Eravacycline is a novel, fully-synthetic fluorocycline antibiotic with in vitro activity against aerobic and anaerobic Gram-positive and Gram-negative pathogens including multi-drug resistant (MDR) bacteria. The pharmacokinetics (PK), urinary excretion, and safety/tolerability of intravenous (IV) eravacycline were evaluated in single- and multiple ascending dose studies. Healthy subjects received single IV doses of 0.1 to 3 mg/kg or 10 days treatment with 0.5 or 1.5 mg/kg q24h over 30 minutes, 1.5 mg/kg q24h over 60 minutes, or 1 mg/kg q12h over 60 minutes. After single doses, total exposure (AUC) and peak plasma concentrations (Cmax) of eravacycline increased in an approximately dose-proportional manner. After multiple doses, steady-state was achieved within 5 to 7 days. Accumulation (AUC0-24) ranged between approximately 7% and 38% with the q24h dosing regimens and 45% with 1 mg/kg q12h. Eravacycline was generally well tolerated, with dose-related nausea, infusion site effects, and superficial phlebitis that were mild or moderate. These results provide support for the 1 mg/kg q12h regimen used in clinical studies of eravacycline.
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