tcsc5695 Avasimibe

Avasimibe is a ACAT inhibitor incluing ACAT-1 and ACAT-2

In vitro: 1) Avasimibe has beneficial on plasma lipids and direct antiatherosclerotic activity, independent of lipid effects, in various animal models of hypercholesterolemia

2) Avasimibe enhances the lipid lowering effect of atorvastatin in subjects with homozygousfamilial hypercholesterolemia.

In vivo: 1) The reference for administration is daily dosages up to 1000 mg/d for up to 2 weeks and 750 mg/d for up to 8 weeks.

2) Avasimibe reduced plasma apoB levels by 20% in A-PLUS when given at a dose of 750 mg.

3) Avasimibe can potently lowered plasma cholesterol levels in ApoE*3-Leiden mice and considerably reduced atherosclerotic lesion area in addition to its cholesterol-lowering effect.