTS47IC50100nMCHEMBL_ACT_25014721
ADAMTS57IC50100nMCHEMBL_ACT_25014725
ABCB16.91IC50124.1nMCHEMBL_ACT_15612286
ABCB16.91IC50122.6nMCHEMBL_ACT_15612288
PKMYT16.86IC50137nMCHEMBL_ACT_29067684
PKMYT16.86IC50137nMCHEMBL_ACT_29138234
APP6.85IC50140nMCHEMBL_ACT_25079663
APP6.75IC50180nMCHEMBL_ACT_25076262
DYRK1A6.7IC50200nMCHEMBL_ACT_25892130
P0DTD16.7IC50200nMCHEMBL_ACT_29231020
BCL26.63Ki234.4nMCHEMBL_ACT_2150741
DYRK1A6.63IC50232nMCHEMBL_ACT_24846230
P114126.6IC50250nMCHEMBL_ACT_2144799
RAD526.56IC50277nMCHEMBL_ACT_19491420
RAD526.56IC50277nMCHEMBL_ACT_22990744
MTOR6.5Ki320nMCHEMBL_ACT_24995820
TDP16.5Potency316.2nMCHEMBL_ACT_3930013
DYRK1A6.48IC50330nMCHEMBL_ACT_13881655
Q634706.48IC50330nMCHEMBL_ACT_15654983
DYRK1A6.48IC50330nMCHEMBL_ACT_18762088
DYRK1A6.48IC50330nMCHEMBL_ACT_24691636
DYRK1A6.48IC50330nMCHEMBL_ACT_25076354
DYRK1A6.48IC50330nMCHEMBL_ACT_25892120
BCL26.47Ki335nMCHEMBL_ACT_12457518
BID6.44IC50360nMCHEMBL_ACT_24723959

Target pathways

Aggregated over 4 target gene(s): DYRK1A, EP300, KAT2B, TAS2R5.

Top Reactome pathways

110 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction2KAT2B, TAS2R5
Pre-NOTCH Transcription and Translation2EP300, KAT2B
Regulation of gene expression in late stage (branching morphogenesis) pancreatic bud precursor cells2EP300, KAT2B
NOTCH1 Intracellular Domain Regulates Transcription2EP300, KAT2B
Constitutive Signaling by NOTCH1 PEST Domain Mutants2EP300, KAT2B
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants2EP300, KAT2B
HATs acetylate histones2EP300, KAT2B
B-WICH complex positively regulates rRNA expression2EP300, KAT2B
Metalloprotease DUBs2EP300, KAT2B
RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function2EP300, KAT2B
RUNX3 regulates NOTCH signaling2EP300, KAT2B
NOTCH3 Intracellular Domain Regulates Transcription2EP300, KAT2B
NOTCH4 Intracellular Domain Regulates Transcription2EP300, KAT2B
Estrogen-dependent gene expression2EP300, KAT2B
Regulation of FOXO transcriptional activity by acetylation2EP300, KAT2B
Formation of paraxial mesoderm2EP300, KAT2B
Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells)2EP300, KAT2B
Regulation of gene expression by Hypoxia-inducible Factor1EP300
Developmental Biology1KAT2B
G0 and Early G11DYRK1A
Polo-like kinase mediated events1EP300
Signaling by NOTCH1KAT2B
Disease1KAT2B
Regulation of beta-cell development1KAT2B
Pre-NOTCH Expression and Processing1KAT2B
Signaling by NOTCH11KAT2B
PPARA activates gene expression1EP300
Formation of the beta-catenin:TCF transactivating complex1EP300
YAP1- and WWTR1 (TAZ)-stimulated gene expression1KAT2B
Epigenetic regulation of gene expression1KAT2B

Dominant GO biological processes

GO termTargets
positive regulation of DNA-templated transcription3
chromatin remodeling3
regulation of transcription by RNA polymerase II3
nervous system development2
circadian rhythm2
negative regulation of transcription by RNA polymerase II2
protein acetylation2
heart development2
positive regulation of neuron projection development2
N-terminal peptidyl-lysine acetylation2
internal peptidyl-lysine acetylation2
transcription initiation-coupled chromatin remodeling2
positive regulation of transcription by RNA polymerase II2
gluconeogenesis2
regulation of DNA-templated transcription2

