romidepsin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
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: ONP

  • 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 ┬ÁM/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

Approvals:

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

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
Peripheral T-cell lymphoma unspecified 263.12 51.93 29 229 57 2357770
Thrombocytopenia 53.13 51.93 17 241 19114 2338713
Pyrexia 52.34 51.93 22 236 53686 2304141

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
Peripheral T-cell lymphoma unspecified 365.70 52.00 44 283 91 1746363
Angioimmunoblastic T-cell lymphoma 68.26 52.00 9 318 45 1746409

Pharmacologic Action:

SourceCodeDescription
ATC L01XX39 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
MeSH PA D000903 Antibiotics, Antineoplastic
MeSH PA D000970 Antineoplastic Agents
CHEBI has role CHEBI:35610 antineoplastic agent
FDA EPC N0000175588 Histone Deacetylase Inhibitor
FDA MoA N0000175071 Histone Deacetylase Inhibitors

Drug Use (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

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)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histone deacetylase Enzyme INHIBITOR Ki 5.96 IUPHAR DRUG LABEL
Histone deacetylase 4 Enzyme IC50 6.29 WOMBAT-PK
Histone deacetylase 7 Enzyme INHIBITOR Ki 5.90 IUPHAR
Histone deacetylase 6 Enzyme Ki 6.52 WOMBAT-PK
Histone deacetylase 3 Enzyme Ki 7.60 WOMBAT-PK
Histone deacetylase 1 Enzyme IC50 7 WOMBAT-PK
Histone deacetylase 2 Enzyme IC50 7.33 WOMBAT-PK
Histone deacetylase 9 Enzyme INHIBITOR Ki 5.96 IUPHAR
Histone deacetylase 5 Enzyme INHIBITOR Ki 6.26 IUPHAR
Histone deacetylase 8 Enzyme INHIBITOR Ki 9.82 IUPHAR
Histone deacetylase 3/NCoR1 Transcription factor Ki 9.82 CHEMBL
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) Transcription factor IC50 7.74 CHEMBL
Histone deacetylase 6 Unclassified IC50 6.41 CHEMBL

External reference:

IDSource
4029461 VUID
N0000180306 NUI
C1527027 UMLSCUI
D06637 KEGG_DRUG
444737005 SNOMEDCT_US
877510 RXNORM
26838 MMSL
4029461 VANDF
444608004 SNOMEDCT_US
d07512 MMSL
013396 NDDF
267261 MMSL
CX3T89XQBK UNII
8656 INN_ID
CHEMBL343448 ChEMBL_ID
DB06176 DRUGBANK_ID
CHEBI:61080 CHEBI
5352062 PUBCHEM_CID
7006 IUPHAR_LIGAND_ID
C087123 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Romidepsin HUMAN PRESCRIPTION DRUG LABEL 1 0069-0983 KIT 10 mg None NDA AUTHORIZED GENERIC 20 sections
Romidepsin HUMAN PRESCRIPTION DRUG LABEL 1 0703-3071 INJECTION, SOLUTION, CONCENTRATE 5 mg INTRAVENOUS NDA 18 sections
Romidepsin HUMAN PRESCRIPTION DRUG LABEL 1 0703-3125 KIT 10 mg None NDA AUTHORIZED GENERIC 20 sections
Romidepsin HUMAN PRESCRIPTION DRUG LABEL 1 0703-4004 INJECTION, SOLUTION, CONCENTRATE 5 mg INTRAVENOUS NDA 18 sections
ISTODAX HUMAN PRESCRIPTION DRUG LABEL 1 59572-983 KIT 10 mg None NDA 19 sections
ISTODAX HUMAN PRESCRIPTION DRUG LABEL 1 59572-984 KIT 10 mg None NDA 19 sections