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

Stem definitionDrug idCAS RN
antibiotics, cefalosporanic acid derivatives 557 51762-05-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • CGP-9000
  • CGP 9000
  • cefroxadin
  • cefroxadine
orally active, broad spectrum cephalosporin
  • Molecular weight: 365.40
  • Formula: C16H19N3O5S
  • CLOGP: -1.95
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 3
  • TPSA: 121.96
  • ALOGS: -2.57
  • ROTB: 5

Drug dosage:

DoseUnitRoute
2.10 g O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.17 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4.78 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.10 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.74 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 100 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -1.747 High 0.80
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.199 High 0.80
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.603 10^-6 cm/s High 0.80
dh-clint Dog hepatocyte intrinsic clearance 2.588 uL/min/10^6 cells High 0.80
dppb Dog plasma protein binding (% unbound) 76.180 % High 0.80
fcs-ppb Fetal calf serum protein binding (% unbound) 51.090 % High 0.80
herg hERG pIC50 4.394 pIC50 High 0.80
hh-clint Human hepatocyte intrinsic clearance 1.910 uL/min/10^6 cells High 0.80
hlm-clint Human liver microsomal intrinsic clearance 3.475 uL/min/mg protein High 0.80
hppb Human plasma protein binding (% unbound) 52.010 % High 0.80
kinase-safety-class ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,GSK3B,ITK,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PIK3CA,PIK3CB,PIM2,PRKDC,STK33,SYK,TEK,TGFBR1 31
kinase-selectivity-class AXL,BRAF,CDK9,DYRK1B,EIF2AK3,EPHB4,GRK2,JAK2,MAP2K6,MAP3K14,MAPK7,PRKDC,STK33,SYK,TEK,TGFBR1 16
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.904 High 0.80
mh-clint Mouse hepatocyte intrinsic clearance 2.951 High 0.80
mppb Mouse plasma protein binding (% unbound) 67.530 High 0.80
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 2.239 High 0.80
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 51.610 % High 0.80
rh-clint Rat hepatocyte intrinsic clearance 2.065 uL/min/10^6 cells High 0.80
rh-fuinc Rat hepatocyte fraction unbound in incubation 89.380 % High 0.80
rppb Rat plasma protein binding (% unbound) 53.730 % High 0.80
solubility-dd Solubility at pH 7.4 in DMSO 948.418 uM High 0.80

Approvals:

None

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
ATC J01DB11 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER BETA-LACTAM ANTIBACTERIALS
First-generation cephalosporins
CHEBI has role CHEBI:33282 antibacterial agent

Related Drugs by ATC class:

J01DB First-generation cephalosporins 11 drugs
cefacetrilecefadroxilcefalexincefaloridinecefalotincefapirincefatrizinecefazedonecefazolincefradineceftezole

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 2.42 acidic
pKa2 7.56 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D01528 KEGG_DRUG
C0108941 UMLSCUI
CHEBI:31379 CHEBI
CHEMBL3186538 ChEMBL_ID
DB11367 DRUGBANK_ID
C012671 MESH_SUPPLEMENTAL_RECORD_UI
5284529 PUBCHEM_CID
13619 IUPHAR_LIGAND_ID
4722 INN_ID
B908C4MV2R UNII
010923 NDDF

Pharmaceutical products:

None