Niemann-Pick C1-like 1 protein (NPC1L1) is the putative intestinal sterol transporter and the
molecular target of ezetimibe, a potent inhibitor of cholesterol absorption. To address the
role of NPC1L1 in cholesterol trafficking in intestine, the regulation of cholesterol trafficking
by ezetimibe was studied in the human intestinal cell line, CaCo-2. Ezetimibe caused only a
modest decrease in the uptake of micellar cholesterol, but markedly prevented its
esterification. Cholesterol trafficking from the plasma membrane to the endoplasmic …