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To evaluate the pharmacokinetic characteristics and safety of delafloxacin, a new fluoroquinolone drug, in Chinese healthy subjects, and to evaluate the expected microbiological efficacy of delafloxacin in treating infections caused by Staphylococcus aureus and Streptococcus pneumoniae through pharmacokinetic/pharmacodynamic analysis.
This trial consists of two parts. The first part is a randomized, double-blind, placebo-controlled, single-dose/multiple-dose administration trial with a dose range of 150-450 mg. The second part is a randomized, open-label, double-period, self-crossover trial comparing the pharmacokinetic similarities between a 300 mg intravenous infusion of the test drug and the reference drug. Combined with the in vitro pharmacodynamic data of delafloxacin against Staphylococcus aureus and Streptococcus pneumoniae clinically isolated in China, the Monte Carlo simulation method was used to analyze the probability of target attainment and cumulative fraction of response of the 300 mg q12 h intravenous infusion over 60 min and to evaluate the expected microbiological efficacy.
After administering 150, 300 and 450 mg of delafloxacin to Chinese healthy subjects in single doses, the Cmax, AUC0-t and AUC0-∞ increase proportionally with the dose. The apparent volume of distribution ranged from 45.79 to 144.38 L. The elimination half-life of each dose group ranged from 2.99 to 11.87 h. The cumulative urinary excretion rates of (47.69±8.11)% and (73.71±9.32)% were observed for single doses of 300 and 450 mg, respectively, suggesting that the primary route of excretion was renal. The 90% confidence interval of Cmax, AUC0-t and AUC0-∞ of test drug over reference drug after single-dose intravenous infusion are all within 80.00%-125.00%. After reaching steady state with multiple-dose administration in the 300 mg group, the plasma exposure level was similar to that of the single-dose administration group.
Single-dose intravenous infusion of 150-450 mg delafloxacin in healthy subjects showed linear pharmacokinetic characteristics, and there was no accumulation after 300 mg q12 h administration. Adverse effects were mild, indicating good safety, and good microbiological efficacy.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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