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Tucidinostat

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Also known as ChidamideCS-055CS055EpidazaEpidaza in chinaHBI-8000Tucidinostat

Summary

Tucidinostat (CHEMBL3621988) is a phase-3 clinical-stage small molecule (ATC L01XH06) targeting HDAC1; indicated across 40 conditions including peripheral t-cell lymphoma, not otherwise specified and diffuse large b-cell lymphoma.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • ATC class: L01XH06
  • Targets: 1 (HDAC1)
  • Indications: 40 conditions
  • Clinical trials: 159
  • Chemistry: 390.4 Da · C22H19FN4O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3621988
NameTucidinostat
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID12136798
ATCL01XH06
Molecular formulaC22H19FN4O2
Molecular weight390.4
InChIKeySZMJVTADHFNAIS-BJMVGYQFSA-N

SMILES: C1=CC(=CN=C1)/C=C/C(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N

IUPAC name: N-(2-amino-4-fluorophenyl)-4-[[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]methyl]benzamide

Also known as: Chidamide, CS-055, CS055, Epidaza, Epidaza in china, HBI-8000, Tucidinostat, TUCIDINOSTAT, chidamide, Chidamide; Tucidinostat

Patent coverage: 909 distinct patent families (2,182 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 2,085 (96%) 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
HDAC1histone deacetylase 1Inhibition4.5%Q13547

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Nicotinamide phosphoribosyltransferase, Histone deacetylase 3, Histone deacetylase 2, Histone deacetylase, Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2), Histone deacetylase 8, Histone deacetylase 1, Histone deacetylase 11, Polyamine deacetylase HDAC10.

Bioactivity

ChEMBL activities: 59 potent at pChembl ≥ 5 of 59 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
HDAC18.05IC509nMCHEMBL_ACT_28736123
HDAC27.32IC5048.25nMCHEMBL_ACT_25876576
HDAC17.21IC5062.12nMCHEMBL_ACT_25561264
HDAC37.2IC5063.3nMCHEMBL_ACT_26111241
HDAC37.17IC5067nMCHEMBL_ACT_25543822
HDAC107.11IC5078nMCHEMBL_ACT_25543828
HDAC37.08IC5082.87nMCHEMBL_ACT_25561268
HDAC27.03IC5093.28nMCHEMBL_ACT_25561266
HDAC17.03IC5093nMCHEMBL_ACT_25694639
HDAC17.02IC5095nMCHEMBL_ACT_25543813
HDAC17.01IC5098.7nMCHEMBL_ACT_26111199
HDAC107IC50100nMCHEMBL_ACT_22974839
HDAC17IC50100nMCHEMBL_ACT_22974884
HDAC37IC50100nMCHEMBL_ACT_22974891
HDAC17IC50100nMCHEMBL_ACT_26150506
HDAC37IC50100nMCHEMBL_ACT_26150516
HDAC107IC50100nMCHEMBL_ACT_26150537
HDAC26.96IC50110nMCHEMBL_ACT_18979102
HDAC16.95IC50112nMCHEMBL_ACT_18520584
HDAC16.91IC50122.1nMCHEMBL_ACT_25876479
HDAC16.89IC50130nMCHEMBL_ACT_18979097
HDAC16.85IC50140nMCHEMBL_ACT_29020580
HDAC26.8IC50160nMCHEMBL_ACT_25543818
HDAC16.79IC50163nMCHEMBL_ACT_26161718
HDAC16.78IC50167nMCHEMBL_ACT_19208641
HDAC36.78IC50167nMCHEMBL_ACT_24958817
HDAC26.74IC50184nMCHEMBL_ACT_26111220
HDAC26.73IC50186nMCHEMBL_ACT_25694644
HDAC16.71IC50196nMCHEMBL_ACT_24418319
HDAC16.71IC50196nMCHEMBL_ACT_24821025

Target pathways

Aggregated over 1 target gene(s): HDAC1.

