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oxaprozin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2013 | 21256-18-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.90 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 1.60 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 88.64 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 98 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TEK,TGFBR1 | 23 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,ERBB2,GRK2 | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 29, 1992 | FDA | GD SEARLE |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 585.70 | 27.87 | 219 | 1004 | 463390 | 90163834 |
| General symptom | 29.46 | 27.87 | 10 | 1213 | 14658 | 90612566 |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 99.92 | 40.13 | 32 | 210 | 99357 | 42521736 |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 615.96 | 30.30 | 213 | 974 | 453877 | 110134235 |
| General symptom | 36.71 | 30.30 | 10 | 1177 | 8836 | 110579276 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M01AE12 | MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Propionic acid derivatives |
| FDA CS | M0001335 | Anti-Inflammatory Agents, Non-Steroidal |
| FDA MoA | N0000000160 | Cyclooxygenase Inhibitors |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D016861 | Cyclooxygenase Inhibitors |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| FDA EPC | N0000175722 | Nonsteroidal Anti-inflammatory Drug |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:35842 | antirheumatic drug |
Related Drugs by ATC class:
M01AE Propionic acid derivatives 21 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Rheumatoid arthritis | indication | 69896004 | DOID:7148 |
| Osteoarthritis | indication | 396275006 | |
| Juvenile rheumatoid arthritis | indication | 410795001 | |
| Ankylosing spondylitis | off-label use | 9631008 | DOID:7147 |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Gastrointestinal ulcer | contraindication | 40845000 | |
| Chronic heart failure | contraindication | 48447003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Hepatic failure | contraindication | 59927004 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Coronary artery bypass graft | contraindication | 232717009 | |
| Pregnancy, function | contraindication | 289908002 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Smokes tobacco daily | contraindication | 449868002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.51 | acidic |
| pKa2 | 0.69 | Basic |
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 | 4.44 | IUPHAR | CHEMBL | |||
| Prostaglandin G/H synthase 1 | Enzyme | INHIBITOR | IC50 | 6.07 | DRUG MATRIX | CHEMBL | |||
| fMet-Leu-Phe receptor | GPCR | WOMBAT-PK | |||||||
| Retinoic acid receptor RXR-alpha | Nuclear hormone receptor | EC50 | 4.79 | CHEMBL | |||||
| Retinoic acid receptor RXR-beta | Nuclear hormone receptor | EC50 | 4.60 | CHEMBL | |||||
| Retinoic acid receptor RXR-gamma | Nuclear hormone receptor | EC50 | 4.40 | CHEMBL | |||||
| Bifunctional epoxide hydrolase 2 | Enzyme | INHIBITOR | IC50 | 5.30 | IUPHAR | ||||
| Complement C5 | Secreted | Kd | 6.19 | CHEMBL | |||||
| Nuclear receptor subfamily 4 group A member 1 | Nuclear other | IC50 | 4.80 | CHEMBL | |||||
| Serine hydroxymethyltransferase, mitochondrial | Enzyme | IC50 | 5.71 | CHEMBL | |||||
| Nuclear receptor subfamily 4 group A member 2 | Nuclear other | IC50 | 4.40 | CHEMBL | |||||
| Nuclear receptor subfamily 4 group A member 3 | Nuclear other | IC50 | 4.66 | CHEMBL | |||||
| Bifunctional epoxide hydrolase 2 [Includes: Cytosolic epoxide hydrolase 2 | Enzyme | IC50 | 4.45 | CHEMBL | |||||
| Bifunctional epoxide hydrolase 2 [Includes: Cytosolic epoxide hydrolase 2 | Enzyme | IC50 | 4.20 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4020735 | VUID |
| N0000148313 | NUI |
| D00463 | KEGG_DRUG |
| 4020735 | VANDF |
| C0069739 | UMLSCUI |
| CHEBI:7822 | CHEBI |
| CHEMBL1071 | ChEMBL_ID |
| DB00991 | DRUGBANK_ID |
| CHEMBL1200463 | ChEMBL_ID |
| D000077431 | MESH_DESCRIPTOR_UI |
| 4614 | PUBCHEM_CID |
| 7252 | IUPHAR_LIGAND_ID |
| 3458 | INN_ID |
| 174064-08-5 | SECONDARY_CAS_RN |
| MHJ80W9LRB | UNII |
| 32613 | RXNORM |
| 41102 | MMSL |
| 5210 | MMSL |
| d00853 | MMSL |
| 004113 | NDDF |
| 108518005 | SNOMEDCT_US |
| 386031002 | SNOMEDCT_US |
| 427736002 | SNOMEDCT_US |
| BJ6 | PDB_CHEM_ID |
| MHJ80W9LRB | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Daypro | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0025-1381 | TABLET, FILM COATED | 600 mg | ORAL | NDA | 32 sections |
| OXAPROZIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-178 | TABLET | 600 mg | ORAL | ANDA | 24 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-100 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 27 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52959-800 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 23 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-4548 | TABLET | 600 mg | ORAL | ANDA | 16 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55111-170 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 28 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60760-382 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 28 sections |
| OXAPROZIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61919-178 | TABLET | 600 mg | ORAL | ANDA | 21 sections |
| OXAPROZIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61919-673 | TABLET | 600 mg | ORAL | ANDA | 21 sections |
| OXAPROZIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62135-176 | TABLET | 600 mg | ORAL | ANDA | 20 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66336-722 | TABLET | 600 mg | ORAL | ANDA | 25 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-0523 | TABLET | 600 mg | ORAL | ANDA | 29 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1120 | TABLET | 600 mg | ORAL | ANDA | 28 sections |
| Coxanto | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69499-403 | CAPSULE | 300 mg | ORAL | NDA | 30 sections |
| OXAPROZIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70332-310 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 20 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70332-311 | TABLET | 600 mg | ORAL | ANDA | 27 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70512-787 | CAPSULE | 300 mg | ORAL | NDA | 18 sections |
| COXANTO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70512-814 | CAPSULE | 300 mg | ORAL | NDA | 32 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-0393 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 27 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-0617 | TABLET | 600 mg | ORAL | ANDA | 28 sections |
| OXAPROZIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72189-077 | TABLET | 600 mg | ORAL | ANDA | 16 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72189-595 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 19 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73308-403 | CAPSULE | 300 mg | ORAL | NDA | 30 sections |
| Oxaprozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 82804-261 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 28 sections |