Garenoxacin (Mesylate hydrate)

Garenoxacin (BMS284756) Mesylate hydrate is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms^[1]. In Vitro: Garenoxacin (BMS284756) (0-8 days) inhibits mycoplasmas and ureaplasmas with MIC₉₀s ≤0.25 μg/mL against tested strains^[1].
Garenoxacin (48 h) inhibits S. aureus wild type and mutants with MICs of 0.0128-4.0 μg/mL^[2].
Garenoxacin inhibits topoisomerase IV and gyrase from S. aureus with IC₅₀s of 1.25 to 2.5 and 1.25 μg/mL, respectively^[2].
Garenoxacin has a low propensity for selective enrichment of fluoroquinolone-resistant mutants among ciprofloxacin-susceptible isolates of S. aureus^[3]. In Vivo: Garenoxacin (12.5-50 mg/kg; s.c.; once) is highly effective against the wild-type strain and mutants harboring a single mutation in a mouse pneumonia model with S. pneumonia infection^[4].
Garenoxacin (10 and 30 mg/kg; p.o.; once) reduces the viable cell counts in the lungs and significantly prolongs survival on experimental secondary pneumococcal pneumonia caused by S. pneumoniae D-979 in BALB/c female mice^[5].