Ezetimibe: Its Novel Effects on the Prevention and the Treatment of Cholesterol Gallstones and Nonalcoholic Fatty Liver Disease

Figure 5

Pathways underlying the absorption of cholesterol from the intestinal lumen and its delivery to the liver. High dietary cholesterol delivery through the chylomicron pathway could provide an important source of excess cholesterol molecules for hepatic secretion into bile, thereby inducing cholesterol-supersaturated bile and enhancing cholesterol gallstone formation. Ezetimibe significantly suppresses cholesterol absorption from the small intestine via the Niemann-Pick C1-like 1 (NPC1L1) pathway, possibly by a transporter-facilitated mechanism. This effect of ezetimibe could significantly diminish the cholesterol content of the liver, which in turn remarkably decreases bioavailability of cholesterol for hepatic secretion into bile. ABCG5/G8: ATP-binding cassette (transporters) G5 and G8; ACAT2: acyl-CoA:cholesterol acyltransferase isoform 2; APO-B48: apolipoprotein B48; MTTP: microsomal triglyceride transfer protein. See text for details.