Avasimibe (CAS 166518-60-1) is an orally bioavailable inhibitor of acyl-coenzyme A cholesterol acyltransferase (ACAT) an enzyme involved in cholesterol esterification It exhibits potent inhibition with an IC50 of approximately 60 nM In cell-based studies avasimibe reduces intracellular cholesterol esters in a dose-dependent manner without elevating free cholesterol levels suggesting an advantageous safety profile Additionally avasimibe reduces synthesis and secretion of Apo B 100 a constituent of very low-density lipoprotein (VLDL) in HepG2 cells and increases bile acid synthesis in rat hepatocytes Beyond dyslipidemic modulation and anti-atherogenic activities it influences amyloid precursor protein (APP) trafficking reducing its maturation and subsequent amyloid-beta (A ) peptide generation providing avenues for Alzheimer s disease research