THE SAFETY AND TOLERABILITY OF SINGLE INTRAVENOUS DOSES OF LUBELUZOLE(PROSYNAP) IN HEALTHY-VOLUNTEERS

The safety and tolerability of single escalating doses of lubeluzole w ere evaluated in healthy male volunteers in 2 studies. In the first of 2 randomized, single-blind, placebo-controlled, dose-escalation studi es, 6 subjects received single 30-minute infusions of 2.5, 5, and 10 m g of lubeluzole, and 2 additional subjects received placebo. In the se cond study 6 different subjects received a 1-hour infusion of 15 mg of lubeluzole, 5 of whom received the 20-mg dose, and 2 received 25 mg o f lubeluzole. Two additional subjects received placebo. Small increase s and decreases in PQ, QRS, QT, QTc, and QTm intervals were noted afte r infusion of all lubeluzole doses and placebo, however, these changes were within the normal ranges for these values except for the QTc for the 25-mg dose of lubeluzole. Significant prolongation of the QTc int erval was observed at the end of the 1-hour infusion in both subjects receiving the 25-mg dose of lubeluzole. No clinically relevant changes in systolic time intervals, heart rate, blood pressure, and clinical laboratory values were noted in subjects receiving 2.5-25 mg of lubelu zole or placebo. Adverse experiences, predominantly lightheadedness an d dizziness, were reported by subjects receiving doses of lubeluzole g reater than or equal to 10 mg. Lubeluzole, administered as single intr avenous doses of 2.5-15 mg, is safe and well tolerated in healthy male volunteers.