Besifloxacin, a new ophthalmic fluoroquinolone for the treatment of bacterial conjunctivitis.
Besifloxacin is a new fluoroquinolone anti-infective developed for ophthalmic use. Besifloxacin ophthalmic suspension 0.6% (Besivance) was recently approved for the treatment of bacterial conjunctivitis. The objective of this article is to provide a comprehensive overview of microbiological, pharmacokinetic/pharmacodynamic and clinical studies with besifloxacin. Microbiological studies have demonstrated that besifloxacin has wide-spectrum and potent activity against common ocular pathogens, including Gram-negative and Gram-positive pathogens associated with bacterial conjunctivitis, and retained activity against fluoroquinolone-resistant staphylococci and multidrug-resistant strains. In preclinical and human studies, topically applied besifloxacin had a prolonged ocular concentration and minimal systemic exposure. In clinical studies, patients randomized to besifloxacin ophthalmic suspension 0.6% experienced significantly higher rates of clinical resolution and microbial eradication than patients randomized to vehicle. Besifloxacin ophthalmic suspension 0.6% was also found to be as effective and well tolerated as moxifloxacin ophthalmic solution 0.5%. The low minimum inhibitory concentrations and high attainment of pharmacodynamic targets with besifloxacin may contribute to a lower risk for the emergence of bacterial resistance, although further studies are needed. These data indicate that besifloxacin ophthalmic suspension 0.6% is an important new option for the treatment of bacterial conjunctivitis.
Bertino
Joseph S
JS
Pharmacology College of Physicians and Surgeons, Columbia University, New York, NY 10032, USA. sbertino@ix.netcom.com
Zhang
Jin-Zhong
JZ
D000287:Administration, Topical; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D001372:Aza Compounds / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use; D001381:Azepines / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D003234:Conjunctivitis, Bacterial / Q000188:drug therapy* / Q000382:microbiology; D024881:Drug Resistance, Bacterial; D024841:Fluoroquinolones / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D008826:Microbial Sensitivity Tests; D000077266:Moxifloxacin; D009883:Ophthalmic Solutions; D011804:Quinolines / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use
D000900:Anti-Bacterial Agents; D001372:Aza Compounds; D001381:Azepines; D024841:Fluoroquinolones; D009883:Ophthalmic Solutions; D011804:Quinolines; C522124:besifloxacin; D000077266:Moxifloxacin