benzbromarone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

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
Renal impairment 45.09 27.54 29 876 81304 29492318
Hepatic function abnormal 29.39 27.54 17 888 39242 29534380

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
Renal impairment 68.35 30.39 39 1251 134978 64362464
Hepatic function abnormal 39.09 30.39 21 1269 64292 64433150

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Drug Use (View source of the data)

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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:

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
Multidrug resistance-associated protein 1 Transporter Ki 6.72 CHEMBL
Cytochrome P450 2C9 Enzyme IC50 7.80 DRUG MATRIX
Aldo-keto reductase family 1 member C1 Enzyme IC50 7.32 CHEMBL
Tyrosine-protein phosphatase non-receptor type 1 Enzyme IC50 4.27 CHEMBL
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
5-hydroxytryptamine receptor 2B GPCR Ki 5.94 DRUG MATRIX
Eyes absent homolog 2 Enzyme IC50 4.99 CHEMBL
Eyes absent homolog 3 Enzyme IC50 5.08 CHEMBL
Envelope glycoprotein gp160 Viral envelope protein IC50 4.89 CHEMBL
Polymerase acidic protein Enzyme Kd 4.32 CHEMBL
Eyes absent homolog 3 Enzyme IC50 4.96 CHEMBL
Envelope glycoprotein gp160 [Cleaved into: Surface protein gp120 Unclassified IC50 4.89 CHEMBL
Inosine-5'-monophosphate dehydrogenase Unclassified IC50 4.26 CHEMBL
M1-family alanyl aminopeptidase Enzyme IC50 4.20 CHEMBL

External reference:

IDSource
N0000166974 NUI
D01056 KEGG_DRUG
1385 RXNORM
C0005035 UMLSCUI
CHEBI:3023 CHEBI
R75 PDB_CHEM_ID
CHEMBL388590 ChEMBL_ID
D001553 MESH_DESCRIPTOR_UI
DB12319 DRUGBANK_ID
2333 PUBCHEM_CID
1427 INN_ID
4POG0RL69O UNII
005311 NDDF
698025001 SNOMEDCT_US
703372005 SNOMEDCT_US

Pharmaceutical products:

None