Romidepsin
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Also known as ChromadaxDepsipeptideFK-228FK228FR-901228FR901228IstodaxNSC-630176RomidepsinaRomidepsineNSC754143ROMIDEPSIN (FK228 ,DEPSIPEPTIDE)CYCLIC (1.FWDARW.2)-DISULFIDEFK 228FR 901228NSC 630176RomedepsinSID144206460
Summary
Romidepsin (CHEMBL343448) is an approved protein antineoplastic agent (ATC L01XH02) targeting HDAC2, HDAC3, and HDAC6; indicated across 47 conditions including primary cutaneous t-cell non-hodgkin lymphoma and peripheral t-cell lymphoma, not otherwise specified.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Protein
- ATC class: L01XH02
- Targets: 9 (HDAC2, HDAC3, HDAC6…)
- Indications: 47 conditions
- Clinical trials: 94
- Chemistry: 540.7 Da · C24H36N4O6S2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL343448 |
| Name | Romidepsin |
| Type | Protein |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 5352062 |
| ChEBI | CHEBI:61080 |
| ATC | L01XH02 |
| Molecular formula | C24H36N4O6S2 |
| Molecular weight | 540.7 |
| InChIKey | OHRURASPPZQGQM-GCCNXGTGSA-N |
SMILES: C/C=C\1/C(=O)N[C@H](C(=O)O[C@H]\2CC(=O)N[C@@H](C(=O)N[C@H](CSSCC/C=C2)C(=O)N1)C(C)C)C(C)C
IUPAC name: (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
ChEBI definition: A cyclodepsipeptide consisting of the cyclic disulfide of (2Z)-2-aminobut-2-enoyl, L-valyl, (3S,4E)-3-hydroxy-7-sulfanylhept-4-enoyl, D-valyl and D-cysteinyl residues coupled in sequence and cyclised head-to tail.
Pharmacological roles (ChEBI): antineoplastic agent, EC 3.5.1.98 (histone deacetylase) inhibitor.
Also known as: Chromadax, Depsipeptide, FK-228, FK228, FR-901228, FR901228, Istodax, NSC-630176, Romidepsin, Romidepsina, Romidepsine, NSC754143
Patent coverage: 5,445 distinct patent families (12,963 SureChEMBL compound mentions), from 1 matched compound structure(s). 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 |
|---|---|---|---|---|---|
| HDAC2 | histone deacetylase 2 | Inhibition | 10.42 | 3.1% | Q92769 |
| HDAC3 | histone deacetylase 3 | Inhibition | 9.82 | 95.1% (common-essential) | O15379 |
| HDAC6 | histone deacetylase 6 | Inhibition | 8.02 | 0% | Q9UBN7 |
| HDAC8 | histone deacetylase 8 | Inhibition | 9.82 | 4.9% | Q9BY41 |
| HDAC9 | histone deacetylase 9 | Inhibition | 5.96 | 0% | Q9UKV0 |
| HDAC1 | histone deacetylase 1 | Inhibition | 11.82 | 4.5% | Q13547 |
| HDAC4 | histone deacetylase 4 | Inhibition | 7.69 | 3.1% | P56524 |
| HDAC5 | histone deacetylase 5 | Inhibition | 6.26 | 0.5% | Q9UQL6 |
| HDAC7 | histone deacetylase 7 | Inhibition | 5.9 | 4.2% | Q8WUI4 |
Broader ChEMBL bioactivity targets: 21 (assay-derived). Sample: Bromodomain-containing protein 4, Histone deacetylase 3, Protein deacetylase HDAC6, Histone deacetylase 2, Thromboxane A2 receptor, Histone deacetylase, Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2), Histone deacetylase 5, Histone deacetylase 7, Protein deacetylase HDAC6.
