Ezetimibe: a novel cholesterol absorption inhibitor (PDF)

Ezetimibe (Zetia), approved in late October, represents the first new class of cholesterol-lowering drugs in 15 years. Ezetimibe, an intestinal cholesterol absorption inhibitor, has a unique mechanism of action, distinct from those of statins and bile acid sequestrants. When used as monotherapy, ezetimibe lowers low-density lipoprotein cholesterol (LDL-C) levels up to 18.5%. Coadministration of ezetimibe with statin therapy reduces LDL-C levels up to an additional 22%. The article reviews ezetimibe?s chemistry, pharmacology, pharmacokinetics, and clinical trial results.