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tolfenamic 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 | 2698 | 13710-19-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
| 0.30 | g | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 8 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 21.83 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 60 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.16 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.37 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.15 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.222 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.380 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 87.096 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 130.918 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.230 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.320 | % | High | 1 |
| herg | hERG pIC50 | 4.324 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 109.648 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 23.823 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.280 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K21,MAP3K7,MAPK12,MAPK14,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 | 55 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,BRAF,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,JAK1,MAP2K6,MAPK7,MTOR,PDK4,SIK2,SIK3,STK33,TEK,TTK | 21 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.905 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 102.329 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.530 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.486 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.310 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 193.642 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 32.620 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.160 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 522.396 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1976 | 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 | M01AG02 | MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Fenamates |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D011448 | Prostaglandin Antagonists |
| MeSH PA | D012702 | Serotonin Antagonists |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
| CHEBI has role | CHEBI:35544 | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:77194 | EC 2.7.1.33 (pantothenate kinase) inhibitor |
Related Drugs by ATC class:
M01AG Fenamates 3 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 | 4.43 | 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 | IC50 | 8.30 | WOMBAT-PK | |||||
| Prostaglandin G/H synthase 1 | Enzyme | IC50 | 6.24 | WOMBAT-PK | |||||
| Transthyretin | Secreted | IC50 | 4.40 | CHEMBL | |||||
| Androgen receptor | Nuclear hormone receptor | IC50 | 4.33 | WOMBAT-PK | |||||
| Aldo-keto reductase family 1 member C3 | Enzyme | Ki | 8.10 | CHEMBL | |||||
| Cytochrome c oxidase subunit 2 | Enzyme | IC50 | 5.93 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01183 | KEGG_DRUG |
| C0076799 | UMLSCUI |
| CHEBI:32243 | CHEBI |
| TLF | PDB_CHEM_ID |
| CHEMBL121626 | ChEMBL_ID |
| DB09216 | DRUGBANK_ID |
| C009500 | MESH_SUPPLEMENTAL_RECORD_UI |
| 610479 | PUBCHEM_CID |
| 8769 | IUPHAR_LIGAND_ID |
| 2926 | INN_ID |
| 3G943U18KM | UNII |
| 38377 | RXNORM |
| 006023 | NDDF |
| 322817007 | SNOMEDCT_US |
| 395910008 | SNOMEDCT_US |
Pharmaceutical products:
None