Bioactivity
ChEMBL activities: 132 potent at pChembl ≥ 5 of 136 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HDAC2 | 10.42 | Ki | 0.04 | nM | CHEMBL_ACT_13431789 |
| HDAC2 | 10.42 | Ki | 0.04 | nM | CHEMBL_ACT_3389934 |
| HDAC8 | 9.82 | Ki | 0.15 | nM | CHEMBL_ACT_13431777 |
| HDAC3 | 9.82 | Ki | 0.15 | nM | CHEMBL_ACT_13431782 |
| HDAC3 | 9.82 | Ki | 0.15 | nM | CHEMBL_ACT_3389935 |
| HDAC8 | 9.82 | Ki | 0.15 | nM | CHEMBL_ACT_3389940 |
| HDAC1 | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_10981405 |
| HDAC11 | 9.52 | IC50 | 0.3 | nM | CHEMBL_ACT_15136657 |
| HDAC11 | 9.52 | IC50 | 0.3 | nM | CHEMBL_ACT_22975017 |
| HDAC11 | 9.52 | IC50 | 0.3 | nM | CHEMBL_ACT_25992126 |
| HDAC1 | 9.51 | IC50 | 0.31 | nM | CHEMBL_ACT_14550859 |
| HDAC2 | 9.33 | Ki | 0.47 | nM | CHEMBL_ACT_25472544 |
| Q9Z2V5 | 9.2 | IC50 | 0.62 | nM | CHEMBL_ACT_15002559 |
| HDAC1 | 9.1 | IC50 | 0.8 | nM | CHEMBL_ACT_15136621 |
| HDAC1 | 9.06 | Ki | 0.88 | nM | CHEMBL_ACT_25472541 |
| HDAC10 | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_15136660 |
| HDAC3 | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_24420366 |
| HDAC2 | 9 | IC50 | 1 | nM | CHEMBL_ACT_10981401 |
| HDAC1 | 9 | IC50 | 1 | nM | CHEMBL_ACT_12074993 |
| HDAC1 | 9 | IC50 | 1 | nM | CHEMBL_ACT_15002545 |
| HDAC2 | 9 | IC50 | 1 | nM | CHEMBL_ACT_15136618 |
| HDAC3 | 9 | IC50 | 1 | nM | CHEMBL_ACT_18784792 |
| HDAC10 | 9 | IC50 | 1 | nM | CHEMBL_ACT_22974842 |
| HDAC1 | 9 | IC50 | 1 | nM | CHEMBL_ACT_22974886 |
| HDAC2 | 9 | IC50 | 1 | nM | CHEMBL_ACT_22974890 |
| HDAC3 | 9 | IC50 | 1 | nM | CHEMBL_ACT_22974894 |
| HDAC1 | 9 | IC50 | 1 | nM | CHEMBL_ACT_25992086 |
| HDAC2 | 9 | IC50 | 1 | nM | CHEMBL_ACT_25992090 |
| HDAC3 | 9 | IC50 | 1 | nM | CHEMBL_ACT_25992094 |
| HDAC10 | 9 | IC50 | 1 | nM | CHEMBL_ACT_25992122 |
Target pathways
Aggregated over 9 target gene(s): HDAC2, HDAC3, HDAC6, HDAC8, HDAC9, HDAC1, HDAC4, HDAC5, HDAC7.
Top Reactome pathways
71 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| NOTCH1 Intracellular Domain Regulates Transcription | 9 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| Constitutive Signaling by NOTCH1 PEST Domain Mutants | 9 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants | 9 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| Notch-HLH transcription pathway | 9 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells) | 9 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| Regulation of PTEN gene transcription | 5 | HDAC1, HDAC2, HDAC3, HDAC5, HDAC7 |
| HDACs deacetylate histones | 4 | HDAC1, HDAC2, HDAC3, HDAC8 |
| p75NTR negatively regulates cell cycle via SC1 | 3 | HDAC1, HDAC2, HDAC3 |
| SUMOylation of chromatin organization proteins | 3 | HDAC1, HDAC2, HDAC4 |
| Regulation of MECP2 expression and activity | 3 | HDAC1, HDAC2, HDAC3 |
| STAT3 nuclear events downstream of ALK signaling | 3 | HDAC1, HDAC2, HDAC3 |
| ERCC6 (CSB) and EHMT2 (G9a) positively regulate rRNA expression | 2 | HDAC1, HDAC2 |
| NoRC negatively regulates rRNA expression | 2 | HDAC1, HDAC2 |
| Regulation of TP53 Activity through Acetylation | 2 | HDAC1, HDAC2 |
| RNA Polymerase I Transcription Initiation | 2 | HDAC1, HDAC2 |
| RUNX2 regulates osteoblast differentiation | 2 | HDAC3, HDAC6 |
| MECP2 regulates neuronal receptors and channels | 2 | HDAC1, HDAC2 |
| FOXO-mediated transcription of oxidative stress, metabolic and neuronal genes | 2 | HDAC1, HDAC2 |
