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carprofen 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory agents, ibuprofen derivatives | 518 | 53716-49-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
anti-inflammatory drug (NSAID) of the propionic acid class with selective inhibition of COX-2 versus COX-1
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 0.22 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.51 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) | 9.90 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 90 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.716 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.642 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 112.980 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 15.488 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.360 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.820 | % | High | 1 |
| herg | hERG pIC50 | 4.397 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 7.031 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.105 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.470 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK2,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,KDR,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 | 58 | |||
| kinase-selectivity-class | ACVR2B,AXL,CDK9,DYRK1B,EIF2AK3,MAP2K6,MAPK7,TTK | 8 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 11.641 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 37.757 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.430 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.694 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.250 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 6.934 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 37.010 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.400 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 862.979 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 31, 1987 | FDA | ROCHE |
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 |
|---|---|---|
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D003879 | Dermatologic Agents |
| MeSH PA | D011838 | Radiation-Sensitizing Agents |
| MeSH PA | D017319 | Photosensitizing Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| 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:35544 | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor |
| CHEBI has role | CHEBI:47868 | photosensitizing agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Dogs | Postoperative pain associated with soft tissue and orthopedic surgery | Indication |
| Dogs | Pain and inflammation associated with osteoarthritis | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Rimadyl Sterile Injectable Solution | Zoetis Inc. | 1 |
| Rimadyl Caplets | Zoetis Inc. | 1 |
| Rimadyl Chewable Tablets | Zoetis Inc. | 1 |
| Carprofen Caplets, Novox Caplets | Dechra Veterinary Products LLC | 1 |
| Vetprofen | Belcher Pharmaceuticals Inc. | 1 |
| Carprofen | Dechra Veterinary Products LLC | 1 |
| Carprieve Caplets | Norbrook Laboratories, Ltd. | 1 |
| Carprieve Injection | Norbrook Laboratories, Ltd. | 1 |
| Carprofen Sterile Injectable Solution | Dechra Veterinary Products LLC | 1 |
| quellin | Elanco US Inc. | 1 |
| Carprofen Chewable Tablets | Dechra Veterinary Products LLC | 1 |
| Carprofen Flavored Tablets | Belcher Pharmaceuticals Inc. | 1 |
| Carprofen Injection | Accord Healthcare Inc. | 1 |
| Carprieve Chewable Tablets | Norbrook Laboratories, Ltd. | 1 |
| Carprofen Tablets | Dechra Veterinary Products LLC | 1 |
| Carprofen Chewable Tablets | Cronus Pharma Specialities India Private Limited | 1 |
| Carprofen Tablets | Dechra Veterinary Products LLC | 1 |
| CARPROFEN Chewable Tablets | Felix Pharmaceuticals Pvt. Ltd. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.53 | acidic |
| pKa2 | 11.59 | 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 | 7 | CHEMBL | CHEMBL | |||
| Prostaglandin G/H synthase 1 | Enzyme | IC50 | 4.88 | CHEMBL | |||||
| Complement C5 | Secreted | Kd | 6.24 | CHEMBL | |||||
| Prostaglandin G/H synthase 1 | Enzyme | IC50 | 4.89 | CHEMBL | |||||
| Fatty-acid amide hydrolase 1 | Enzyme | IC50 | 4.10 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D03410 | KEGG_DRUG |
| 20343 | RXNORM |
| C0054827 | UMLSCUI |
| CHEBI:364453 | CHEBI |
| CHEMBL1316 | ChEMBL_ID |
| DB00821 | DRUGBANK_ID |
| C007005 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2581 | PUBCHEM_CID |
| 7141 | IUPHAR_LIGAND_ID |
| 3980 | INN_ID |
| FFL0D546HO | UNII |
| 125710006 | SNOMEDCT_US |
| 424611009 | SNOMEDCT_US |
| 4025237 | VANDF |
| 005102 | NDDF |
Pharmaceutical products:
None