benzbromarone indications/contra

Stem definitionDrug idCAS RN
antiarrhythmics 318 3562-84-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • benzbromarone
  • benzbromaron
  • azubromaron
Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.
  • Molecular weight: 424.09
  • Formula: C17H12Br2O3
  • CLOGP: 5.98
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 1
  • TPSA: 50.44
  • ALOGS: -4.51
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.10 g O

Approvals:

None

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC M04AB03 MUSCULO-SKELETAL SYSTEM
ANTIGOUT PREPARATIONS
ANTIGOUT PREPARATIONS
Preparations increasing uric acid excretion
MeSH PA D018501 Antirheumatic Agents
MeSH PA D006074 Gout Suppressants
MeSH PA D012076 Renal Agents
MeSH PA D014528 Uricosuric Agents
CHEBI has role CHEBI:35841 uricosuric drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hyperuricemia indication 35885006 DOID:1920
Gout indication 90560007 DOID:13189

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.91 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Solute carrier family 22 member 12 Transporter INHIBITOR IC50 7.59 CHEMBL SCIENTIFIC LITERATURE
Adenosine receptor A3 GPCR Ki 5.53 DRUG MATRIX
Cytochrome P450 2C9 Enzyme IC50 7.80 DRUG MATRIX
cAMP-specific 3',5'-cyclic phosphodiesterase 4A Enzyme IC50 5.98 DRUG MATRIX
Mitogen-activated protein kinase 14 Kinase IC50 5.91 DRUG MATRIX
Mitogen-activated protein kinase 1 Kinase IC50 5.71 DRUG MATRIX
Multidrug resistance-associated protein 1 Transporter Ki 6.72 CHEMBL
Aldo-keto reductase family 1 member C1 Enzyme IC50 7.32 CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 5.94 DRUG MATRIX
Envelope glycoprotein gp160 Unclassified IC50 4.89 CHEMBL
M1-family alanyl aminopeptidase Unclassified IC50 4.20 CHEMBL

External reference:

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IDSource
N0000166974 NUI
C0005035 UMLSCUI
D01056 KEGG_DRUG
4POG0RL69O UNII
1427 INN_ID
1385 RXNORM
N0000166974 NDFRT
698025001 SNOMEDCT_US
703372005 SNOMEDCT_US
005311 NDDF
CHEMBL388590 ChEMBL_ID
2333 PUBCHEM_CID
DB12319 DRUGBANK_ID
D001553 MESH_DESCRIPTOR_UI
CHEBI:3023 CHEBI

Pharmaceutical products:

None