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

Stem definitionDrug idCAS RN
1220 91503-79-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • flurbiprofen axetil
  • ropiopn
an analgesic
  • Molecular weight: 330.36
  • Formula: C19H19FO4
  • CLOGP: 4.33
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 52.60
  • ALOGS: -5.25
  • ROTB: 7
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
CL (Clearance) 0.26 mL/min/kg Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
BA (Bioavailability) 92 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.410 Moderate 0.65
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.579 Moderate 0.65
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 13.868 10^-6 cm/s Moderate 0.65
dh-clint Dog hepatocyte intrinsic clearance 481.948 uL/min/10^6 cells Moderate 0.65
dppb Dog plasma protein binding (% unbound) 0.650 % Moderate 0.65
fcs-ppb Fetal calf serum protein binding (% unbound) 0.680 % Moderate 0.65
herg hERG pIC50 5.058 pIC50 Moderate 0.65
hh-clint Human hepatocyte intrinsic clearance 1348.963 uL/min/10^6 cells Moderate 0.65
hlm-clint Human liver microsomal intrinsic clearance 254.683 uL/min/mg protein Moderate 0.65
hppb Human plasma protein binding (% unbound) 0.640 % Moderate 0.65
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PIK3CG,PRKDC 15
kinase-selectivity-class AXL 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.321 Moderate 0.65
mh-clint Mouse hepatocyte intrinsic clearance 1076.465 Moderate 0.65
mppb Mouse plasma protein binding (% unbound) 1.410 Moderate 0.65
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.286 Moderate 0.65
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 1.530 % Moderate 0.65
rh-clint Rat hepatocyte intrinsic clearance 308.319 uL/min/10^6 cells Moderate 0.65
rh-fuinc Rat hepatocyte fraction unbound in incubation 15.730 % Moderate 0.65
rppb Rat plasma protein binding (% unbound) 1.110 % Moderate 0.65
solubility-dd Solubility at pH 7.4 in DMSO 0.798 uM Moderate 0.65

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hepatic function abnormal 62.25 41.65 18 404 46270 90581755

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hepatic function abnormal 40.37 36.05 16 394 51551 42569374

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hepatic function abnormal 94.57 36.27 34 965 89261 110499039

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 D018373 Peripheral Nervous System Agents
MeSH PA D018501 Antirheumatic Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D016861 Cyclooxygenase Inhibitors
CHEBI has role CHEBI:33282 antibacterial agent
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35481 non-narcotic analgesic
CHEBI has role CHEBI:35493 antipyretic
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35544 EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:66981 ophthalmology drug
CHEBI has role CHEBI:75835 anti-anaemic agent
FDA EPC N0000175722 Nonsteroidal Anti-inflammatory Drug

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

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D01475 KEGG_DRUG
4019154 VANDF
C1610514 UMLSCUI
CHEBI:31627 CHEBI
FLP PDB_CHEM_ID
DB14938 DRUGBANK_ID
C504422 MESH_SUPPLEMENTAL_RECORD_UI
3395 PUBCHEM_CID
I0OU31PUI5 UNII
4502 RXNORM
4753 MMSL
72 MMSL
d00239 MMSL
002382 NDDF
373506008 SNOMEDCT_US
54344006 SNOMEDCT_US
C0016377 UMLSCUI
DB00712 DRUGBANK_ID
3394 PUBCHEM_CID
3220 INN_ID
D005480 MESH_DESCRIPTOR_UI
CHEBI:5130 CHEBI
I0OU31PUI5 INXIGHT DRUGS

Pharmaceutical products:

None