| Potential therapeutics for SARS | 2 | HDAC1, HDAC2 |
| Negative Regulation of CDH1 Gene Transcription | 2 | HDAC1, HDAC2 |
| Factors involved in megakaryocyte development and platelet production | 2 | HDAC1, HDAC2 |
| Regulation of endogenous retroelements by KRAB-ZFP proteins | 2 | HDAC1, HDAC2 |
| Transcriptional regulation of brown and beige adipocyte differentiation by EBF2 | 2 | HDAC1, HDAC2 |
| Regulation of endogenous retroelements by Piwi-interacting RNAs (piRNAs) | 2 | HDAC1, HDAC2 |
| NuRD complex assembly | 2 | HDAC1, HDAC2 |
| Interaction of NuRD complexes with transcription factors | 2 | HDAC1, HDAC2 |
| Transcription of E2F targets under negative control by DREAM complex | 1 | HDAC1 |
| Transcription of E2F targets under negative control by p107 (RBL1) and p130 (RBL2) in complex with HDAC1 | 1 | HDAC1 |
| G0 and Early G1 | 1 | HDAC1 |
| PPARA activates gene expression | 1 | HDAC3 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| chromatin organization | 9 |
| negative regulation of transcription by RNA polymerase II | 8 |
| negative regulation of DNA-templated transcription | 8 |
| positive regulation of transcription by RNA polymerase II | 5 |
| protein deacetylation | 5 |
| epigenetic regulation of gene expression | 5 |
| negative regulation of gene expression, epigenetic | 5 |
| negative regulation of macromolecule biosynthetic process | 4 |
| chromatin remodeling | 3 |
| positive regulation of cell population proliferation | 3 |
| response to xenobiotic stimulus | 3 |
| heterochromatin formation | 3 |
| circadian regulation of gene expression | 3 |
| positive regulation of intracellular estrogen receptor signaling pathway | 3 |
| negative regulation of apoptotic process | 3 |
Indications & clinical
Indications
47 indications (6 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 |
|---|---|---|---|
| primary cutaneous T-cell non-Hodgkin lymphoma | 4 | MONDO:0000607 | EFO:0002913 |
| peripheral T-cell lymphoma, not otherwise specified | 4 | MONDO:0004964 | EFO:0000211 |
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| mature T-cell and NK-cell non-Hodgkin lymphoma | 4 | MONDO:0000430 | MONDO:0000430 |
| T-cell non-Hodgkin lymphoma | 4 | MONDO:0015760 | MONDO:0015760 |
| angioimmunoblastic T-cell lymphoma | 3 | MONDO:0004977 | EFO:0000255 |
| lymphoma | 3 | MONDO:0005062 | EFO:0000574 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| HIV infectious disease | 2 | MONDO:0005109 | EFO:0000180 |
| acute promyelocytic leukemia | 2 | MONDO:0012883 | EFO:0000224 |
| diffuse large B-cell lymphoma | 2 | MONDO:0018905 | EFO:0000403 |
| thyroid gland follicular carcinoma | 2 | MONDO:0005034 | EFO:0000501 |
| gastric adenocarcinoma | 2 | MONDO:0005036 | EFO:0000503 |
| thyroid gland papillary carcinoma | 2 | MONDO:0005075 | EFO:0000641 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| male breast carcinoma | 2 | MONDO:0005628 | EFO:0006861 |
| mantle cell lymphoma | 2 | MONDO:0018876 | EFO:1001469 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| follicular lymphoma | 2 | MONDO:0018906 | MONDO:0018906 |
| anaplastic large cell lymphoma | 2 | MONDO:0020325 | EFO:0003032 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| anaplastic astrocytoma | 1 | MONDO:0016684 | EFO:0002499 |
| anaplastic oligodendroglioma | 1 | MONDO:0016696 | EFO:0002501 |
