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 male subjects. In the first study, 6 subjects received an intravenous infusion 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 received 20 mg and 2 also 25 mg lubeluzole. Following the infusion, plasma lubeluzole concentrations decayed biphasically, with a mean distribution half-life (t1/2alpha) of 30 to 65 minutes and a mean terminal half-life (t1/2beta) 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.
Van de Velde
V
V
Janssen Research Foundation, Beerse, Belgium.
Crabbe
R
R
Van Peer
A
A
Woestenborghs
R
R
Van Osselaer
N
N
Hantson
L
L
Heykants
J
J
D000328:Adult; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D008875:Middle Aged; D018696:Neuroprotective Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D010880:Piperidines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D016037:Single-Blind Method; D013844:Thiazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D018696:Neuroprotective Agents; D010880:Piperidines; D013844:Thiazoles; C097722:lubeluzole