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Ezetimibe

Mechanism of action:
Ezetimibe is a cholesterol absorption inhibitor. Ezetimibe inhibits the activity of the NPC1L1 transporter. NPC1L1 (Niemann-Pick C1-Like 1) is an important transporter responsible for cholesterol absorption in small intestinal epithelial cells. When Ezetimibe inhibits NPC1L1, it prevents dietary cholesterol and biliary cholesterol from entering intestinal epithelial cells.
Reference(s):
1. Garcia-Calvo M et al. (2005). The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1). Proc Natl Acad Sci USA.
2. Phan BA et al. (2012). Ezetimibe therapy: mechanism of action and clinical update. Vasc Health Risk Manag.
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