[Molecular mechanism of action of ezetimibe and recent therapeutics]

ABSTRACT

High blood Low density lipoprotein cholesterol is a major cardiovascular risk factor and must be the primary target of primary and secondary heart protection. Statines, 3-hydroxy-3-methylglutaryl-coenzyme A [HMG-CoA] reductase inhibitors, are the cornerstone of lipid-lowering therapy for reducing LDLc levels. However, some patients at high risk fail to achieve LDLc target despite high-dose statin therapy. Statins may also induce adverse effects. Ezetimibe is the first potent cholesterol absorption inhibitor. Several ongoing clinical interventional trials will shed more light on the association statin plus ezetimibe in high risk patients. A better understanding of intestinal cholesterol absorption will lead to novel approaches for the prevention and treatment of hyperlipidemia