BPN-15606 besylate (p.o.; 10 mg/kg, 25 mg/kg, and 50 mg/kg; 7 days) shows excellent dose-dependent efficacy in both plasma and brain on lowering of Aβ42 and Aβ40 levels in mice. BPN-15606 besylate (p.o.; 5 mg/kg, 25 mg/kg and 50 mg/kg; 9 days) dose-dependently reduces CSF on lowering of Aβ42 and Aβ40 levels in rats. BPN-15606 besylate (p.o.; 25 mg/kg; single dose) shows a robust effect on both brain and plasma Aβ 42 and Aβ40 levels, which begins approximately 30–60 minutes following the single-dose administration and lasted for ≥24 hours in C57BL/6 mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.