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Ezetimibe, a Selective Inhibitor of the Transport of Cholesterol

2008; The Japanese Society of Internal Medicine; Volume: 47; Issue: 13 Linguagem: Inglês

10.2169/internalmedicine.47.1099

1349-7235

Shin-ichiro Miura, Keijiro Saku,

Diabetes Treatment and Management

Niemann-Pick C1-like 1 (NPC1L1) has recently been identified and has been shown to have features of a plasma membrane transporter, including a secretion signal, 13 predicted transmembrane domains, extensive N-linked glycosylation sites and a sterol-sensing domain. It is highly expressed on the surface of absorptive jejunal enterocytes. NPC1L1 has been shown to be a direct target of ezetimibe, and an ezetimibe-sensitive pathway plays a role in intestinal cholesterol absorption. Ezetimibe-based therapy represents an exciting new area in the treatment of dyslipidemia.