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bufexamac 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory agents, ibufenac derivatives | 3047 | 2438-72-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A benzeneacetamide with anti-inflammatory, analgesic, and antipyretic action. It is administered topically, orally, or rectally.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.883 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.957 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 52 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 43.853 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 23.360 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 29.660 | % | High | 1 |
| herg | hERG pIC50 | 4.099 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 48.195 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 9.886 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 16.860 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EGFR,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,MAP2K6,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK | 22 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.770 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 358.922 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 21.830 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.799 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 37.380 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 107.895 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 93.370 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 16.760 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 781.628 | uM | High | 1 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Appendicolith | 125.86 | 103.94 | 30 | 1282 | 14225 | 110573762 |
| Blood phosphorus increased | 116.74 | 103.94 | 29 | 1283 | 16311 | 110571676 |
| Blood uric acid increased | 108.81 | 103.94 | 29 | 1283 | 21500 | 110566487 |
| Appendicitis | 105.28 | 103.94 | 30 | 1282 | 28434 | 110559553 |
| Myasthenia gravis | 104.09 | 103.94 | 28 | 1284 | 21483 | 110566504 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M01AB17 | MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Acetic acid derivatives and related substances |
| ATC | M02AA09 | MUSCULO-SKELETAL SYSTEM TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN Antiinflammatory preparations, non-steroids for topical use |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
| CHEBI has role | CHEBI:35493 | antipyretic |
Related Drugs by ATC class:
M01AB Acetic acid derivatives and related substances 16 drugs
M02AA Antiinflammatory preparations, non-steroids for topical use 28 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.5 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Histone deacetylase 6 | Enzyme | INHIBITOR | Kd | 4.97 | IUPHAR | ||||
| Histone deacetylase 10 | Enzyme | INHIBITOR | Kd | 4.91 | IUPHAR | ||||
| Arachidonate 5-lipoxygenase | Enzyme | IC50 | 6.89 | CHEMBL | |||||
| M1-family alanyl aminopeptidase | Enzyme | IC50 | 4.09 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000166889 | NUI |
| D01271 | KEGG_DRUG |
| C0006351 | UMLSCUI |
| CHEBI:31317 | CHEBI |
| CHEMBL94394 | ChEMBL_ID |
| DB13346 | DRUGBANK_ID |
| D002019 | MESH_DESCRIPTOR_UI |
| 2466 | PUBCHEM_CID |
| 7498 | IUPHAR_LIGAND_ID |
| 2557 | INN_ID |
| 4T3C38J78L | UNII |
| 1796 | RXNORM |
| 003713 | NDDF |
| 273952005 | SNOMEDCT_US |
| 332124001 | SNOMEDCT_US |
| A4Z | PDB_CHEM_ID |
| 4T3C38J78L | INXIGHT DRUGS |
Pharmaceutical products:
None