| gliosarcoma | 1 | MONDO:0016681 | EFO:1001465 |
| Hodgkins lymphoma | 1 | MONDO:0004952 | EFO:0000183 |
| leukemia | 1 | MONDO:0005059 | EFO:0000565 |
| liposarcoma | 1 | MONDO:0005060 | EFO:0000569 |
| exocrine pancreatic carcinoma | 1 | MONDO:0005192 | EFO:0002618 |
| triple-negative breast carcinoma | 1 | MONDO:0005494 | EFO:0005537 |
| non-Hodgkin lymphoma | 1 | MONDO:0018908 | EFO:0005952 |
| Sezary syndrome | 1 | MONDO:0017844 | EFO:1000785 |
| inflammatory breast carcinoma | 1 | MONDO:0006804 | EFO:1000984 |
| mycosis fungoides | 1 | MONDO:0009691 | EFO:1001051 |
| glioblastoma | 1 | MONDO:0018177 | EFO:0000519 |
| brain neoplasm | 1 | MONDO:0021211 | EFO:0003833 |
| pancreatic ductal adenocarcinoma | 1 | MONDO:0005184 | MONDO:0005184 |
| hematopoietic and lymphoid system neoplasm | 1 | MONDO:0002334 | MONDO:0044881 |
5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 94.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 33 |
| PHASE1 | 32 |
| PHASE1/PHASE2 | 20 |
| PHASE3 | 5 |
| Not specified | 3 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03703375 | PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety of Oral Azacitidine (CC-486) Compared to Investigator’s Choice Therapy in Patients With Relapsed or Refractory Angioimmunoblastic T Cell Lymphoma |
| NCT01482962 | PHASE3 | COMPLETED | Alisertib (MLN8237) or Investigator’s Choice in Patients With Relapsed/Refractory Peripheral T-Cell Lymphoma |
| NCT01796002 | PHASE3 | COMPLETED | Efficacy and Safety of Romidepsin CHOP vs CHOP in Patients With Untreated Peripheral T-Cell Lymphoma |
| NCT03355768 | PHASE3 | WITHDRAWN | Romidepsin Versus Combination of Romidepsin Plus Pralatrexate in PTCL |
| NCT03593018 | PHASE3 | COMPLETED | Efficacy and Safety of Oral Azacitidine Compared to Investigator’s Choice Therapy in Patients With Relapsed or Refractory AITL |
| NCT02393794 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Cisplatin Plus Romidepsin & Nivolumab in Locally Recurrent or Metastatic Triple Negative Breast Cancer (TNBC) |
| NCT03161223 | PHASE1/PHASE2 | RECRUITING | Durvalumab in Different Combinations With Pralatrexate, Romidepsin and Oral 5-Azacitidine for Lymphoma |
| NCT03278782 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Study of Pembrolizumab (MK-3475) in Combination With Romidepsin |
| NCT04747236 | PHASE2 | RECRUITING | Randomized Phase IIB Trial of Oral Azacytidine Plus Romidepsin Versus Investigator’s Choice in PTCL |
| NCT00007345 | PHASE2 | COMPLETED | Depsipeptide to Treat Patients With Cutaneous T-Cell Lymphoma and Peripheral T-Cell Lymphoma |
| NCT00020202 | PHASE2 | COMPLETED | FR901228 in Treating Patients With Refractory or Progressive Small Cell Lung Cancer or Non-small Cell Lung Cancer |
| NCT00042822 | PHASE2 | COMPLETED | FR901228 in Treating Patients With Myelodysplastic Syndrome, Acute Myeloid Leukemia, or Non-Hodgkin’s Lymphoma |
| NCT00062075 | PHASE2 | COMPLETED | Romidepsin in Treating Patients With Relapsed or Refractory Acute Myeloid Leukemia |
| NCT00066638 | PHASE2 | COMPLETED | FR901228 in Treating Patients With Relapsed or Refractory Multiple Myeloma |
| NCT00077194 | PHASE2 | COMPLETED | FR901228 in Treating Patients With Relapsed or Refractory Non-Hodgkin’s Lymphoma |
| NCT00077337 | PHASE2 | COMPLETED | FR901228 in Treating Patients With Previously Treated Unresectable Locally Advanced or Metastatic Colorectal Cancer |