Top Reactome pathways

42 total, by targets touching each:

PathwayTargetsGenes
Transcription of E2F targets under negative control by DREAM complex1HDAC1
Transcription of E2F targets under negative control by p107 (RBL1) and p130 (RBL2) in complex with HDAC11HDAC1
G0 and Early G11HDAC1
p75NTR negatively regulates cell cycle via SC11HDAC1
Formation of the beta-catenin:TCF transactivating complex1HDAC1
NOTCH1 Intracellular Domain Regulates Transcription1HDAC1
Downregulation of SMAD2/3:SMAD4 transcriptional activity1HDAC1
SMAD2/SMAD3:SMAD4 heterotrimer regulates transcription1HDAC1
Constitutive Signaling by NOTCH1 PEST Domain Mutants1HDAC1
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants1HDAC1
HDACs deacetylate histones1HDAC1
Notch-HLH transcription pathway1HDAC1
Deactivation of the beta-catenin transactivating complex1HDAC1
ERCC6 (CSB) and EHMT2 (G9a) positively regulate rRNA expression1HDAC1
NoRC negatively regulates rRNA expression1HDAC1
SUMOylation of chromatin organization proteins1HDAC1
Repression of WNT target genes1HDAC1
Regulation of TP53 Activity through Acetylation1HDAC1
G1/S-Specific Transcription1HDAC1
RNA Polymerase I Transcription Initiation1HDAC1
RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function1HDAC1
Regulation of PTEN gene transcription1HDAC1
Estrogen-dependent gene expression1HDAC1
Loss of MECP2 binding ability to 5mC-DNA1HDAC1
Regulation of MECP2 expression and activity1HDAC1
MECP2 regulates neuronal receptors and channels1HDAC1
MECP2 regulates transcription of neuronal ligands1HDAC1
FOXO-mediated transcription of oxidative stress, metabolic and neuronal genes1HDAC1
Potential therapeutics for SARS1HDAC1
STAT3 nuclear events downstream of ALK signaling1HDAC1

Dominant GO biological processes

GO termTargets
negative regulation of transcription by RNA polymerase II1
chromatin organization1
chromatin remodeling1
DNA methylation-dependent constitutive heterochromatin formation1
regulation of transcription by RNA polymerase II1
endoderm development1
positive regulation of cell population proliferation1
epidermal cell differentiation1
positive regulation of gene expression1
negative regulation of gene expression1
hippocampus development1
neuron differentiation1
negative regulation of cell migration1
negative regulation of transforming growth factor beta receptor signaling pathway1
heterochromatin formation1

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
peripheral T-cell lymphoma, not otherwise specified3MONDO:0004964EFO:0000211
diffuse large B-cell lymphoma3MONDO:0018905EFO:0000403
lymphoma3MONDO:0005062EFO:0000574
neoplasm3MONDO:0005070EFO:0000616
mature T-cell and NK-cell non-Hodgkin lymphoma3MONDO:0000430MONDO:0000430
breast neoplasm3MONDO:0021100MONDO:0007254
T-cell non-Hodgkin lymphoma3MONDO:0015760MONDO:0015760
neoplasm of mature B-cells2MONDO:0004949EFO:0000096
T-cell acute lymphoblastic leukemia2MONDO:0004963EFO:0000209
acute myeloid leukemia2MONDO:0018874EFO:0000222
adenoid cystic carcinoma2MONDO:0004971EFO:0000231
angioimmunoblastic T-cell lymphoma2MONDO:0004977EFO:0000255
HIV infectious disease2MONDO:0005109EFO:0000764
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
non-Hodgkin lymphoma2MONDO:0018908EFO:0005952
acute lymphoblastic leukemia2MONDO:0004967EFO:0000220
plasma cell myeloma2MONDO:0009693EFO:0001378
thrombocytopenia2MONDO:0002049HP:0001873
Hodgkins lymphoma2MONDO:0004952EFO:0000183
sarcoma2MONDO:0005089EFO:0000691
primary cutaneous T-cell non-Hodgkin lymphoma2MONDO:0000607EFO:0002913
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
nasal cavity and paranasal sinus lethal midline granuloma2MONDO:0006828MONDO:0019472
colorectal carcinoma2MONDO:0024331EFO:1001951
esophageal squamous cell carcinoma2MONDO:0005580EFO:0005922
neuroendocrine carcinoma2MONDO:0002120MONDO:0002120
acute monocytic leukemia2MONDO:0007896EFO:0000221
acute promyelocytic leukemia2MONDO:0012883EFO:0000224
B-cell non-Hodgkin lymphoma2MONDO:0015759EFO:1001938
osteosarcoma2MONDO:0009807EFO:0000637
T-cell leukemia2MONDO:0005525EFO:0005592
colorectal neoplasm2MONDO:0005335MONDO:0005575
AIDS1MONDO:0012268EFO:0000765
cervical adenocarcinoma1MONDO:0005153EFO:0001416
neuroblastoma1MONDO:0005072EFO:0000621
hepatocellular carcinoma1MONDO:0007256EFO:0000182

