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Besifloxacin Ophthalmic Suspension 0.6%

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Abstract

Besifloxacin is a novel fluoroquinolone that, like other fluoroquinolones, acts by inhibiting the essential bacterial enzymes DNA gyrase and topoisomerase IV. Topical besifloxacin ophthalmic suspension 0.6% is indicated for use in patients with bacterial conjunctivitis caused by susceptible bacteria.

Besifloxacin had in vitro activity against a broad spectrum of Gram-positive and -negative bacteria that commonly cause ocular infections (e.g. Haemophilus influenzae, Staphylococcus aureus, S. epidermidis and Streptococcus pneumoniae), including drug-resistant strains.

In two randomized, double-blind, multicentre trials, besifloxacin ophthalmic suspension 0.6% administered at the recommended dose for 5 days in patients aged ≥1 year with bacterial conjunctivitis was significantly (p<0.01) more effective than vehicle in terms of clinical resolution and microbial eradication rates (coprimary endpoints) at study visit two (day 5±1) or three (day 8 or 9) [primary timepoints].

Besifloxacin ophthalmic suspension 0.6% was noninferior to moxifloxacin ophthalmic solution 0.5% in patients aged ≥1 year with bacterial conjunctivitis with regard to clinical resolution (58.3% vs 59.4%) and microbial eradication (93.3% vs 91.1%) rates on day 5±1 of treatment (coprimary endpoints) in a randomized, double-blind, multicentre trial; both drugs were administered at a dosage of one drop in the affected eye(s) three times daily for 5 days.

Besifloxacin ophthalmic suspension 0.6% was generally well tolerated in clinical trials, with most adverse events being mild in severity. The tolerability profile of besifloxacin ophthalmic suspension 0.6% was similar to that of moxifloxacin ophthalmic solution 0.5%.

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References

  1. Høvding G. Acute bacterial conjunctivitis. Acta Ophthalmol 2008 Feb; 86(1): 5–17

    Article  PubMed  Google Scholar 

  2. Tarabishy AB, Jeng BH. Bacterial conjunctivitis: a review for internists. Cleve Clin J Med 2008 Jul; 75(7): 507–12

    Article  PubMed  Google Scholar 

  3. Hwang DG. Fluoroquinolone resistance in ophthalmology and the potential role for newer ophthalmic fluoroquinolones. Surv Ophthalmol 2004 Mar; 49 (2 Suppl. 2): S79–83

    Article  PubMed  Google Scholar 

  4. Tepedino ME, Heller WH, Usner DW, et al. Phase III efficacy and safety study of besifloxacin ophthalmic suspension 0.6% in the treatment of bacterial conjunctivitis. Curr Med Res Opin 2009 May; 25(5): 1159–69

    Article  PubMed  CAS  Google Scholar 

  5. Bausch & Lomb Incorporated. Besivance™ (besifloxacin ophthalmic suspension) 0.6%: highlights of US prescribing information [online]. Available from URL: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022308lbl.pdf [Accessed 2009 Nov 30]

  6. Bausch & Lomb Incorporated. Besifloxacin ophthalmic suspension 0.6% (Besivance): Canadian Product Monograph. Vaughan (ON): Bausch & Lomb Incorporated, 2009 Oct 23

  7. Proksch JW, Granvil CP, Siou-Mermet R, et al. Ocular pharmacokinetics of besifloxacin following topical administration to rabbits, monkeys, and humans. J Ocul Pharmacol Ther 2009; 25(4): 1–9

    Article  Google Scholar 

  8. Cambau E, Matrat S, Pan X-S, et al. Target specificity of the new fluoroquinolone besifloxacin in Streptococcus pneumoniae, Staphylococcus aureus and Escherichia coli. J Antimicrob Chemother 2009 Mar; 63(3): 443–50

    Article  PubMed  CAS  Google Scholar 

  9. Ward KW, Lepage J-F, Driot J-Y. Nonclinical pharmacodynamics, pharmacokinetics, and safety of BOL-303224-A, a novel fluoroquinolone antimicrobial agent for topical ophthalmic use. J Ocul Pharmacol Ther 2007 Jun; 23(3): 243–56

    Article  PubMed  CAS  Google Scholar 

  10. Haas W, Pillar CM, Zurenko GE, et al. Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria. Antimicrob Agents Chemother 2009 Aug; 53(8): 3552–60

    Article  PubMed  CAS  Google Scholar 

  11. Haas W, Brunner LS, Pillar C, et al. Bactericidal activity of besifloxacin and other ophthalmic antibacterials against recent ocular isolates [poster no. 2675]. Annual Meeting of the Association for Research in Vision and Ophthalmology; 2009 May 3–7; Fort Lauderdale (FL)

  12. Proksch JW, Chappa AK, Haas W, et al. Besifloxacin, moxifloxacin, and gatifloxacin ocular tissue AUC/MIC ratios for fluoroquinolone-resistant organisms [poster no. 0905]. Annual Meeting of the Association for Research in Vision and Ophthalmology; 2009 May 3–7; Fort Lauderdale (FL)

  13. Haas W, Zurenko GE, Lee J, et al. Activity of besifloxacin and comparators against ciprofloxacin resistant Staphylococcus aureus and Staphylococcus epidermidis ocular isolates from 2005–2008 [poster]. 3rd Congress of the Federation of European Microbiologists; 2009 Jun 28–Jul 2; Gothenberg

  14. Brunner LS, Norton SE, Blondeau JM. In vitro activity of SS734, a novel fluoroquinolone, against pathogens associated with bacterial conjunctivitis [poster no. P1679]. 17th European Congress of Clinical Microbiology and Infectious Diseases and 25th International Congress of Chemotherapy and Infectious Diseases; 2007 Mar 31–Apr 3; Munich

