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

Stem definitionDrug idCAS RN
antibacterials, nalidixic acid derivatives 2070 127045-41-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pazufloxacin mesilate
  • pazufloxacin mesylate
  • pazufloxacin
  • Molecular weight: 318.30
  • Formula: C16H15FN2O4
  • CLOGP: -1.19
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 92.86
  • ALOGS: -2.12
  • ROTB: 2

Drug dosage:

DoseUnitRoute
1 g P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.68 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4.87 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.79 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.10 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.732 Moderate 0.66
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.158 Moderate 0.66
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 3.412 10^-6 cm/s Moderate 0.66
dh-clint Dog hepatocyte intrinsic clearance 1.089 uL/min/10^6 cells Moderate 0.66
dppb Dog plasma protein binding (% unbound) 80.140 % Moderate 0.66
fcs-ppb Fetal calf serum protein binding (% unbound) 79.210 % Moderate 0.66
herg hERG pIC50 4.364 pIC50 Moderate 0.66
hh-clint Human hepatocyte intrinsic clearance 1.156 uL/min/10^6 cells Moderate 0.66
hlm-clint Human liver microsomal intrinsic clearance 3.126 uL/min/mg protein Moderate 0.66
hppb Human plasma protein binding (% unbound) 77.810 % Moderate 0.66
kinase-safety-class ACVR2B,EIF2AK3,GRK2,PDK1,PDK2,PDK4,PRKDC 7
kinase-selectivity-class AXL,CDK9,DYRK1B,EIF2AK3,GRK2,MAP2K6,MAPK7,PDK4,PIK3CD,PRKDC,STK33,SYK,TGFBR1,TTK 14
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 8.110 Moderate 0.66
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 5.200 Moderate 0.66
mh-clint Mouse hepatocyte intrinsic clearance 3.034 Moderate 0.66
mppb Mouse plasma protein binding (% unbound) 73.590 Moderate 0.66
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 10.233 Moderate 0.66
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 82.420 % Moderate 0.66
rat-kpuu-brain Rat brain Kpuu 0.119 % Moderate 0.66
rh-clint Rat hepatocyte intrinsic clearance 1.156 uL/min/10^6 cells Moderate 0.66
rh-fuinc Rat hepatocyte fraction unbound in incubation 86.910 % Moderate 0.66
rppb Rat plasma protein binding (% unbound) 65.790 % Moderate 0.66
solubility-dd Solubility at pH 7.4 in DMSO 899.498 uM Moderate 0.66

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 J01MA18 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
QUINOLONE ANTIBACTERIALS
Fluoroquinolones
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000995 Antitubercular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D059003 Topoisomerase Inhibitors
MeSH PA D059005 Topoisomerase II Inhibitors

Related Drugs by ATC class:

J01MA Fluoroquinolones 22 drugs
ciprofloxacindelafloxacinenoxacinfleroxacingarenoxacingatifloxacingemifloxacingrepafloxacinlascufloxacinlevofloxacinlomefloxacinmoxifloxacin show all 22 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Sepsis due to Streptococcus pneumoniae indication 448421008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.12 acidic
pKa2 7.56 Basic
pKa3 0.78 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D01153 KEGG_DRUG
163680-77-1 SECONDARY_CAS_RN
C0175022 UMLSCUI
CHEBI:31964 CHEBI
CHEMBL240163 ChEMBL_ID
DB11774 DRUGBANK_ID
C078052 MESH_SUPPLEMENTAL_RECORD_UI
65957 PUBCHEM_CID
12410 IUPHAR_LIGAND_ID
7247 INN_ID
4CZ1R38NDI UNII

Pharmaceutical products:

None