title: Comparative activity of garenoxacin and other agents by susceptibility and time-kill testing against Staphylococcus aureus, Streptococcus pyogenes and respiratory pathogens.
abstract: OBJECTIVE
  Garenoxacin is a novel des-F(6)quinolone that has shown excellent antimicrobial activity against a wide range of clinically important microorganisms. In this study, its activity was examined, in comparison with that of other antimicrobial agents, by susceptibility and time-kill testing against Staphylococcus aureus, Streptococcus pyogenes and respiratory pathogens.
  
  
  METHODS
  Overall, 200 bacterial strains were tested. The antimicrobial activity of garenoxacin was compared with that of ciprofloxacin, levofloxacin, moxifloxacin, amoxicillin, co-amoxiclav, cefuroxime, cefotaxime, ceftriaxone, imipenem, erythromycin and clarithromycin. In addition, the bactericidal activity of garenoxacin, moxifloxacin, levofloxacin and ciprofloxacin was evaluated by time-kill analysis against four strains each of staphylococci [two methicillin-susceptible (MSSA) and two methicillin-resistant (MRSA)], pneumococci (two penicillin-susceptible and two penicillin-resistant) and Streptococcus pyogenes (two erythromycin-susceptible and two erythromycin-resistant). Antibiotics were tested at concentrations 1-8 x MIC.
  
  
  RESULTS
  MIC90 values of garenoxacin for the MSSA and MRSA strains were 0.03 and 2 mg/L, respectively. Among all the quinolones tested, garenoxacin yielded the lowest MIC values against all pneumococci (MIC90 0.12 mg/L) irrespective of macrolide resistance; the rank order of activity was garenoxacin> moxifloxacin>levofloxacin>ciprofloxacin. Excellent activity was shown also against Haemophilus influenzae (MIC90 <or= 0.03 mg/L) and Moraxella catarrhalis (MIC90 <or= 0.03 mg/L). Ninety percent of S. pyogenes were inhibited at garenoxacin concentrations equal to 0.25 mg/L, its activity not being influenced by macrolide susceptibility. Garenoxacin was rapidly bactericidal against staphylococci, producing a >or= 3 log10 decrease in viable counts (cfu/mL) within 3 h at 4 x MIC, whereas a moderate, slower killing rate was observed versus streptococci.
  
  
  CONCLUSIONS
  This investigational des-F(6)quinolone represents a promising alternative for the treatment of respiratory tract infections.
mesh_terms: D000890:Anti-Infective Agents / Q000494:pharmacology*; D001424:Bacterial Infections / Q000382:microbiology; D015169:Colony Count, Microbial; D024881:Drug Resistance, Bacterial; D024841:Fluoroquinolones / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006095:Gram-Positive Cocci / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D012141:Respiratory Tract Infections / Q000382:microbiology*; D013211:Staphylococcus aureus / Q000187:drug effects; D013297:Streptococcus pyogenes / Q000187:drug effects; D013997:Time Factors
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; C419689:garenoxacin