romidepsin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
depsipeptide derivatives 4119 128517-07-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • romidepsin
  • chromadax
  • istodax
  • FR901228
  • FK228
a bicyclic depsipeptide and a potent histone deacetylase inhibitor from Chromobacterium violaceum
  • Molecular weight: 540.69
  • Formula: C24H36N4O6S2
  • CLOGP: 3.44
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 4
  • TPSA: 142.70
  • ALOGS: -4.41
  • ROTB: 2
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.64 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 1.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 7.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.07 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 11 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PRKDC,TEK 16
kinase-selectivity-class BRAF,GRK2,PDK1 3
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
July 3, 2017 PMDA Celgene KK
Nov. 5, 2009 FDA CELGENE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Electrocardiogram QT prolonged 114.22 44.03 39 959 72417 90555032
Platelet count decreased 61.63 44.03 30 968 136939 90490510
Thrombocytopenia 60.41 44.03 34 964 208691 90418758
Atrial fibrillation 53.36 44.03 27 971 133584 90493865
Tumour lysis syndrome 47.81 44.03 13 985 11139 90616310

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Thrombocytopenia 57.17 37.08 45 1144 190234 42429912
Disease progression 49.71 37.08 37 1152 143619 42476527
Platelet count decreased 46.39 37.08 35 1154 138546 42481600

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Platelet count decreased 104.08 38.40 60 1972 230383 110356884
Thrombocytopenia 99.94 38.40 68 1964 348817 110238450
Atrial fibrillation 85.93 38.40 53 1979 229589 110357678
Malignant neoplasm progression 59.45 38.40 38 1994 174529 110412738
Therapy partial responder 55.25 38.40 22 2010 37039 110550228
Disease progression 52.33 38.40 40 1992 243994 110343273
Tumour lysis syndrome 48.41 38.40 19 2013 30782 110556485
Pyrexia 46.90 38.40 69 1963 898196 109689071
Death 39.78 38.40 56 1976 698813 109888454
Cytopenia 38.44 38.40 16 2016 30100 110557167

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XH02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Histone deacetylase (HDAC) inhibitors
FDA MoA N0000175071 Histone Deacetylase Inhibitors
MeSH PA D000903 Antibiotics, Antineoplastic
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D056572 Histone Deacetylase Inhibitors
FDA EPC N0000175588 Histone Deacetylase Inhibitor
FDA MoA N0000187061 Organic Cation Transporter 2 Inhibitors
FDA MoA N0000190107 Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA N0000190108 Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA N0000190110 Organic Anion Transporter 1 Inhibitors
FDA MoA N0000193845 Bile Salt Export Pump Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:61115 EC 3.5.1.98 (histone deacetylase) inhibitor

Related Drugs by ATC class:

L01XH Histone deacetylase (HDAC) inhibitors 4 drugs
belinostatpanobinostattucidinostatvorinostat

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Peripheral T-cell lymphoma indication 109977009
Primary cutaneous T-cell lymphoma indication 400122007
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Lymphocytopenia contraindication 48813009 DOID:614
Leukopenia contraindication 84828003 DOID:615
Chronic renal failure syndrome contraindication 90688005
Prolonged QT interval contraindication 111975006
Acute disease of cardiovascular system contraindication 128487001
Hypomagnesemia contraindication 190855004
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Breastfeeding (mother) contraindication 413712001
Congenital long QT syndrome contraindication 442917000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.47 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
27.5MG/5.5ML (5MG/ML) ROMIDEPSIN AMNEAL A219099 June 2, 2026 RX SOLUTION INTRAVENOUS Dec. 7, 2026 COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Histone deacetylase Enzyme INHIBITOR Ki 5.96 IUPHAR DRUG LABEL
Histone deacetylase 2 Enzyme IC50 7.33 WOMBAT-PK
Histone deacetylase 1 Enzyme IC50 7 WOMBAT-PK
Histone deacetylase 3 Enzyme Ki 7.60 WOMBAT-PK
Histone deacetylase 6 Enzyme Ki 6.52 WOMBAT-PK
Histone deacetylase 7 Enzyme INHIBITOR Ki 5.90 IUPHAR
Histone deacetylase 8 Enzyme INHIBITOR Ki 9.82 IUPHAR
Histone deacetylase 5 Enzyme INHIBITOR Ki 6.26 IUPHAR
Histone deacetylase 9 Enzyme INHIBITOR Ki 5.96 IUPHAR
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase IC50 4.24 CHEMBL
Bromodomain-containing protein 4 Nuclear other IC50 7.44 CHEMBL
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) Transcription factor IC50 7.74 CHEMBL
Histone deacetylase 3/NCoR1 Transcription factor Ki 9.82 CHEMBL
Histone deacetylase 4 Enzyme IC50 6.29 WOMBAT-PK
Histone deacetylase 6 Enzyme IC50 6.41 CHEMBL

External reference:

IDSource
4029461 VUID
N0000180306 NUI
D06637 KEGG_DRUG
4029461 VANDF
C1527027 UMLSCUI
CHEBI:61080 CHEBI
CHEMBL343448 ChEMBL_ID
DB06176 DRUGBANK_ID
C087123 MESH_SUPPLEMENTAL_RECORD_UI
7006 IUPHAR_LIGAND_ID
8656 INN_ID
CX3T89XQBK UNII
5352062 PUBCHEM_CID
877436 RXNORM
169125 MMSL
267261 MMSL
26838 MMSL
d07512 MMSL
013396 NDDF
444608004 SNOMEDCT_US
444737005 SNOMEDCT_US
CX3T89XQBK INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ROMIDEPSIN HUMAN PRESCRIPTION DRUG LABEL 1 70121-2250 INJECTION, SOLUTION, CONCENTRATE 5 mg INTRAVENOUS ANDA 28 sections