Lascufloxacin (KRP-AM1977X) is a potent and orally active fluoroquinolone antibacterial agent. Lascufloxacin potently inhibits infections caused by various pathogens, including quinolone-resistant strains. Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections^[1][2].

In the Gram-negative bacteria, Lascufloxacin shows antibacterial activities againstMoraxella catarrhalisand β-lactamase-negative ampicillin-susceptible and ampicillin-resistant strains ofHaemophilus influenzae, with an MIC₉₀value of 0.06 μg/mL in all cases. The MIC₉₀values againstEnterobacter spp.,Klebsiella pneumoniae, andAcinetobacter spp.are 0.25 μg/mL, 0.25 μg/mL, and 0.5 μg/mL, respectively. Lascufloxacin inhibitsE. coliandP. aeruginosawith MIC₉₀s of 0.25 μg/mL and 4 μg/mL, respectively. The MIC₅₀and MIC₉₀values of Lascufloxacin againstM. pneumoniaeare 0.12 μg/mL and 0.25 μg/mL, respectively. Lascufloxacin shows potent activity against macrolide-resistantM. pneumoniaeisolates with an MIC₉₀of 0.12 μg/mL^[1].
The MICs of Lascufloxacin against parentS. aureusstrains ranged from 0.008 to 0.015 μg/mL, and those against fourth-stepparC,gyrA,parC, andgyrAmutant strains are all 2 μg/mL. Lascufloxacin shows incomplete cross-resistance against the mutant strains. The activities of Lascufloxacin against first- and second-step mutant strains ofS. pneumoniaeare more potent than the activities of other quinolones, and the MICs of Lascufloxacin againstgyrAandparCdouble mutants are 0.25 to 0.5 μg/mL^[1].

A pharmacodynamic study using a mouse thigh infection model indicates that the ratios of the free area under the curve (fAUC) to MIC in plasma required for bacteriostasis, or 1-log or 2-log CFU killing againstS. pneumoniaeisolates, are 10, 16, and 28, respectively. Lascufloxacin shows significant bacterial killing in the mouse model when emulated the area under the concentration-time curve (AUC) in plasma in dose of 75 mg per day [q.d.])^[2].

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