Ezetimibe (Molecule of the Month for May 2017)
Zetia, Ezetrol, Vytorin, Inegy
Ezetimibe is a drug that lowers plasma cholesterol levels. It acts by decreasing cholesterol absorption in the small intestine. It may be used alone when other cholesterol-lowering medications are not tolerated or together with statins when statins alone do not control cholesterol.
Ezetimibe is recommended as second line therapy for those intolerant of statins or unable to achieve target LDL cholesterol levels on statins alone by several major medical group practice guidelines.
Ezetimibe inhibits the absorption of cholesterol from the small intestine and decreases the amount of cholesterol normally available to liver cells, leading them to absorb more from circulation and thus lowering levels of circulating cholesterol. The exact mechanism is not known, but it appears that ezetimibe 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; blocks aminopeptidase N, and interrupts a Caveolin 1-Annexin A2 complex involved in trafficking cholesterol
Formal Chemical Name (IUPAC)
Update by Karl Harrison
(Molecule of the Month for May 2017 )
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