In Vivo |
In Sprague-Dawley (SD) rats, beagle dogs, and CD-1 mice, KBP-7072 demonstrated a linear PK profile after the administration of single oral and i.v. and multiple oral doses. The oral bioavailability ranged from 12% to 32%. The mean time to maximum concentration (T max) ranged from 0.5 to 4 h, and the mean half-life ranged from approximately 6 to 11 h. The administration of oral doses in the fed state resulted in marked reductions in the maximum plasma concentration (C max) and the area under the concentration-time curve (AUC) compared with dosing in fasted animals. The mean bound fractions of KBP-7072 were 77.5%, 69.8%, 64.5%, 69.3%, and 69.2% in mouse, rat, dog, monkey, and human plasma, respectively[1]. KBP-7072 exhibits dose-dependent potent activity against selected methicillin-susceptible (MSSA) and methicillin-resistant (MRSA) S. aureus strains over the dose range studied (0.25 to 64 mg/kg/6 h) in neutropenic murine pneumonia infection model[2].
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