Update on the efficacy and safety of combination ezetimibe plus statin therapy

The primary aim of lipid-related cardiovascular disease (CVD) risk management is the lowering of LDL-C levels. Numerous studies have shown that statins, which inhibit cholesterol biosynthesis, effectively reduce serum LDL-C and subsequent CVD risk. Ezetimibe is an LDL-C-lowering drug that inhibits the absorption of dietary and biliary cholesterol through its interaction with the intestinal Niemann Pick CI-like I sterol transporter. When combined with statin therapy, the complementary inhibition of cholesterol absorption and synthesis with these two agents is highly effective in not only reducing LDL-C, but also in improving serum levels of other lipid fractions and reducing high-sensitivity C-reactive protein levels compared with either agent alone. This article summarizes the most current clinical data available on the lipid-altering efficacy and safety of ezetimibe coadministered with statins in patients with hypercholesterolemia and in other diverse populations. In addition, the impact of ezetimibe on surrogate imaging, clinical outcome measures and other potential effects that may translate into CVD risk reduction are also described. An assessment of the full clinical significance of ezetimibe therapy will depend on the results of cardiovascular outcomes trials anticipated during the next few years.