In vitro and in vivo antibacterial activity of T-3912, a novel non-fluorinated topical quinolone

J Antimicrob Chemother. 2002 Mar;49(3):455-65. doi: 10.1093/jac/49.3.455.

Abstract

The in vitro and in vivo activity of T-3912, a novel non-fluorinated topical quinolone, was compared with that of nadifloxacin, ofloxacin, levofloxacin, clindamycin, erythromycin and gentamicin. The in vitro activity of T-3912 against methicillin-susceptible Staphylococcus aureus, ofloxacin-resistant and methicillin-resistant S. aureus, Staphylococcus epidermidis, ofloxacin-resistant S. epidermidis, penicillin-resistant Streptococcus pneumoniae and Propionibacterium acnes was four-fold to 16 000-fold greater than that of other agents at the MIC90 for the clinical isolates. The activity of T-3912 was not influenced by grlA mutation in S. aureus, and the degree of MIC increase of T-3912 for grlA-gyrA double and triple mutants was lowest among the quinolones tested (nadifloxacin, levofloxacin and ofloxacin). The inhibitory activity of T-3912 was compared with other quinolones for DNA gyrase and topoisomerase IV of S. aureus SA113. T-3912 showed the greatest inhibitory activity for both enzymes among the quinolones tested. The isolation frequency of spontaneous mutants resistant to T-3912 was < 1.7 x 10(-9) and < 2.0 x 10(-9) for S. aureus SA113 and P. acnes JCM 6425, respectively. Furthermore, resistance to T-3912 could not be clearly detected in the 28th transfer by the serial passage method. T-3912 exhibited more potent bactericidal activity against S. aureus and P. acnes than nadifloxacin and clindamycin in a short time period. T-3912 in a 1% gel formulation showed good therapeutic activity against a burn infection model caused by S. aureus SA113, P. acnes JCM6425 and multidrug-resistant S. aureus F-2161. These results indicate that T-3912 is potentially a useful quinolone for the treatment of skin and soft-tissue infections and that its potent bactericidal activity might be able to shorten the treatment period.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Infective Agents / pharmacology
  • Anti-Infective Agents / therapeutic use
  • Clindamycin / pharmacology
  • Clindamycin / therapeutic use
  • Colony Count, Microbial
  • DNA Topoisomerase IV / antagonists & inhibitors
  • Drug Resistance, Bacterial / genetics
  • Erythromycin / pharmacology
  • Erythromycin / therapeutic use
  • Fluoroquinolones*
  • Gene Frequency
  • Genes, Bacterial
  • Gentamicins / pharmacology
  • Gentamicins / therapeutic use
  • Levofloxacin
  • Male
  • Mice
  • Mice, Inbred ICR
  • Microbial Sensitivity Tests
  • Mutation
  • Ofloxacin / pharmacology
  • Ofloxacin / therapeutic use
  • Quinolines / pharmacology*
  • Quinolines / therapeutic use*
  • Quinolizines / pharmacology
  • Quinolizines / therapeutic use
  • Staphylococcal Skin Infections / drug therapy*
  • Staphylococcus aureus / drug effects*
  • Staphylococcus aureus / enzymology
  • Staphylococcus aureus / genetics
  • Staphylococcus epidermidis / drug effects*
  • Staphylococcus epidermidis / enzymology
  • Staphylococcus epidermidis / genetics
  • Topoisomerase II Inhibitors

Substances

  • Anti-Infective Agents
  • Fluoroquinolones
  • Gentamicins
  • Quinolines
  • Quinolizines
  • T3912
  • Topoisomerase II Inhibitors
  • Clindamycin
  • Erythromycin
  • nadifloxacin
  • Levofloxacin
  • Ofloxacin
  • DNA Topoisomerase IV