Avasimibe

Avasimibe is a small molecule inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), specifically targeting both ACAT1 and ACAT2 isoforms (also known as sterol O-acyltransferases SOAT1 and SOAT2). It was developed to reduce cholesterol esterification, lower plasma cholesterol levels, and inhibit the formation of foam cells by enhancing free cholesterol efflux and inhibiting modified LDL uptake. Avasimibe also acts as a potent activator of the pregnane X receptor, indirectly inducing CYP3A4 and P-glycoprotein, while inhibiting several cytochrome P450 isoenzymes. Initially investigated for hyperlipidemia, atherosclerosis, and peripheral vascular disease, it reached phase III clinical trials but was discontinued in 2003 after disappointing results in these indications. Later research has explored its potential antiviral activity against hepatitis C virus by impairing viral assembly through effects on lipid metabolism, as well as anticancer properties via induction of apoptosis in glioblastoma cells[1][3][4][5][6].

Other names

avasimibe sodium