Pazufloxacin mesylate (T-3762)

Pazufloxacin is a broad-spectrum synthetic fluoroquinolone antibiotic.¹ It is active against Gram-negative and Gram-positive bacteria, including clinical isolates of E. coli, K. pneumoniae, methicillin-susceptible and -resistant S. aureus, and methicillin-susceptible and -resistant S. epidermidis (MIC₉₀s = 0.05, 0.1, 0.39, 12.5, 0.39, and 6.25 μg/ml, respectively). It inhibits E. coli, P. aeruginosa, and S. aureus DNA gyrase (IC₅₀s = 0.88, 1.9, and 10.2 μg/ml, respectively) and S. aureus topoisomerase IV (IC₅₀ = 24.2 μg/ml) in cell-free assays.^1,2 In vivo, pazufloxacin is active against systemic E. coli, K. pneumoniae, and methicillin-resistant S. aureus infections in mice (ED₅₀s = 0.15, 5.5, and 4.5 mg/kg, respectively).³

1.Muratani, T., Inoue, M., and Mitsuhashi, S.In vitro activity of T-3761, a new fluoroquinoloneAntimicrob. Agents Chemother.36(10)2293-2303(1992) 2.Takei, M., Fukuda, H., Kishii, R., et al.Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibitionAntimicrob. Agents Chemother.45(12)3544-3547(2001) 3.Fukuoka, Y., Ikeda, Y., Yamashiro, Y., et al.In vitro and in vivo antibacterial activities of T-3761, a new quinolone derivative.Antimicrob. Agents Chemother.37(3)384-392(1993)