PHARMACOKINETICS OF LUBELUZOLE (PROSYNAP) AFTER SINGLE INTRAVENOUS DOSES IN HEALTHY-SUBJECTS

The single-dose pharmacokinetics of lubeluzole were investigated in 2 single-blind, placebo-controlled, dose-escalation studies in healthy m ale subjects. In the first study, 6 subjects received an intravenous i nfusion of 2.5, 5, and 10 mg lubeluzole. In the second study, a 15 mg dose of lubeluzole was administered to 6 subjects, of whom 5 also rece ived 20 mg and 2 also 25 mg lubeluzole. Following the infusion, plasma lubeluzole concentrations decayed biphasically, with a mean distribut ion half-life (t(1/2 alpha)) of 30 to 65 minutes and a mean terminal h alf-life (t(1/2 beta)) of 15 to 24 hours. The results of the 2 studies indicate that lubeluzole exhibits linear kinetics over the dose range tested in healthy male subjects.