| NCT00079443 | PHASE2 | TERMINATED | FR901228 Alone or Combined With Rituximab and Fludarabine in Treating Patients With Relapsed or Refractory Low-Grade B-Cell Non-Hodgkin’s Lymphoma |
| NCT00084461 | PHASE2 | TERMINATED | Romidepsin in Treating Patients With Locally Advanced or Metastatic Neuroendocrine Tumors |
| NCT00084682 | PHASE2 | COMPLETED | Depsipeptide in Unresectable Recurrent or Metastatic Squamous Cell Carcinoma of the Head and Neck |
| NCT00085527 | PHASE2 | WITHDRAWN | FR901228 in Treating Patients With Relapsed or Refractory Advanced Ovarian Epithelial Cancer |
| NCT00085540 | PHASE1/PHASE2 | COMPLETED | FR901228 in Treating Patients With Recurrent High-Grade Gliomas |
| NCT00086827 | PHASE2 | COMPLETED | Romidepsin in Treating Patients With Relapsed Small Cell Lung Cancer |
| NCT00087295 | PHASE2 | TERMINATED | S0400, FR901228 in Treating Patients With Advanced Cancer of the Urothelium |
| NCT00091195 | PHASE2 | TERMINATED | Depsipeptide (Romidepsin) in Treating Patients With Recurrent Ovarian Epithelial or Peritoneal Cavity Cancer |
| NCT00098397 | PHASE2 | COMPLETED | FR901228 in Treating Patients With Metastatic Breast Cancer |
| NCT00098527 | PHASE2 | TERMINATED | FR901228 in Treating Patients With Refractory Stomach Cancer or Gastroesophageal Junction Cancer |
| NCT00098813 | PHASE2 | COMPLETED | Romidepsin in Treating Patients With Recurrent and/or Metastatic Thyroid Cancer That Has Not Responded to Radioactive Iodine |
| NCT00104884 | PHASE2 | TERMINATED | FR901228 in Treating Patients With Unresectable Stage III or Stage IV Malignant Melanoma |
| NCT00106301 | PHASE2 | COMPLETED | Continuation Trial Evaluating the Tolerability and Activity of FK228 in Patients That Completed Prior Study With FK228 |
| NCT00106418 | PHASE2 | COMPLETED | A Research Study for Patients With Prostate Cancer |
| NCT00106613 | PHASE2 | COMPLETED | A Research Study for Patients With Metastatic Renal Cell Carcinoma |
| NCT00112463 | PHASE2 | COMPLETED | Depsipeptide (Romidepsin) in Treating Patients With Metastatic or Unresectable Soft Tissue Sarcoma |
| NCT00299351 | PHASE2 | UNKNOWN | A Multicenter, Open-Label Continuation Trial Evaluating the Tolerability and Activity of Depsipeptide (FK228) in Patients That Have Completed a Prior Clinical Study With Depsipeptide. |
| NCT00383565 | PHASE2 | TERMINATED | FR901228 in Treating Patients With Relapsed or Refractory Non-Hodgkin’s Lymphoma |
| NCT00426764 | PHASE2 | COMPLETED | A Trial of Romidepsin for Progressive or Relapsed Peripheral T-cell Lymphoma |
| NCT00431990 | PHASE1/PHASE2 | UNKNOWN | A Phase I/II Trial of Romidepsin (Depsipeptide) and Bortezomib in Patients With Relapsed Myeloma |
| NCT00765102 | PHASE2 | TERMINATED | Trial of Romidepsin and Bortezomib for Multiple Myeloma |
| NCT01280526 | PHASE1/PHASE2 | COMPLETED | A Study of Escalating Doses of Romidepsin in Association With CHOP in the Treatment of Peripheral T-Cell Lymphomas |
| NCT01353664 | PHASE2 | COMPLETED | A Rollover Study for Patients Who Participated in Other Romidepsin Protocols |
| NCT01456039 | PHASE1/PHASE2 | COMPLETED | A Japanese Phase 1/2 Study to Assess the Efficacy, Safety and Pharmacokinetics of Romidepsin in Patients With Peripheral T-cell Lymphoma (PTCL) |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
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.
