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

Stem definitionDrug idCAS RN
prednisone and prednisolone derivatives 1216 53-34-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fluprednisolone
  • alphadrol
  • etadrol
A synthetic glucocorticoid with anti-inflammatory properties.
  • Molecular weight: 378.44
  • Formula: C21H27FO5
  • CLOGP: 1.47
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 3
  • TPSA: 94.83
  • ALOGS: -3.16
  • ROTB: 2
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.719 High 0.80
caco2-efflux Caco-2 efflux ratio (BA/AB) 5.585 High 0.80
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 26.977 10^-6 cm/s High 0.80
dh-clint Dog hepatocyte intrinsic clearance 5.176 uL/min/10^6 cells High 0.80
dppb Dog plasma protein binding (% unbound) 37.170 % High 0.80
fcs-ppb Fetal calf serum protein binding (% unbound) 53.280 % High 0.80
herg hERG pIC50 4.412 pIC50 High 0.80
hh-clint Human hepatocyte intrinsic clearance 3.540 uL/min/10^6 cells High 0.80
hlm-clint Human liver microsomal intrinsic clearance 11.749 uL/min/mg protein High 0.80
hppb Human plasma protein binding (% unbound) 27.270 % High 0.80
kinase-safety-class ACVR2B,CDK5,EIF2AK3,GRK2,ITK,MAPK10,PDK1,PDK2,PDK4,PRKDC 10
kinase-selectivity-class GRK2,MAP2K6 2
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 7.362 Moderate 0.67
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 10.965 High 0.80
mh-clint Mouse hepatocyte intrinsic clearance 29.107 High 0.80
mppb Mouse plasma protein binding (% unbound) 38.910 High 0.80
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 22.856 High 0.80
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 Moderate 0.67
pppb Pig plasma protein binding (% unbound) 44.440 % High 0.80
rat-kpuu-brain Rat brain Kpuu 0.044 % Moderate 0.67
rh-clint Rat hepatocyte intrinsic clearance 44.978 uL/min/10^6 cells High 0.80
rh-fuinc Rat hepatocyte fraction unbound in incubation 81.570 % High 0.80
rppb Rat plasma protein binding (% unbound) 23.280 % High 0.80
solubility-dd Solubility at pH 7.4 in DMSO 391.742 uM High 0.80

Approvals:

DateAgencyCompanyOrphan
Dec. 7, 1982 FDA PHARMACIA AND UPJOHN

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 D000893 Anti-Inflammatory Agents
MeSH PA D005938 Glucocorticoids
MeSH PA D006728 Hormones

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 levelDissociation constantType (acidic/basic)
pKa1 12.18 acidic
pKa2 12.91 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
Glucocorticoid receptor Nuclear hormone receptor AGONIST CHEMBL CHEMBL

External reference:

IDSource
N0000167459 NUI
D04227 KEGG_DRUG
C0016369 UMLSCUI
CHEBI:34474 CHEBI
CHEMBL1200774 ChEMBL_ID
DB09378 DRUGBANK_ID
D005477 MESH_DESCRIPTOR_UI
5876 PUBCHEM_CID
1352 INN_ID
9H05937G3X UNII
4497 RXNORM
002163 NDDF
116599004 SNOMEDCT_US
4126008 SNOMEDCT_US
9H05937G3X INXIGHT DRUGS

Pharmaceutical products:

None