Garenoxacin (BMS284756)

Garenoxacin is a quinolone antibiotic.¹ It is active against a variety of Gram-positive and Gram-negative bacteria (MIC₉₀s = 0.025-6.25 and 0.0125-100 ?g/ml, respectively). Garenoxacin inhibits E. coli DNA gyrase supercoiling and S. aureus topoisomerase IV decatenation activities (IC₅₀s = 0.17 and 2.19 mg/L, respectively).² It is selective for S. aureus topoisomerase IV over human topoisomerase II (IC₅₀ = 509.7 ?g/L). Garenoxacin is efficacious against systemic quinolone-resistant S. aureus infection and pneumonia induced by the penicillin-resistant S. pneumoniae clinical isolate D-979 in mice (ED₅₀s = 0.0189 and 0.0278 mg/animal, respectively).¹

1.Takahata, M., Mitsuyama, J., Yamashiro, Y., et al.In vitro and in vivo antimicrobial activities of T-3811ME, a novel des-F(6)-quinoloneAntimicrob. Agents Chemother.43(5)1077-1084(1999) 2.Lawrence, L.E., Wu, P., Fan, L., et al.The inhibition and selectivity of bacterial topoisomerases by BMS-284756 and its analoguesJ. Antimicrob. Chemother.48(2)195-201(2001)