Begacestat

Begacestat selectively inhibits cleavage of amyloid precursor protein (APP) over Notch. Lowers levels of Aβ42 and Aβ40 (EC50 values are 12.4 and 14.8 nM respectively in cells expressing human recombinant APP). In healthy human volunteers, oral administration of a single dose of GSI-953 produces dose-dependent changes in plasma Abeta levels, which confirms pharmacodynamic activity of GSI-953 in humans.