Besifloxacin: a topical fluoroquinolone for the treatment of bacterial conjunctivitis.

Abstract

BACKGROUND:

Besifloxacin is a topical ophthalmic fluoroquinolone that was approved by the US Food and Drug Administration (FDA) in May 2009 for the treatment of bacterial conjunctivitis caused by susceptible bacterial strains.

OBJECTIVE:

This article provides an overview of the pharmacology, clinical efficacy, and tolerability of ophthalmic besifloxacin when used for the treatment of bacterial conjunctivitis.

METHODS:

Relevant reports pertaining to the pharmacology, efficacy, and tolerability of besifloxacin were identified through a search of MEDLINE (1985-December 2009) and International Pharmaceutical Abstracts (1985-December 2009) using the terms besifloxacin, BOL-303224-A, ophthalmic fluoroquinolones, and bacterial conjunctivitis. Additional publications were identified by reviewing the reference lists of identified articles and searching the FDA Web site.

RESULTS:

Besifloxacin has potent in vitro inhibitory activity against most common ocular bacterial pathogens (MIC90 values generally < or =4 microg/mL), including Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae. In an ocular pharmacokinetic study in 64 healthy volunteers, the C(max) in tears (mean [SD], 610 [540] microg/mL) was reached 10 minutes after a single ocular instillation of besifloxacin; concentrations > or =1.6 microg/g of tear were sustained for at least 24 hours; and the elimination t(1/2) was ~3.4 hours. In a study in 24 patients with a clinical diagnosis of bilateral bacterial conjunctivitis, systemic exposure (C(max)) after administration of besifloxacin ophthalmic suspension 3 times daily for 5 days was <0.5 ng/mL. In 2 randomized, double-masked, vehicle-controlled clinical trials, besifloxacin ophthalmic suspension was well tolerated and significantly more efficacious than vehicle in achieving clinical resolution (73.3% vs 43.1%, respectively, in one of the studies [P < 0.001]; 45.2% vs 33.0% in the other [P = 0.008]) and microbial eradication (88.3% vs 60.3% [P < 0.001] and 91.5% vs 59.7% [P < 0.001], respectively). In a randomized, double-masked, parallel-group, noninferiority trial comparing besifloxacin ophthalmic suspension 0.6% with moxifloxacin ophthalmic solution 0.5%, besifloxacin was found to be noninferior to moxifloxacin (predefined cutoff for noninferiority = -15), with no significant differences in rates of clinical resolution (58.3% and 59.4%, respectively; 95% CI, -9.48 to 7.29) or microbial eradication (93.3% and 91.1%; 95% CI, -2.44 to 6.74). Besifloxacin was generally well tolerated in these clinical trials, with the most common (> or =1.5%) ocular adverse events being nonspecific conjunctivitis (2.6%), blurred vision (2.1%), bacterial conjunctivitis (1.8%), and eye pain (1.5%). The recommended dose of besifloxacin is 1 drop in the affected eye(s) 3 times daily (4-12 hours apart) for 7 days.

CONCLUSION:

Besifloxacin ophthalmic suspension 0.6% appeared to be well tolerated in the populations studied and was efficacious in the treatment of bacterial conjunctivitis caused by susceptible isolates.

• Authors: Mei H Chang, Horatio B Fung
• Journal: Clinical therapeutics (Clin Ther) Vol. 32 Issue 3 Pg. 454-71 (Mar 2010) ISSN: 1879-114X [Electronic] United States
• PMID: 20399984 (Publication Type: Journal Article, Review)
• Copyright: Copyright 2010 Excerpta Medica Inc. All rights reserved.

Chemical References

• Anti-Bacterial Agents
• Azepines
• Fluoroquinolones
• Ophthalmic Solutions
• besifloxacin

Topics

• Administration, Topical
• Animals
• Anti-Bacterial Agents (administration & dosage, adverse effects, therapeutic use)
• Azepines (administration & dosage, adverse effects, therapeutic use)
• Clinical Trials as Topic
• Conjunctivitis, Bacterial (drug therapy, microbiology)
• Fluoroquinolones (administration & dosage, adverse effects, therapeutic use)
• Humans
• Microbial Sensitivity Tests
• Ophthalmic Solutions
• Treatment Outcome