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lomefloxacin 🐶 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 | 1594 | 98079-51-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic broad-spectrum fluoroquinolone with antibacterial activity. Lomefloxacin inhibits DNA gyrase, a type II topoisomerase involved in the induction or relaxation of supercoiling during DNA replication. This inhibition leads to a decrease in DNA synthesis during bacterial replication, resulting in cell growth inhibition and eventually cell lysis.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 1.64 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 65 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 16.26 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 97 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 2.04 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3.98 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 8.10 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 | -0.430 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.928 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 5.610 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.355 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 77.370 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 82.950 | % | High | 1 |
| herg | hERG pIC50 | 4.637 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.102 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.357 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 80.220 | % | High | 1 |
| kinase-safety-class | GRK2,PDK1,PDK2,PDK4 | 4 | |||
| kinase-selectivity-class | AXL,CAMK2D,CDK9,DYRK1B,EIF2AK3,GRK2,MAPK7,PDK4,PRKDC,STK33,TEK,TTK | 12 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 9.183 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.236 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 79.590 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 14.825 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 81.040 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.365 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 87.400 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 62.080 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 853.100 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 21, 1992 | FDA |
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 | J01MA07 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones |
| ATC | J04AM09 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF TUBERCULOSIS Combinations of drugs for treatment of tuberculosis |
| ATC | J04AM10 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF TUBERCULOSIS Combinations of drugs for treatment of tuberculosis |
| ATC | S01AE04 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Fluoroquinolones |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D059003 | Topoisomerase Inhibitors |
| MeSH PA | D059005 | Topoisomerase II Inhibitors |
| CHEBI has role | CHEBI:33231 | antitubercular agent |
| CHEBI has role | CHEBI:33281 | antimicrobial agent |
| CHEBI has role | CHEBI:47868 | photosensitizing agent |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
Related Drugs by ATC class:
J01MA Fluoroquinolones 22 drugs
J04AM Combinations of drugs for treatment of tuberculosis 11 drugs
S01AE Fluoroquinolones 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Bronchitis | indication | 32398004 | DOID:6132 |
| Lower respiratory tract infection | indication | 50417007 | |
| Klebsiella cystitis | indication | 60867007 | |
| Urinary tract infectious disease | indication | 68566005 | |
| Acute bacterial bronchitis | indication | 233598009 | |
| Escherichia coli urinary tract infection | indication | 301011002 | |
| Acute exacerbation of chronic bronchitis | indication | 425748003 | |
| Urinary tract infection caused by Klebsiella | indication | 369001000119100 | |
| Proteus Cystitis | indication | ||
| Moraxella Catarrhalis Chronic Bronchitis | indication | ||
| Staphylococcus Cystitis | indication | ||
| Prevention of Infection in Transrectal Prostate Biopsy | indication | ||
| Haemophilus Influenzae Chronic Bronchitis | indication | ||
| Complicated Proteus UTI | indication | ||
| E. Coli Cystitis | indication | ||
| Complicated UTI with Pseudomonas Aeruginosa | indication | ||
| Prevention of Infection from Transurethral Surgery | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.84 | acidic |
| pKa2 | 8.18 | 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 | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| DNA gyrase subunit A | Enzyme | IC50 | 5.15 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4020246 | VUID |
| N0000148144 | NUI |
| D00873 | KEGG_DRUG |
| 98079-52-8 | SECONDARY_CAS_RN |
| 4020246 | VANDF |
| 4020537 | VANDF |
| CHEBI:116278 | CHEBI |
| CHEMBL561 | ChEMBL_ID |
| CHEMBL1728 | ChEMBL_ID |
| C053091 | MESH_SUPPLEMENTAL_RECORD_UI |
| 12407 | IUPHAR_LIGAND_ID |
| DB00978 | DRUGBANK_ID |
| L6BR2WJD8V | UNII |
| 235762 | RXNORM |
| 4990 | MMSL |
| d00104 | MMSL |
| 003642 | NDDF |
| 003643 | NDDF |
| 387553002 | SNOMEDCT_US |
| 412239000 | SNOMEDCT_US |
| 96088001 | SNOMEDCT_US |
| C0065162 | UMLSCUI |
| 6222 | INN_ID |
| 3948 | PUBCHEM_CID |
Pharmaceutical products:
None