Avasimibe (CI-1011, PD-148515) is a potent, selective inhibitor of acyl-CoA: cholesterol O-acyl transferase (ACAT) with IC50 of 60 nM.
Avasimibe potently reduces plasma cholesterol in chow-fed rats and in rabbits fed a cholesterol-free, casein-containing diet characterized by both hepatic overproduction of apo B-containing lipoproteins and delayed lipoprotein clearance.
Avasimibe decreases both VLDL and LDL apolipoprotein B production in miniature pigs.
Avasimibe synergistically reduces cholesteryl ester content in THP-1 macrophages combined with Atorvastatin,
