Ezetimibe is a medication used to treat high blood cholesterol and certain other lipid abnormalities.[1][2] Generally it is used together with dietary changes and a statin.[3] It is also available in the fixed combinations ezetimibe/simvastatin (Vytorin),[4] ezetimibe/atorvastatin,[5] ezetimibe/rosuvastatin,[2][6] and ezetimibe/bempedoic acid.[7] See also [1].
Ezetimibe inhibits the absorption of cholesterol from the small intestine and decreases the amount of cholesterol normally available to liver cells. The lower levels of cholesterol in the liver cells leads them to absorb more cholesterol from circulation and thus lowering the levels of circulating cholesterol. It blocks the critical mediator of cholesterol absorption, the Niemann-Pick C1-like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells, as well as in hepatocytes; it blocks aminopeptidase N and interrupts a caveolin 1–annexin A2 complex involved in trafficking cholesterol.[8]
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