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oxyphenbutazone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory analgesics, phenylbutazone derivatives | 2036 | 129-20-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A non-steroidal anti-inflammatory drug. Oxyphenbutazone eyedrops have been used abroad in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. (From AMA, Drug Evaluations Annual, 1994, p2000) It had been used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p27)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
| 0.30 | g | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 35.23 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| S (Water solubility) | 1 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.905 | High | 0.87 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.914 | High | 0.87 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 62.373 | 10^-6 cm/s | High | 0.87 |
| dh-clint | Dog hepatocyte intrinsic clearance | 4.853 | uL/min/10^6 cells | High | 0.87 |
| dppb | Dog plasma protein binding (% unbound) | 2.210 | % | High | 0.87 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.830 | % | High | 0.87 |
| herg | hERG pIC50 | 4.608 | pIC50 | High | 0.87 |
| hh-clint | Human hepatocyte intrinsic clearance | 4.529 | uL/min/10^6 cells | High | 0.87 |
| hlm-clint | Human liver microsomal intrinsic clearance | 5.140 | uL/min/mg protein | High | 0.87 |
| hppb | Human plasma protein binding (% unbound) | 1.090 | % | High | 0.87 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K21,MAP3K7,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 | 57 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,CAMK2D,GRK2,MAP2K6,MAPK7,STK33,TEK,TTK | 10 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 5.035 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 6.607 | High | 0.87 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 19.454 | High | 0.87 | |
| mppb | Mouse plasma protein binding (% unbound) | 2.490 | High | 0.87 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.133 | High | 0.87 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.890 | % | High | 0.87 |
| rat-kpuu-brain | Rat brain Kpuu | 0.260 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 6.918 | uL/min/10^6 cells | High | 0.87 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 70.050 | % | High | 0.87 |
| rppb | Rat plasma protein binding (% unbound) | 0.820 | % | High | 0.87 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 887.156 | uM | High | 0.87 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 21, 1960 | FDA |
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 | M01AA03 | MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Butylpyrazolidines |
| ATC | M02AA04 | MUSCULO-SKELETAL SYSTEM TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN Antiinflammatory preparations, non-steroids for topical use |
| ATC | S01BC02 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFLAMMATORY AGENTS Antiinflammatory agents, non-steroids |
| 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:33281 | antimicrobial agent |
| 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:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:35845 | gout suppressant |
| CHEBI has role | CHEBI:49103 | drug metabolite |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
| CHEBI has role | CHEBI:76206 | xenobiotic metabolite |
Related Drugs by ATC class:
M01AA Butylpyrazolidines 4 drugs
M02AA Antiinflammatory preparations, non-steroids for topical use 28 drugs
S01BC Antiinflammatory agents, non-steroids 10 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 | 4.62 | acidic |
| pKa2 | 7.03 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Cyclooxygenase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| fMet-Leu-Phe receptor | GPCR | WOMBAT-PK | |||||||
| Prostacyclin synthase | Enzyme | WOMBAT-PK | |||||||
| Nicotinate phosphoribosyltransferase | Enzyme | Ki | 9.52 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019078 | VUID |
| N0000147339 | NUI |
| D08324 | KEGG_DRUG |
| 7081-38-1 | SECONDARY_CAS_RN |
| 4019078 | VANDF |
| C0030078 | UMLSCUI |
| CHEBI:76259 | CHEBI |
| OPB | PDB_CHEM_ID |
| CHEMBL3989676 | ChEMBL_ID |
| DB03585 | DRUGBANK_ID |
| D010113 | MESH_DESCRIPTOR_UI |
| 4641 | PUBCHEM_CID |
| H806S4B3NS | UNII |
| 7816 | RXNORM |
| 002376 | NDDF |
| 387269008 | SNOMEDCT_US |
| 49267000 | SNOMEDCT_US |
Pharmaceutical products:
None