Indications & clinical

Indications

40 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
anogenital human papillomavirus infection3MONDO:0005647EFO:0007147
lichen planus, oral3MONDO:0043923EFO:0008517
multiple system atrophy3MONDO:0007803EFO:1001050
uterine corpus leiomyoma3MONDO:0007886EFO:0000731
benign prostatic hyperplasia2MONDO:0010811EFO:0000284
Down syndrome2MONDO:0008608EFO:0001064
endometriosis2MONDO:0005133EFO:0001065
plasma cell myeloma2MONDO:0009693EFO:0001378
cirrhosis of liver2MONDO:0005155EFO:0001422
epidermolysis bullosa dystrophica2MONDO:0006543Orphanet:303
ductal breast carcinoma in situ2MONDO:0005023EFO:0000432
breast neoplasm2MONDO:0021100MONDO:0007254
lung neoplasm2MONDO:0021117MONDO:0008903
follicular lymphoma2MONDO:0018906MONDO:0018906
brain injury2MONDO:0043510MONDO:0043510
viral infectious disease2MONDO:0005108EFO:0000763
Alzheimer disease2MONDO:0004975MONDO:0004975
type 2 diabetes mellitus2MONDO:0005148MONDO:0005148
Parkinson disease2MONDO:0005180MONDO:0005180
multiple sclerosis2MONDO:0005301MONDO:0005301
Huntington disease2MONDO:0007739MONDO:0007739
fragile X syndrome2MONDO:0010383MONDO:0010383
Duchenne muscular dystrophy2MONDO:0010679MONDO:0010679
hereditary amyloidosis2MONDO:0018634MONDO:0019438
systemic lupus erythematosus2MONDO:0007915MONDO:0007915
plasma cell neoplasm2MONDO:0004959EFO:0000200
nasopharyngeal carcinoma2MONDO:0015459MONDO:0015459
Barrett esophagus1MONDO:0013662EFO:0000280
leukemia1MONDO:0005059EFO:0000565
neoplasm1MONDO:0005070EFO:0000616
prostate adenocarcinoma1MONDO:0005082EFO:0000673
HIV infectious disease1MONDO:0005109EFO:0000764
idiopathic pulmonary fibrosis1MONDO:0800504EFO:0000768
non-small cell lung carcinoma1MONDO:0005233EFO:0003060
osteoporosis1MONDO:0005298EFO:0003882
relapsing-remitting multiple sclerosis1MONDO:0005314EFO:0003929
colonic neoplasm0MONDO:0005401MONDO:0021063

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

Clinical trials

Total trials: 21.

Phase distribution

PhaseTrials
Not specified7
PHASE26
PHASE1/PHASE23
PHASE2/PHASE32
EARLY_PHASE12
PHASE41

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03199430PHASE4COMPLETEDEpigallocatechin Gallate Lowers Circulating Catecholamine Concentrations and Alters Lipid Metabolism.
NCT00951834PHASE2/PHASE3COMPLETEDSunphenon EGCg (Epigallocatechin-Gallate) in the Early Stage of Alzheimer´s Disease
NCT01183767PHASE2/PHASE3COMPLETEDSunphenon Epigallocatechin-Gallate (EGCg) in Duchenne Muscular Dystrophy
NCT06068543PHASE2RECRUITINGReducing Frailty for Older Cancer Survivors Using Supplements II
NCT06398405PHASE2RECRUITINGA Phase II Clinical Study of Epigallocatechin-3-gallate in Patients With Esophageal Squamous Cancer
NCT06524609PHASE1/PHASE2RECRUITINGEGCG for the Prevention and Treatment of TIPN
NCT00476138PHASE1/PHASE2UNKNOWNEffect of Epigallocatechin-Gallate on Inner Retinal Function in Ocular Hypertension and Early Glaucoma
NCT00525668PHASE1/PHASE2COMPLETEDSunphenon Epigallocatechin-gallate (EGCg) in Relapsing-remitting Multiple Sclerosis (SuniMS Study)
NCT01394796PHASE2COMPLETEDEgcg, a dyrk1a Inhibitor as Therapeutic Tool for Reversing Cognitive Deficits in Down Syndrome Individuals.
NCT01699711PHASE2COMPLETEDNormalization of dyrk1A and APP Function as an Approach to Improve Cognitive Performance and Decelerate AD Progression in DS Subjects: Epigallocatechin Gallate as Therapeutic Tool
NCT02015312PHASE2COMPLETEDA Trial for the Treatment of Cardiac AL-Amyloidosis With the Green Tea Compound Epigallocatechin-3-gallate (TAME-AL)
NCT03740295PHASE2COMPLETEDImpact of Ketone Bodies and Epigallocatechin Gallate in Multiple Sclerosis
NCT06531863EARLY_PHASE1RECRUITINGCurcumin and EGCG Supplementation to Improve Serum BDNF and Mood Disturbance
NCT03928847EARLY_PHASE1COMPLETEDFibroblast Specific Inhibition of LOXL2 and TGFbeta1 Signaling in Patients With Pulmonary Fibrosis.
NCT01317953Not specifiedAVAILABLEOral Green Tea Extract for Small Cell Lung Cancer
NCT05448365Not specifiedRECRUITINGVitamin D, Epigallocatechin Gallate, D-chiro-inositol and Vitamin B6 in Uterine Fibroid
NCT02558933Not specifiedCOMPLETEDEpigallocatechin Gallate (EGCG) to Improve Cognitive Performance in Foetal Alcohol Syndrome (FAS) Children
NCT03194620Not specifiedCOMPLETEDAbsorption, Metabolism and Excretion of Dietary Polyphenolic Bioactives in Humans
NCT03883880Not specifiedTERMINATEDSalivary Interactions With Chemosensations
NCT05988788Not specifiedCOMPLETEDEffect of Epigallocatechin-3-Gallate Solution as a Root Canal Irrigant on Post-Operative Pain Intensity and Bacterial Load Reduction in Necrotic Tooth
NCT06314113Not specifiedUNKNOWNEvaluation of Oral EGCG Treatment for L-SIL Associated With HPV Infection

