romidepsin indications/contra

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

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 5, 2009 FDA CELGENE

FDA Adverse Event Reporting System

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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 231.53 51.85 29 533 122 3385175
Thrombocytopenia 147.29 51.85 48 514 35220 3350077
Pyrexia 108.35 51.85 48 514 81067 3304230
Death 95.89 51.85 54 508 152270 3233027
Vomiting 91.35 51.85 44 518 89487 3295810
Fatigue 86.71 51.85 45 517 107195 3278102
Nausea 84.17 51.85 47 515 129598 3255699
Anaemia 81.47 51.85 35 527 54298 3330999
Decreased appetite 66.27 51.85 28 534 41462 3343835
Mycosis fungoides 64.52 51.85 11 551 458 3384839
Neutropenia 61.62 51.85 25 537 33361 3351936
T-cell lymphoma 61.12 51.85 10 552 323 3384974
Disease progression 52.18 51.85 22 540 32237 3353060
Febrile neutropenia 52.10 51.85 19 543 18956 3366341

Pharmacologic Action:

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

Drug Use (View source of the data)

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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 DOID:784
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

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG/VIAL ISTODAX CELGENE N022393 Nov. 5, 2009 RX POWDER IV (INFUSION) June 16, 2018 TREATMENT OF PERIPHERAL T-CELL LYMPHOMA (PTCL) IN PATIENTS WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY

Bioactivity Summary:

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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:

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IDSource
4029461 VUID
N0000180306 NUI
C1527027 UMLSCUI
7006 IUPHAR_LIGAND_ID
D06637 KEGG_DRUG
877510 RXNORM
26838 MMSL
4029461 VANDF
N0000180306 NDFRT
444608004 SNOMEDCT_US
444737005 SNOMEDCT_US
d07512 MMSL
013396 NDDF
267261 MMSL
5352062 PUBCHEM_CID
CHEMBL1213490 ChEMBL_ID
CX3T89XQBK UNII
8656 INN_ID
DB06176 DRUGBANK_ID
C087123 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:61080 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Romidepsin HUMAN PRESCRIPTION DRUG LABEL 1 0069-0983 KIT 10 mg None NDA authorized generic 19 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