  15. McDonald MB, Blondeau JM, DeCory HH, et al. Multidrug-resistant strains in clinical trials of besifloxacin in the treatment of bacterial conjunctivitis [poster no. PO070]. Annual Meeting of the American Academy of Ophthalmology; 2008 Nov 8–11; Atlanta (GA)

  16. Brunner LS, Walsh PA, Norton SE, et al. Bactericidal activity of SS734, a novel fluoroquinolone, against pathogens associated with bacterial conjunctivitis [poster no. P1680]. 17th European Congress of Clinical Microbiology and Infectious Diseases and 25th International Congress of Chemotherapy and Infectious Diseases; 2007 Mar 31–Apr 3; Munich

  17. Blondeau JM, Brunner L, Norton S. In vitro activity against Gram-negative pathogens of SS734: a new fluoroquinolone (FQ) for the treatment of bacterial conjunctivitis (BC). 46th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2006 Sep 27–30; San Francisco (CA)

  18. Morris TW, Haas W, Brunner LS, et al. Clinical efficacy of besifloxacin ophthalmic suspension; integrated microbiological analysis of 3 trials for topical treatment of bacterial conjunctivitis [poster no. 5945]. Annual Meeting of the Association for Research in Vision and Ophthalmology; 2009 May 3–7; Fort Lauderdale (FL)

  19. Center for Drug Evaluation and Research. Besifloxacin: microbiology review(s) [online]. Available from URL: http://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022308s000_MicroR.pdf [Accessed 2009 Nov 30]

  20. Clinical and Laboratory Standards Institute. Methods for dilution antimicrobial susceptiblity tests for bacteria that grow aerobically; approved standard, eighth edition (document M07-A8). Wayne (PA): Clinical and Laboratory Standards Institute, 2008 Dec 30

    Google Scholar 

  21. 21. Clinical and Laboratory Standards Institute. Performance standards for antimicrobial susceptiblity testing; nineteenth informational supplement (document M100-S19). Wayne (PA): Clinical and Laboratory Standards Institute, 2009; 28(1)

    Google Scholar 

  22. Zhang J-Z, Ward KW. Besifloxacin, a novel fluoroquinolone antimicrobial agent, exhibits potent inhibition of pro-inflammatory cytokines in human THP-1 monocytes. J Antimicrob Chemother 2008 Jan; 61(1): 111–6

    Article  Google Scholar 

  23. Zhang J-Z, Cavet ME, Ward KW. Anti-inflammatory effects of besifloxacin, a novel fluoroquinolone, in primary human corneal epithelial cells. Curr Eye Res 2008 Nov; 33(11): 923–32

    Article  Google Scholar 

  24. McDonald MB, Protzko EE, Brunner LS, et al. Efficacy and safety of besifloxacin ophthalmic suspension 0.6% compared with moxifloxacin ophthalmic solution 0.5% for treating bacterial conjunctivitis. Ophthalmology 2009 Sep; 116(9): 1615–23

    Article  PubMed  Google Scholar 

  25. Karpecki P, DePaolis M, Hunter JA, et al. Besifloxacin ophthalmic suspension 0.6% in patients with bacterial conjunctivitis: a multicenter, prospective, randomized, double-masked, vehicle-controlled, 5-day efficacy and safety study. Clin Ther 2009 Mar; 31(3): 514–26

    Article  PubMed  CAS  Google Scholar 

  26. Comstock TL, Paterno MR, Lynch JA, et al. Efficacy and safety of besifloxacin ophthalmic suspension, 0.6% in pediatric patients with bacterial conjunctivitis [poster no. 2667]. Annual Meeting of the Association for Research in Vision and Ophthalmology; 2009 May 3–7; Fort Lauderdale (FL)

  27. McDonnell G, Russell AD. Antiseptics and disinfectants: activity, action, and resistance. Clin Microbiol Rev 1999 Jan; 12(1): 147–79

    PubMed  CAS  Google Scholar 

  28. Blondeau JM, Borsos S, Hesje CK. Antimicrobial efficacy of gatifloxacin and moxifloxacin with and without benzalkonium chloride compared with ciprofloxacin and levofloxacin against methicillin-resistant Staphylococcus aureus. J Chemother 2007; 19(2): 146–51

    PubMed  CAS  Google Scholar 

  29. Hesje CK, Borsos SD, Blondeau JM. Benzalkonium chloride enhances antibacterial activity of gatifloxacin and reduces its propensity to select for fluoroquinolone-resistant strains. J Ocul Pharmacol Ther 2009; 25(4): 329–33

    Article  PubMed  CAS  Google Scholar 

  30. Paterno MR, Comstock TL, Lynch JA, et al. Besifloxacin ophthalmic suspension, 0.6% is safe and well tolerated in the treatment of bacterial conjunctivitis [poster no. 2674]. Annual Meeting of the Association for Research in Vision and Ophthalmology; 2009 May 3–7; Fort Lauderdale (FL)

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Acknowledgements and Disclosures

The manuscript was reviewed by: M.B. Abelson, Ora Inc., Ophthalmic Research Associates, North Andover, Massachusetts, USA; J.S. Bertino Jr, Bertino Consulting, Schenectady, New York, USA; J.M. Blondeau, Department of Clinical Microbiology, Royal University Hospital, Saskatoon, Saskatchewan, Canada.

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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  1. Adis, a Wolters Kluwer Business, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore 0754, Auckland, New Zealand

    Natalie J. Carter & Lesley J. Scott

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  1. Natalie J. Carter
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  2. Lesley J. Scott
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Correspondence to Natalie J. Carter.

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Carter, N.J., Scott, L.J. Besifloxacin Ophthalmic Suspension 0.6%. Drugs 70, 83–97 (2010). https://doi.org/10.2165/11203820-000000000-00000

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