Safety, tolerability and pharmacokinetics of the new long-acting quinolone DW-116 after single and multiple dosing in healthy subjects.

The safety, tolerability and pharmacokinetics of DW-116, a new fluoroquinolone with a broad antibacterial spectrum, were evaluated in healthy male subjects after administration of single oral doses of 100, 200, 300 and 800 mg and after administration of multiple oral doses of 300 or 400 mg, respectively, for 7 days. DW-116 was well tolerated. Gastrointestinal symptoms and skin reactions were noted and considered to be possibly related to DW-116. The geometric means of the maximum plasma concentrations (Cmax) linearly increased with the dose administered from 1.19 mg/L to 8.73 mg/L after single dose administration. At steady state, the geometric mean minimum and maximum plasma concentrations were 2.14 and 5.65 mg/L, respectively, after the multiple 300 mg dose and 2.73 and 8.00 mg/L, respectively, for the multiple 400 mg dose. Tmax varied between 1 and 5 h. The terminal half-life ranged from 11.37 to 24.89 h. The geometric mean renal clearance was approximately 30 mL/min. Approximately 45% of the dose was excreted unchanged in urine within 60 h. There was no clinically relevant deviation from dose proportionality. The changes in steady-state pharmacokinetic parameters when DW-116 was taken before a high-fat breakfast were not clinically relevant. In conclusion, DW-116 was safe in this study, the first administration to human subjects. Its pharmacokinetics indicate that once-daily dosing may be possible.

RCT Entities:   Population Interventions Outcomes