CI-1011 (Avasimibe) is an orally-available acylsulfamic acid inhibitor of Acyl Coenzyme A cholesterol acyltransferase (ACAT), an enzyme that catalyzes the esterification of cholesterol. inhibition of ACAT by CI-1011 presumably operates by modulating apoB synthesis and secretion, thereby lowering plasma concentration of apoB-containing lipoproteins. [3] CI-1011 inhibits ACAT at 3.3 uM, though it has been shown to be more potent dependent on microsome concentration. [1] CI-1011 also inhibits CYP450 enzymes 2C9, 1A2, and 2C19 at 2.9 uM, 13.9 uM, and 26.5 uM, respectively. [2] CI-1011 has been shown to be a PXR activator and has CYP3A4 induction profile approximately 10 fold more potent than rifampin. [2]

CI-1011 reduces plasma triglyceride levels in chow-fed rats, cholesterol-fed rats, sucrose-fed rats, and hamsters. [1] In addition to inhibiting lipid accumulation in macrophages, and thus reducing atherosclerotic lesion occurrence, CI-1011 also has plaque-stabilizing properties by inhibiting MMP expression and activity.