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

Clinical trials

Total trials: 159.

Phase distribution

PhaseTrials
PHASE293
PHASE1/PHASE232
PHASE311
Not specified10
PHASE18
PHASE2/PHASE33
PHASE42

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04490590PHASE4UNKNOWNA Clinical Trial of Chidamide Combined With Etoposide in Relapsed or Refractory NK/T-cell Lymphoma
NCT05191914PHASE4UNKNOWNClinical Study of Fulvestrant Combined With Chidamide in the Treatment of Hormone Receptor-positive Advanced Breast Cancer Resistant to CDK4/6 Inhibitors
NCT04668690PHASE3ACTIVE_NOT_RECRUITINGClinical Study of Mitoxantrone Hydrochloride Liposome Injection vs. Chidamide in Patients With Relapsed/Refractory PTCL
NCT05678933PHASE3ENROLLING_BY_INVITATIONAC-CHOP Versus CHOP in Patients With Previously Untreated PTCL-TFH
NCT06497985PHASE3RECRUITINGA Study of Tucidinostat in Combination With Sintilimab and Bevacizumab in MSS/pMMR Colorectal Cancer Patients
NCT06947967PHASE3RECRUITINGTucidinostat in Combination With CHOP in Newly Diagnosed Peripheral T-Cell Lymphoma With Follicular Helper of T Cell Phenotype
NCT07234162PHASE3RECRUITINGA Phase 3 Multinational Study of Golidocitinib Versus Investigator’s Choice in r/r PTCL (JACKPOT19)
NCT07493109PHASE3RECRUITINGChidamide for Maintenance Treatment of HBV-infected Diffuse DLBCL in Patients Initially Treated With R-CHOP
NCT02482753PHASE3COMPLETEDTrial of Chidamide in Combination With Exemestane in Patients With Advanced Breast Cancer
NCT03023358PHASE3UNKNOWNCompared the Efficacy and Safety of CDOP Combined With Chidamide and CDOP in de Novo Peripheral T Cell Lymphoma Patients
NCT03553238PHASE2/PHASE3UNKNOWNPrecision Diagnosis Directing HDACi Chidamide Target Therapy for Adult ETP-ALL
NCT03564470PHASE2/PHASE3UNKNOWNPrecision Diagnosis Directing HDACi and TKI Target Therapy for Adult Ph-like ALL
NCT03564704PHASE2/PHASE3UNKNOWNPrecision Diagnosis Directing HDACi Chidamide Target Therapy for Adult T-LBL/ALL
NCT04231448PHASE3COMPLETEDPhase III Study of Tucidinostat in Combination With R-CHOP in Patients With Newly Diagnosed Double-Expressor DLBCL
NCT05075460PHASE3UNKNOWNTucidinostat, Azacitidine Combined With CHOP Versus CHOP in Patients With Untreated Peripheral T-cell Lymphoma
NCT05466318PHASE3UNKNOWNChiCGB vs BEAM in High-risk or R/R Lymphomas
NCT03031262PHASE1/PHASE2ACTIVE_NOT_RECRUITINGEfficacy and Safety of Chidamide in CBF Leukemia
NCT04025450PHASE1/PHASE2RECRUITINGComparation of Chidamide Plus VRD (Bortezomib, Lenalidomide, Dexamethasone) With VRD Regimen for Primary High-Risk Multiple Myeloma Patients
NCT04562311PHASE2ACTIVE_NOT_RECRUITINGChidamide With Immunotherapy for Patients With Locally Advanced or Metastatic Urothelial Carcinoma
NCT04985890PHASE2NOT_YET_RECRUITINGA Proof of Concept Study to Evaluate the Effect of UB-421 in Combination With Chidamide on HIV Viral Reservoir
