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fleroxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibacterials, nalidixic acid derivatives | 1177 | 79660-72-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | O |
| 0.40 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.237 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.500 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 13.213 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.155 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 82.150 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 84.330 | % | High | 1 |
| herg | hERG pIC50 | 4.503 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.153 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.373 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 80.140 | % | High | 1 |
| kinase-safety-class | EIF2AK3,GRK2,PDK1,PDK2,PDK4 | 5 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CAMK2D,CDK9,DYRK1B,EIF2AK3,GRK2,MAPK7,PDK4,PIK3CB,PRKDC,SIK2,STK33,TEK,TTK | 16 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 8.810 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.702 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 80.220 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 13.490 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 82.080 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.018 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 89.590 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 61.910 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 853.100 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| ATC | J01MA08 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D059005 | Topoisomerase II Inhibitors |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| CHEBI has role | CHEBI:50750 | EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| CHEBI has role | CHEBI:53559 | topoisomerase IV inhibitor |
Related Drugs by ATC class:
J01MA Fluoroquinolones 22 drugs
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 level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| DNA gyrase subunit A | Enzyme | IC50 | 4.79 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 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