Besifloxacin

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Besifloxacin
Clinical data
Trade namesBesivance
AHFS/Drugs.comMonograph
MedlinePlusa610011
License data
Routes of
administration		Ophthalmic
ATC code
Legal status
Legal status
Identifiers
  • 7-[(3R)-3-Aminoazepam-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
JSmol)
  • Fc1c(c(Cl)c2c(c1)C(=O)C(\C(=O)O)=C/N2C3CC3)N4CCCC[C@@H](N)C4
  • InChI=1S/C19H21ClFN3O3/c20-15-16-12(18(25)13(19(26)27)9-24(16)11-4-5-11)7-14(21)17(15)23-6-2-1-3-10(22)8-23/h7,9-11H,1-6,8,22H2,(H,26,27)/t10-/m1/s1
  • Key:QFFGVLORLPOAEC-SNVBAGLBSA-N

Besifloxacin (

fluoroquinolone antibiotic. The marketed compound is besifloxacin hydrochloride
. It was developed by SSP Co. Ltd., Japan, and designated SS734. SSP licensed U.S. and European rights to SS734 for ophthalmic use to InSite Vision Incorporated (OTC Pink: INSV) in 2000. InSite Vision developed an eye drop formulation (ISV-403) and conducted preliminary clinical trials before selling the product and all rights to Bausch & Lomb in 2003.[1]

The eye drop was approved by the United States Food and Drug Administration (FDA) on May 29, 2009, and marketed under the trade name Besivance.[2]

Pharmacodynamics

Besifloxacin is a

Gram-negative ocular pathogens: e.g., Corynebacterium pseudodiphtheriticum, Moraxella lacunata, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus hominis, Streptococcus mitis, Streptococcus oralis, Streptococcus pneumoniae and Streptococcus salivarius
. Besifloxacin has been found to inhibit production of pro-inflammatory cytokines in vitro.[3] The mechanism of action of besifloxacin involves inhibition of two enzymes which are essential for the synthesis and replication of bacterial DNA: the bacterial DNA gyrase and topoisomerase IV. Clinical trials indicated that Besifloxacin was 91% effective at eliminating the causative bacteria after five days, compared to 60% in the placebo group. This did not, however necessarily correlate with condition resolution, as bacterial presence is only a part of conjunctivitis.[4]

Medical use

Besifloxacin is indicated in the treatment of bacterial conjunctivitis caused by sensitive bacteria,[5] as well as in the prevention of infectious complications in patients undergoing laser therapy for the treatment of cataracts.[6][7] It has been approved for use in children, adults, and the elderly, with clinically proven efficacy and safety from age one and older.[4]

Besifloxacin is available as a 0.6% ophthalmological suspension, and dosing is 3 times a day, 4 to 12 hours apart for 7 days, regardless of age or condition.[4]

Adverse effects

During the treatment, the most frequently reported ocular adverse reaction was the appearance of conjunctival redness (approximately 2% of patients). Other possible adverse reactions, reported in subjects treated with besifloxacin were: blurred vision, eye pain, eye irritation, eye pruritus and headache.[4]

References

  1. ^ "InSite Vision Reaches Agreement to Sell ISV-403 to Bausch & Lomb" (Press release). InSite Vision. 2003-12-19. Retrieved 2009-08-15.
  2. ^ "Bausch & Lomb Receives FDA Approval of Besivance, New Topical Ophthalmic Antibacterial for the Treatment of Bacterial Conjunctivitis ("Pink Eye")" (Press release). Bausch & Lomb. 2009-05-29. Archived from the original on 2009-06-01. Retrieved 2009-05-29.
  3. PMID 17965029
    .
  4. ^ a b c d "Besivance Full Prescribing Info" (PDF). Bausch & Lomb. 02-01-2022. Retrieved 07-29-2022.
  5. PMID 24142473
    .
  6. PMID 24637269
    .
  7. PMID 23355771
    .


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