1999 Volume 47 Issue Supplement2 Pages 208-217
A Phase I study of gatifloxacin (GFLX), a new quinolone, was conducted to evaluate its safety and pharmacokinetics in healthy adult male volunteers. Six volunteers received 13 total oral doses of 300 mg twice daily on seven consecutive days at 10/14-hour intervals. One subject showed a transitory elevation of glutamic pyruvic transaminase (GPT) on the day after the last dosing, but it returned to normal on the 4th day and later. Except for that, blood biochemistry, subjective and objective symptoms, vital signs, hematology, blood chemistry, urinalysis, ECG, electroencephalogram, audiometry, ophthalmological test, and balance test all showed no abnormal changes attributable to the trial medication. No crystalluria was observed. No significant change was found in disposition in serum on Day 1, 4 and 7 with the succession of doses. Furthermore, the measured concentrations in serum fitted the simulation curve well. The drug was rapidly excreted: within 72 hours after the last dose, 78.8 % of the total dose was eliminated renally unchanged. Concentrations of GFLX in serum and urine reached a steady state within 2 to 3 days. These findings indicate the persistence of linear pharmacokinetics and no accumulation of GFLX in serum during multiple dosing.
In conclusion, GFLX was tolerated well by healthy subjects. This drug is expected to be clinically useful against various infections because of its potent and broad spectrum of antibacterial activity, and its favourable pharmacokinetics.
