Safinamide Mesylate

Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM. Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes with IC50 of 9 μM. Safinamide increases neostriatal dopamine concentration. In addition, safinamide is voltage-dependent sodium and calcium channel blocker. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals. Safinamide significantly inhibits cell body degeneration in the substantia nigra pars compacta. Safinamide has a high oral bioavailability (80–92%), is rapidly absorbed in plasma after reaching the peak within 0.5–2 hours declines, with a terminal half-life of about 3, 7, and 13 hours in mice, rats, and monkeys, respectively. Safinamide is currently in a Phase II clinical trial.