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benzbromarone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiarrhythmics | 318 | 3562-84-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.471 | Moderate | 0.77 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.684 | Moderate | 0.77 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 37.068 | 10^-6 cm/s | Moderate | 0.77 |
| dh-clint | Dog hepatocyte intrinsic clearance | 13.740 | uL/min/10^6 cells | Moderate | 0.77 |
| dppb | Dog plasma protein binding (% unbound) | 0.140 | % | Moderate | 0.77 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.240 | % | Moderate | 0.77 |
| herg | hERG pIC50 | 4.700 | pIC50 | Moderate | 0.77 |
| hh-clint | Human hepatocyte intrinsic clearance | 20.417 | uL/min/10^6 cells | Moderate | 0.77 |
| hlm-clint | Human liver microsomal intrinsic clearance | 101.158 | uL/min/mg protein | Moderate | 0.77 |
| hppb | Human plasma protein binding (% unbound) | 1.150 | % | Moderate | 0.77 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 5.929 | Moderate | 0.77 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 20.989 | Moderate | 0.77 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.190 | Moderate | 0.77 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.932 | Moderate | 0.77 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 0.130 | % | Moderate | 0.77 |
| rh-clint | Rat hepatocyte intrinsic clearance | 55.719 | uL/min/10^6 cells | Moderate | 0.77 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 3.210 | % | Moderate | 0.77 |
| rppb | Rat plasma protein binding (% unbound) | 0.260 | % | Moderate | 0.77 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 157.398 | uM | Moderate | 0.77 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Renal impairment | 46.63 | 26.79 | 33 | 1243 | 110195 | 42509864 |
| Hepatic function abnormal | 32.91 | 26.79 | 20 | 1256 | 51547 | 42568512 |
| Interstitial lung disease | 29.72 | 26.79 | 22 | 1254 | 78440 | 42541619 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Renal impairment | 85.49 | 30.49 | 47 | 1729 | 188398 | 110399125 |
| Hepatic function abnormal | 48.05 | 30.49 | 25 | 1751 | 89270 | 110498253 |
| Interstitial lung disease | 32.95 | 30.49 | 23 | 1753 | 139311 | 110448212 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M04AB03 | MUSCULO-SKELETAL SYSTEM ANTIGOUT PREPARATIONS ANTIGOUT PREPARATIONS Preparations increasing uric acid excretion |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:35841 | uricosuric drug |
| CHEBI has role | CHEBI:35845 | gout suppressant |
| MeSH PA | D006074 | Gout Suppressants |
| MeSH PA | D014528 | Uricosuric Agents |
| MeSH PA | D018501 | Antirheumatic Agents |
Related Drugs by ATC class:
M04AB Preparations increasing uric acid excretion 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.91 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Solute carrier family 22 member 12 | Transporter | INHIBITOR | IC50 | 7.59 | CHEMBL | SCIENTIFIC LITERATURE | |||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 5.94 | DRUG MATRIX | |||||
| Adenosine receptor A3 | GPCR | Ki | 5.53 | DRUG MATRIX | |||||
| Transthyretin | Secreted | Kd | 7.82 | CHEMBL | |||||
| Multidrug resistance-associated protein 1 | Transporter | Ki | 6.72 | CHEMBL | |||||
| ATP-binding cassette sub-family G member 2 | Transporter | IC50 | 6.70 | 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 | |||||
| Solute carrier family 22 member 6 | Transporter | IC50 | 5.67 | CHEMBL | |||||
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Enzyme | IC50 | 5.68 | CHEMBL | |||||
| Thyroid hormone receptor beta | Nuclear hormone receptor | Kd | 5.05 | CHEMBL | |||||
| Mitogen-activated protein kinase 14 | Kinase | IC50 | 5.91 | DRUG MATRIX | |||||
| Mitogen-activated protein kinase 1 | Kinase | IC50 | 5.71 | DRUG MATRIX | |||||
| Eyes absent homolog 2 | Enzyme | IC50 | 4.99 | CHEMBL | |||||
| Eyes absent homolog 3 | Enzyme | IC50 | 5.08 | CHEMBL | |||||
| Piezo-type mechanosensitive ion channel component 1 | Ion channel | INHIBITOR | IC50 | 5.40 | IUPHAR | ||||
| Bile acid receptor | Nuclear hormone receptor | EC50 | 4.61 | CHEMBL | |||||
| M1-family alanyl aminopeptidase | Enzyme | IC50 | 4.20 | 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 | Viral envelope protein | IC50 | 4.89 | CHEMBL | |||||
| Inosine-5'-monophosphate dehydrogenase | Enzyme | IC50 | 4.26 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 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 |
| 14007 | IUPHAR_LIGAND_ID |
| 1427 | INN_ID |
| 4POG0RL69O | UNII |
| 005311 | NDDF |
| 698025001 | SNOMEDCT_US |
| 703372005 | SNOMEDCT_US |
| 4POG0RL69O | INXIGHT DRUGS |
Pharmaceutical products:
None