Consistency in efficacy and safety of ezetimibe coadministered with statins for treatment of hypercholesterolemia in women and men.

BACKGROUND: Women are often not treated as aggressively as men to control levels of low-density lipoprotein cholesterol (LDL-C), despite evidence that women and men realize comparable cardiovascular benefit from lipid-lowering therapy. Statins are the most effective drugs currently available for treating hypercholesterolemia. Despite the impressive cholesterol-lowering capacity of statins, however, many patients on statin therapy fail to reach established target levels of LDL-C. The cholesterol absorption inhibitor, ezetimibe, blocks the intestinal absorption of dietary and biliary cholesterol, a mechanism of action complementary to that of statins, which inhibit hepatic cholesterol synthesis. Ezetimibe coadministered with statins produces significant incremental reductions in LDL-C compared with statin monotherapy.

METHODS: Four randomized, double-blind, placebo-controlled, balanced-parallel group trials compared the efficacy and safety of statin monotherapy (lovastatin or pravastatin 10, 20, or 40 mg; simvastatin or atorvastatin 10, 20, 40, or 80 mg) vs. ezetimibe 10 mg plus statin (as above). A gender subset analysis (women, n = 1065; men, n = 796) on data pooled across these four trials was carried out to determine whether ezetimibe plus statin for the treatment of hypercholesterolemia is equally efficacious in women and men.

RESULTS: Compared with statin monotherapy, ezetimibe plus statin demonstrated greater efficacy in reducing blood levels of LDL-C, apolipoprotein B, and triglycerides and raising high-density lipoprotein cholesterol. The beneficial effects of ezetimibe were comparable in women and men. The safety profile of subjects receiving ezetimibe plus statin was similar to that of patients receiving statin monotherapy and similar between the two sexes.

CONCLUSIONS: Ezetimibe plus statin was more effective than statin alone in improving the lipid profile of patients with hypercholesterolemia and was equally efficacious in women and men. Ezetimibe plus statin was well tolerated and had a favorable safety profile in both patient subgroups. Ezetimibe coadministered with statins, a dual inhibition treatment strategy that targets both cholesterol absorption and synthesis, is an effective therapeutic option for women with hypercholesterolemia.