Ezetimibe blocks internalization of the NPC1L1/cholesterol complex.

Chang, Ta-Yuan; Chang, Catherine · Cell Metab · 2008

review · Level V

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Abstract

Niemann-Pick C1-like 1 (NPC1L1) is a target for ezetimibe, a drug that blocks intestinal cholesterol absorption. A new study by Ge et al. (2008) in this issue of Cell Metabolism shows that non-lipoprotein-bound cholesterol induces endocytosis of NPC1L1 and that ezetimibe blocks the internalization of the NPC1L1/cholesterol complex. The in vivo significance of these findings is discussed.

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