96 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| BELINOSTAT | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| CELECOXIB | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| GIVINOSTAT | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| PANOBINOSTAT | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| PHENYLBUTANOIC ACID | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| SODIUM PHENYLBUTYRATE | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| VORINOSTAT | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| ABEXINOSTAT | ChEMBL | Phase 3 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| CAFFEIC ACID | ChEMBL | Phase 3 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| CURCUMIN | ChEMBL | Phase 3 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| ENTINOSTAT | ChEMBL | Phase 3 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| PRACINOSTAT | ChEMBL | Phase 3 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| TACEDINALINE | ChEMBL | Phase 3 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| TUCIDINOSTAT | ChEMBL | Phase 3 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| AR-42 | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| CHLOROGENIC ACID | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| DACINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| FIMEPINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| NANATINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| QUISINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| Pazopanib | PubChem | Approved | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9 |
| RICOLINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8 |
| BENDAMUSTINE | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC8 |
| TINOSTAMUSTINE | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC8 |
| CITARINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC6, HDAC7, HDAC8 |
| BORTEZOMIB | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 |
| MOCETINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 |
| EBSELEN | ChEMBL | Phase 3 | HDAC2, HDAC5, HDAC6, HDAC9 |
| BUTYRIC ACID | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC8 |
| DOMATINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC9 |
| SODIUM BUTYRATE | ChEMBL | Phase 2 | HDAC1, HDAC2, HDAC3, HDAC8 |
| ATORVASTATIN | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC6 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | HDAC1, HDAC6, HDAC8 |
| LOVASTATIN | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2, HDAC6 |
| BAICALEIN | ChEMBL | Phase 2 | HDAC1, HDAC6, HDAC8 |
| .gamma.-aminobutyric acid | PubChem | Approved | HDAC5, HDAC7, HDAC9 |
| acetylcysteine | PubChem | Approved | HDAC5, HDAC7, HDAC9 |
| Crizotinib | PubChem | Approved | HDAC1, HDAC2, HDAC6 |
| VALPROIC ACID | ChEMBL | Phase 4 (approved) | HDAC1, HDAC2 |
| MOLIBRESIB | ChEMBL | Phase 2 | HDAC1, HDAC2 |
| NICOXAMAT | ChEMBL | Phase 2 | HDAC1, HDAC6 |
| RESMINOSTAT | ChEMBL | Phase 2 | HDAC1, HDAC6 |
| Gefitinib | PubChem | Approved | HDAC5, HDAC9 |
| Idelalisib | PubChem | Approved | HDAC1, HDAC6 |
| ABAMETAPIR | ChEMBL | Phase 4 (approved) | HDAC6 |
| ATALUREN | ChEMBL | Phase 4 (approved) | HDAC6 |
| AXITINIB | ChEMBL | Phase 4 (approved) | HDAC6 |
| BUFEXAMAC | ChEMBL | Phase 4 (approved) | HDAC6 |
| EVANS BLUE FREE ACID | ChEMBL | Phase 4 (approved) | HDAC6 |
| EXIFONE | ChEMBL | Phase 4 (approved) | HDAC1 |
| FEBUXOSTAT | ChEMBL | Phase 4 (approved) | HDAC6 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | HDAC6 |
| GENTIAN VIOLET | ChEMBL | Phase 4 (approved) | HDAC6 |
| INDOPROFEN | ChEMBL | Phase 4 (approved) | HDAC6 |
| MARIBAVIR | ChEMBL | Phase 4 (approved) | HDAC6 |
| MOMELOTINIB | ChEMBL | Phase 4 (approved) | HDAC1 |
| MONOBENZONE | ChEMBL | Phase 4 (approved) | HDAC6 |
| NITAZOXANIDE | ChEMBL | Phase 4 (approved) | HDAC6 |
| PHENYL AMINOSALICYLATE | ChEMBL | Phase 4 (approved) | HDAC6 |
| PIPERACETAZINE | ChEMBL | Phase 4 (approved) | HDAC6 |
Related Atlas pages
- Genes: HDAC2, HDAC3, HDAC6, HDAC8, HDAC9, HDAC1, HDAC4, HDAC5, HDAC7
- Diseases: primary cutaneous T-cell non-Hodgkin lymphoma, peripheral T-cell lymphoma, not otherwise specified, neoplasm, mature T-cell and NK-cell non-Hodgkin lymphoma, T-cell non-Hodgkin lymphoma, angioimmunoblastic T-cell lymphoma, lymphoma
- Drugs: Belinostat, Celecoxib, Givinostat, Panobinostat, Phenylbutanoic Acid, Abexinostat, Caffeic Acid, Curcumin, Entinostat, Pracinostat, Tacedinaline, Tucidinostat, Pazopanib, Bendamustine, Bortezomib, Ebselen, Atorvastatin, Daunorubicin, Lovastatin, acetylcysteine, Crizotinib, Valproic Acid, Gefitinib, Idelalisib, Abametapir, Ataluren, Axitinib, Bufexamac, Evans Blue Free Acid, Exifone, Febuxostat, Fluphenazine, Indoprofen, Maribavir, Momelotinib, Monobenzone, Nitazoxanide, Phenyl Aminosalicylate, Piperacetazine