fleroxacin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antibacterials, nalidixic acid derivatives 1177 79660-72-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fleroxacin
  • flerofloxacin
  • megalocin
  • megalone
  • quinodis
A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.
  • Molecular weight: 369.34
  • Formula: C17H18F3N3O3
  • CLOGP: -0.08
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 64.09
  • ALOGS: -3.11
  • ROTB: 4

Drug dosage:

DoseUnitRoute
0.40 g O
0.40 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.87 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 72.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.47 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.73 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 8.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1992 YEAR INTRODUCED

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 J01MA08 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
QUINOLONE ANTIBACTERIALS
Fluoroquinolones
CHEBI has role CHEBI:36047 antibacterial drugs
CHEBI has role CHEBI:50750 inhibitors of type II topoisomerase
CHEBI has role CHEBI:53559 topoisomerase IV inhibitors
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D059005 Topoisomerase II Inhibitors
MeSH PA D059003 Topoisomerase Inhibitors

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

None




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.47 acidic
pKa2 8.04 Basic

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
DNA gyrase subunit A Enzyme IC50 4.79 WOMBAT-PK

External reference:

IDSource
N0000166916 NUI
D01716 KEGG_DRUG
C0085161 UMLSCUI
CHEBI:31810 CHEBI
CHEMBL6273 ChEMBL_ID
DB04576 DRUGBANK_ID
D016576 MESH_DESCRIPTOR_UI
3357 PUBCHEM_CID
12476 IUPHAR_LIGAND_ID
5966 INN_ID
N804LDH51K UNII
42322 RXNORM
006886 NDDF
702750000 SNOMEDCT_US
96085003 SNOMEDCT_US

Pharmaceutical products:

None