fleroxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 |
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 |
| 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
🐶 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