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.

57 molecules share ≥1 primary target. Top 57 by shared-target count:

MoleculeSourceStatusShared targets
COENZYME_AChEMBLPhase 3EP300, KAT2B
CURCUMINChEMBLPhase 3DYRK1A, EP300
AFATINIBChEMBL + PubChemPhase 4 (approved)DYRK1A
BELUMOSUDILChEMBL + PubChemPhase 4 (approved)DYRK1A
ABEMACICLIBChEMBLPhase 4 (approved)DYRK1A
AFATINIB DIMALEATEChEMBLPhase 4 (approved)DYRK1A
ISOPROTERENOLChEMBLPhase 4 (approved)TAS2R5
MIDOSTAURINChEMBLPhase 4 (approved)DYRK1A
NIRAPARIBChEMBLPhase 4 (approved)DYRK1A
PALBOCICLIBChEMBLPhase 4 (approved)DYRK1A
RUCAPARIBChEMBLPhase 4 (approved)DYRK1A
RUXOLITINIBChEMBLPhase 4 (approved)DYRK1A
SUNITINIBChEMBLPhase 4 (approved)DYRK1A
TOVORAFENIBChEMBLPhase 4 (approved)DYRK1A
ALVOCIDIBChEMBLPhase 3DYRK1A
BARASERTIBChEMBLPhase 3DYRK1A
CANERTINIBChEMBLPhase 3DYRK1A
CRENOLANIBChEMBLPhase 3DYRK1A
DEFACTINIBChEMBLPhase 3DYRK1A
ENZASTAURINChEMBLPhase 3DYRK1A
LESTAURTINIBChEMBLPhase 3DYRK1A
LORECIVIVINTChEMBLPhase 3DYRK1A
RUBOXISTAURINChEMBLPhase 3DYRK1A
AT-7519ChEMBLPhase 2DYRK1A
AT-9283ChEMBLPhase 2DYRK1A
BGT-226 FREE BASEChEMBLPhase 2DYRK1A
BMS-690514ChEMBLPhase 2DYRK1A
CC-401ChEMBLPhase 2DYRK1A
LY-2090314ChEMBLPhase 2DYRK1A
MILCICLIBChEMBLPhase 2DYRK1A
MIVEBRESIBChEMBLPhase 2EP300
MOLIBRESIBChEMBLPhase 2EP300
R-406ChEMBLPhase 2DYRK1A
RG-547ChEMBLPhase 2DYRK1A
SELICICLIBChEMBLPhase 2DYRK1A
SILMITASERTIBChEMBLPhase 2DYRK1A
STREPTONIGRINChEMBLPhase 2EP300
SU-014813ChEMBLPhase 2DYRK1A
TG100-115ChEMBLPhase 2DYRK1A
UPROSERTIBChEMBLPhase 2DYRK1A
ZOTIRACICLIBChEMBLPhase 2DYRK1A
AlprazolamPubChemApprovedKAT2B
Berberine ChloridePubChemApprovedEP300
BinimetinibPubChemApprovedDYRK1A
CrizotinibPubChemApprovedDYRK1A
dacomitinibPubChemApprovedDYRK1A
EstazolamPubChemApprovedKAT2B
FostamatinibPubChemApprovedDYRK1A
GefitinibPubChemApprovedDYRK1A
IdelalisibPubChemApprovedDYRK1A
MidazolamPubChemApprovedKAT2B
p-aminophenolPubChemApprovedKAT2B
PazopanibPubChemApprovedDYRK1A
regorafenibPubChemApprovedDYRK1A
SelumetinibPubChemApprovedDYRK1A
TrametinibPubChemApprovedDYRK1A
TriazolamPubChemApprovedKAT2B

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