DB06771 - Besifloxacin
| Identification | |
|---|---|
| Name | Besifloxacin |
| Accession Number | DB06771 |
| Type | small molecule |
| Description | Besifloxacin is a fourth generation fluoroquinolone-type opthalmic antibiotic for the treatment of bacterial conjunctivitis. FDA approved on May 28, 2009. |
| Structure |
|
| Categories (*) | |
| Molecular Weight | 393.84 |
| Groups | approved |
| Monoisotopic Weight | 393.125547465 |
| Pharmacology | |
| Indication | Treatment of bacterial conjunctivitis. Bacterial isolates that are susceptible to besifloxacin include: CDC coryneform group G; Corynebacterium pseudodiphtheriticum; Corynebacterium striatum; Haemophilus influenzae; Moraxella lacunata; Staphylococcus aureus; Staphylococcus epidermidis; Staphylococcus hominis; Staphylococcus lugdunensis; Streptococcus mitis group; Streptococcus oralis; Streptococcus pneumoniae; Streptococcus salivarius* |
| Mechanism of action | Besifloxacin is a bactericidal fluroquinolone-type antibiotic that inhibits bacterial enzymes, DNA gyrase and topoisomerase IV. By inhibiting DNA gyrase, DNA replication, transcription, and repair is impaired. By inhibiting topoisomerase IV, decatenation during cell devision is impaired. Inhibiting these two targets also slows down development of resistance. |
| Absorption | Although ocular surface concentrations are high, average systemic concentrtions after three-times daily dosing was less than 0.5 ng/mL. This indicates that besifloxacin is not appreciably absorbed into the systemic and has a very low risk of systemic side effects. |
| Protein binding | None |
| Biotransformation | No appreciable metabolism |
| Route of elimination | N/A |
| Toxicity | LD50, rat: >2000 mg/kg. The most common adverse reaction reported in 2% of patients treated with besifloxacin was conjunctival redness. |
| Affected organisms |
|
| Interactions | |
| Drug Interactions | Not Available |
| Food Interactions | Not Available |
Targets
| DNA topoisomerase 4 subunit A | |
|---|---|
| Name | DNA topoisomerase 4 subunit A |
| Gene Name | parC |
| Pharmacological action | yes |
| Actions | antagonist |
| References |
|
| DTHybrid score | 1.0063 |
| DNA topoisomerase 4 subunit A | |
| Name | DNA topoisomerase 4 subunit A |
| Gene Name | parC |
| Pharmacological action | yes |
| Actions | antagonist |
| References |
|
| DTHybrid score | 1.0063 |
| DNA gyrase subunit A | |
| Name | DNA gyrase subunit A |
| Gene Name | gyrA |
| Pharmacological action | yes |
| Actions | antagonist |
| References |
|
| DTHybrid score | 1.0386 |
| DNA gyrase subunit A | |
| Name | DNA gyrase subunit A |
| Gene Name | gyrA |
| Pharmacological action | yes |
| Actions | antagonist |
| References |
|
| DTHybrid score | 1.0386 |
Predictions
| Id | Partner name | Gene Name | Score |
|---|---|---|---|
| 886 | DNA topoisomerase 4 subunit A | parC | 1.0063 |
| 5645 | DNA topoisomerase 4 subunit B | parE | 0.3754 |
| 6227 | DNA topoisomerase 4 subunit B | parE | 0.3754 |
| 887 | DNA gyrase subunit B | gyrB | 0.3754 |
| 4150 | DNA gyrase subunit B | gyrB | 0.3754 |
| 6225 | DNA gyrase subunit B | gyrB | 0.3754 |
| 817 | DNA topoisomerase 2-alpha | TOP2A | 0.3509 |
| 4200 | Cytochrome P450 1A2 | CYP1A2 | 0.1333 |
| 587 | Serum albumin | ALB | 0.1007 |
| 118 | Organic cation/carnitine transporter 2 | SLC22A5 | 0.0738 |
| 1729 | Solute carrier family 22 member 6 | SLC22A6 | 0.0655 |
| 1735 | Canalicular multispecific organic anion transporter 1 | ABCC2 | 0.0584 |
| 1588 | Multidrug resistance protein 1 | ABCB1 | 0.0411 |
| 4512 | Cytochrome P450 3A4 | CYP3A4 | 0.0309 |
| 833 | Organic cation/carnitine transporter 1 | SLC22A4 | 0.0292 |
| 862 | Multidrug resistance-associated protein 1 | ABCC1 | 0.024 |
| 6144 | Solute carrier family 22 member 2 | SLC22A2 | 0.0239 |
| 6107 | Cytochrome P450 3A7 | CYP3A7 | 0.021 |
| 4118 | Cytochrome P450 3A5 | CYP3A5 | 0.0197 |
| 5718 | Cytochrome P450 2A6 | CYP2A6 | 0.0098 |
| 6024 | Cytochrome P450 1A1 | CYP1A1 | 0.0094 |