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flufenamic acid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory, anthranilic acid derivatives | 1193 | 530-78-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically. (From Martindale, The Extra Pharmacopoeia, 30th ed, p16)
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.50 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.03 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 7 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 30.48 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.118 | Moderate | 0.65 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.526 | Moderate | 0.65 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 82.035 | 10^-6 cm/s | Moderate | 0.65 |
| dh-clint | Dog hepatocyte intrinsic clearance | 38.107 | uL/min/10^6 cells | Moderate | 0.65 |
| dppb | Dog plasma protein binding (% unbound) | 0.310 | % | Moderate | 0.65 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.520 | % | Moderate | 0.65 |
| herg | hERG pIC50 | 4.405 | pIC50 | Moderate | 0.65 |
| hh-clint | Human hepatocyte intrinsic clearance | 48.306 | uL/min/10^6 cells | Moderate | 0.65 |
| hlm-clint | Human liver microsomal intrinsic clearance | 12.503 | uL/min/mg protein | Moderate | 0.65 |
| hppb | Human plasma protein binding (% unbound) | 0.350 | % | Moderate | 0.65 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,GRK2,GSK3B,IKBKB,JAK2,MAP2K6,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 38 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,BRAF,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,GRK2,JAK1,MAPK7,MTOR,PDK4,PIK3CD,PRKDC,SIK2,SIK3,STK33,TTK | 20 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.698 | Moderate | 0.65 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 66.681 | Moderate | 0.65 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.700 | Moderate | 0.65 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.203 | Moderate | 0.65 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.640 | % | Moderate | 0.65 |
| rh-clint | Rat hepatocyte intrinsic clearance | 105.682 | uL/min/10^6 cells | Moderate | 0.65 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 28.050 | % | Moderate | 0.65 |
| rppb | Rat plasma protein binding (% unbound) | 0.300 | % | Moderate | 0.65 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 734.514 | uM | Moderate | 0.65 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1963 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M01AG03 | MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Fenamates |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
| CHEBI has role | CHEBI:35493 | antipyretic |
| CHEBI has role | CHEBI:35544 | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor |
Related Drugs by ATC class:
M01AG Fenamates 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pain | indication | 22253000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.21 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Enzyme | INHIBITOR | IC50 | 6.93 | WOMBAT-PK | KEGG DRUG | |||
| Prostaglandin G/H synthase 1 | Enzyme | INHIBITOR | IC50 | 5.52 | WOMBAT-PK | KEGG DRUG | |||
| Transthyretin | Secreted | Kd | 7.25 | WOMBAT-PK | |||||
| Androgen receptor | Nuclear hormone receptor | IC50 | 4.12 | WOMBAT-PK | |||||
| Aldose reductase | Enzyme | IC50 | 4 | CHEMBL | |||||
| Aldo-keto reductase family 1 member C1 | Enzyme | IC50 | 5.22 | WOMBAT-PK | |||||
| Aldo-keto reductase family 1 member C2 | Enzyme | IC50 | 6 | WOMBAT-PK | |||||
| Aldo-keto reductase family 1 member C3 | Enzyme | IC50 | 6.10 | WOMBAT-PK | |||||
| Potassium channel subfamily K member 2 | Ion channel | EC50 | 4 | CHEMBL | |||||
| Myeloperoxidase | Enzyme | IC50 | 5.74 | CHEMBL | |||||
| Potassium channel subfamily T member 2 | Ion channel | ACTIVATOR | EC50 | 8.85 | IUPHAR | ||||
| Transient receptor potential cation channel subfamily A member 1 | Ion channel | EC50 | 5.16 | CHEMBL | |||||
| Transient receptor potential cation channel subfamily M member 2 | Ion channel | IC50 | 4.15 | CHEMBL | |||||
| Transient receptor potential cation channel subfamily M member 4 | Ion channel | IC50 | 5.55 | CHEMBL | |||||
| Aldo-keto reductase family 1 member B10 | Enzyme | IC50 | 6.12 | CHEMBL | |||||
| Transient receptor potential cation channel subfamily M member 5 | Ion channel | IC50 | 4.62 | WOMBAT-PK | |||||
| Transcriptional enhancer factor TEF-3 | Transcription factor | IC50 | 4.27 | CHEMBL | |||||
| Transcriptional enhancer factor TEF-4 | Transcription factor | Kd | 4.14 | CHEMBL | |||||
| Nicotinate phosphoribosyltransferase | Enzyme | Ki | 11 | CHEMBL | |||||
| Taste receptor type 2 member 14 | GPCR | AGONIST | EC50 | 6.86 | SCIENTIFIC LITERATURE | ||||
| Prostaglandin G/H synthase 1 | Enzyme | IC50 | 4.85 | CHEMBL | |||||
| Transient receptor potential cation channel subfamily M member 4 | Ion channel | GATING INHIBITOR | IC50 | 5.60 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| N0000166663 | NUI |
| D01581 | KEGG_DRUG |
| C0016282 | UMLSCUI |
| CHEBI:42638 | CHEBI |
| FLF | PDB_CHEM_ID |
| CHEMBL23588 | ChEMBL_ID |
| DB02266 | DRUGBANK_ID |
| D005439 | MESH_DESCRIPTOR_UI |
| 3371 | PUBCHEM_CID |
| 2447 | IUPHAR_LIGAND_ID |
| 1495 | INN_ID |
| 60GCX7Y6BH | UNII |
| 4453 | RXNORM |
| 004195 | NDDF |
| 1156232002 | SNOMEDCT_US |
| 60GCX7Y6BH | INXIGHT DRUGS |
Pharmaceutical products:
None