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

Stem definitionDrug idCAS RN
histone deacetylase inhibitors 4876 414864-00-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • belinostat
  • beleodaq
  • PXD101
a hydroxamate-type inhibitor of histone deacetylase
  • Molecular weight: 318.35
  • Formula: C15H14N2O4S
  • CLOGP: 1.18
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 3
  • TPSA: 95.50
  • ALOGS: -4.05
  • ROTB: 4

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.80 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 23.60 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.06 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 3, 2014 FDA SPECTRUM PHARMS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XH04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Histone deacetylase (HDAC) inhibitors
FDA MoA N0000175071 Histone Deacetylase Inhibitors
FDA EPC N0000175588 Histone Deacetylase Inhibitor
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D056572 Histone Deacetylase Inhibitors
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:61115 hdac inhibitor

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Peripheral T-cell lymphoma indication 109977009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.83 acidic
pKa2 9.83 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
500MG/VIAL BELEODAQ ACROTECH N206256 July 3, 2014 RX POWDER INTRAVENOUS July 3, 2021 TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY PERIPHERAL T-CELL LYMPHOMA

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histone deacetylase 4 Enzyme INHIBITOR IC50 7.57 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Histone deacetylase 10 Enzyme INHIBITOR Ki 7.23 CHEMBL CHEMBL
Histone deacetylase 11 Enzyme INHIBITOR Ki 7.57 CHEMBL CHEMBL
Histone deacetylase 8 Enzyme INHIBITOR Ki 7.66 CHEMBL CHEMBL
Histone deacetylase 9 Enzyme INHIBITOR Ki 7.62 CHEMBL CHEMBL
Histone deacetylase 6 Enzyme INHIBITOR Ki 8.80 CHEMBL CHEMBL
Histone deacetylase 1 Enzyme INHIBITOR Ki 9.07 CHEMBL CHEMBL
Histone deacetylase 3 Enzyme INHIBITOR Ki 8.82 CHEMBL CHEMBL
Histone deacetylase 2 Enzyme INHIBITOR Ki 9.07 CHEMBL CHEMBL
Histone deacetylase 5 Enzyme INHIBITOR Ki 7.60 CHEMBL CHEMBL
Histone deacetylase 7 Enzyme INHIBITOR Ki 7.29 CHEMBL CHEMBL

External reference:

IDSource
F4H96P17NZ UNII
D08870 KEGG_DRUG
4033540 VUID
N0000190861 NUI
866323-14-0 SECONDARY_CAS_RN
4033540 VANDF
C3834212 UMLSCUI
CHEBI:94531 CHEBI
5OG PDB_CHEM_ID
CHEMBL408513 ChEMBL_ID
DB05015 DRUGBANK_ID
8823 INN_ID
C487081 MESH_SUPPLEMENTAL_RECORD_UI
6918638 PUBCHEM_CID
7496 IUPHAR_LIGAND_ID
1543543 RXNORM
222033 MMSL
30383 MMSL
d08271 MMSL
015607 NDDF
704194004 SNOMEDCT_US
704195003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Beleodaq Human Prescription Drug Label 1 72893-002 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS NDA 27 sections