NCT05270200PHASE1/PHASE2RECRUITINGSingle Arm Study of Post-transplant Azacitidine and Chidamide for Prevention of Acute Myelogenous Leukemia Relapse
NCT05566054PHASE2RECRUITINGVenetoclax and Azacitidine Combined With Chidamide (VAC) for the Treatment of Newly Diagnosed Acute Monocytic Leukemia
NCT05572983PHASE2RECRUITINGPhase Ⅱ Study of Chidamide in Combination With CHOP in Previously Untreated Peripheral T-Cell Lymphoma With Follicular Helper of T Cell Phenotype
NCT05675813PHASE1/PHASE2RECRUITINGGenotype-guided Treatment in Newly Diagnosed PTCL
NCT05682755PHASE1/PHASE2RECRUITINGChidamide Prevents Recurrence of High-risk AML After Allo-HSCT
NCT05833724PHASE2RECRUITINGChidamide in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma (R/R PTCL)
NCT05881265PHASE2RECRUITINGTreatment of Chidamide and Venetoclax for Retinoic Acid and Arsenic Resistant Acute Promyelocytic Leukemia
NCT05958719PHASE2RECRUITINGChidamide in Combination With Azacitidine, Liposomal Mitoxantrone, and Prednisone (CAMP Regimen) for the Treatment of Previously Untreated Nodal TFH Cell Lymphoma
NCT05976997PHASE2RECRUITINGProspective, Single Arm, Single Center Study of Duvelisib Combined With Chidamide in the Treatment of Newly Diagnosed Peripheral T-cell Lymphoma (PTCL)
NCT05983107PHASE2RECRUITINGChidamide/Everolimus for PIK3CA Wild-type/Mutant HR+/HER2- Advanced Breast Cancer
NCT06218888PHASE2NOT_YET_RECRUITINGA Phase II Clinical Study of the Efficacy and Safety of Tislelizumab Combined With Fruquintinib and Chidamide in the Treatment of Unresectable or Advanced Microsatellite Stabilized (MSS/pMMR) Colorectal Cancer With Liver Metastases
NCT06220487PHASE2RECRUITINGA Single-arm, Open-label Study of Olverembatinib, CD3/CD19 Bispecific T-cell Engager, and Chidamide in Patients With Newly Diagnosed Ph+ALL
NCT06421948PHASE1/PHASE2RECRUITINGLinperlisib Combined With Chidamide in Patients With PTCL
NCT06451861PHASE2RECRUITINGRandomized Study of ABC-14 Regimen Compared With 3+7 Standard Induction Therapy or AB-14 for ND AML
NCT06492629PHASE2ACTIVE_NOT_RECRUITINGToripalimab Combined With Chidamide for the Treatment of Relapsed/Refractory Peripheral T-Cell Lymphoma
NCT06516978PHASE2NOT_YET_RECRUITINGA Study Comparing the Efficacy and Safety of Pola-RCHP-X Versus RCHOP-X and Pola-RCHP in Previously Untreated Patients With DLBCL
NCT06550336PHASE2ACTIVE_NOT_RECRUITINGA Clinical Study Assessing the Efficacy of Chidamide for CD30-positive Peripheral T-cell Lymphoma (PTCL).
NCT06556862PHASE2NOT_YET_RECRUITINGExploration of Dalpiciclib Plus HDACi in HR+/HER2- Advanced Breast Cancer After Failure of CDK4/6 Inhibitor
NCT06570447PHASE2RECRUITINGGlofitamab Combination With Chidamide in Patients With Recurrent/Refractory DLBCL
NCT06685276PHASE2RECRUITINGSafety and Efficacy of Fruquintinib Plus Chidamide and Sintilimab in the Third and Later Line Treatment of MSS/pMMR Metastatic Colorectal Cancer

