carprofen 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
anti-inflammatory agents, ibuprofen derivatives 518 53716-49-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Ro 205720
  • Ro-205720
  • rimadyl
  • carprofen
  • carprodyl
anti-inflammatory drug (NSAID) of the propionic acid class with selective inhibition of COX-2 versus COX-1
  • Molecular weight: 273.72
  • Formula: C15H12ClNO2
  • CLOGP: 3.98
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 2
  • TPSA: 53.09
  • ALOGS: -4.86
  • ROTB: 2
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
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):

PropertyDescriptionValueUnitConfidenceSimilarity
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:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
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

SpeciesUseRelation
Dogs Postoperative pain associated with soft tissue and orthopedic surgery Indication
Dogs Pain and inflammation associated with osteoarthritis Indication

🐶 Veterinary products

ProductApplicantIngredients
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA 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:

IDSource
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