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.

42 molecules share ≥1 primary target. Top 42 by shared-target count:

MoleculeSourceStatusShared targets
ATORVASTATINChEMBLPhase 4 (approved)HDAC1
BELINOSTATChEMBLPhase 4 (approved)HDAC1
BENDAMUSTINEChEMBLPhase 4 (approved)HDAC1
BORTEZOMIBChEMBLPhase 4 (approved)HDAC1
CELECOXIBChEMBLPhase 4 (approved)HDAC1
DAUNORUBICINChEMBLPhase 4 (approved)HDAC1
EXIFONEChEMBLPhase 4 (approved)HDAC1
GIVINOSTATChEMBLPhase 4 (approved)HDAC1
LOVASTATINChEMBLPhase 4 (approved)HDAC1
MOMELOTINIBChEMBLPhase 4 (approved)HDAC1
PANOBINOSTATChEMBLPhase 4 (approved)HDAC1
PHENYLBUTANOIC ACIDChEMBLPhase 4 (approved)HDAC1
ROMIDEPSINChEMBLPhase 4 (approved)HDAC1
SODIUM PHENYLBUTYRATEChEMBLPhase 4 (approved)HDAC1
VALPROIC ACIDChEMBLPhase 4 (approved)HDAC1
VORINOSTATChEMBLPhase 4 (approved)HDAC1
ABEXINOSTATChEMBLPhase 3HDAC1
CAFFEIC ACIDChEMBLPhase 3HDAC1
CURCUMINChEMBLPhase 3HDAC1
ENTINOSTATChEMBLPhase 3HDAC1
PRACINOSTATChEMBLPhase 3HDAC1
TACEDINALINEChEMBLPhase 3HDAC1
AR-42ChEMBLPhase 2HDAC1
BAICALEINChEMBLPhase 2HDAC1
BUTYRIC ACIDChEMBLPhase 2HDAC1
CHLOROGENIC ACIDChEMBLPhase 2HDAC1
CITARINOSTATChEMBLPhase 2HDAC1
DACINOSTATChEMBLPhase 2HDAC1
DOMATINOSTATChEMBLPhase 2HDAC1
FIMEPINOSTATChEMBLPhase 2HDAC1
MOCETINOSTATChEMBLPhase 2HDAC1
MOLIBRESIBChEMBLPhase 2HDAC1
NANATINOSTATChEMBLPhase 2HDAC1
NICOXAMATChEMBLPhase 2HDAC1
QUISINOSTATChEMBLPhase 2HDAC1
RESMINOSTATChEMBLPhase 2HDAC1
RICOLINOSTATChEMBLPhase 2HDAC1
SODIUM BUTYRATEChEMBLPhase 2HDAC1
TINOSTAMUSTINEChEMBLPhase 2HDAC1
CrizotinibPubChemApprovedHDAC1
IdelalisibPubChemApprovedHDAC1
PazopanibPubChemApprovedHDAC1

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