Ezetimibe - An Overview of its Low-density Lipoprotein Cholesterol Lowering Efficacy

Ezetimibe - An Overview of its Low-density Lipoprotein Cholesterol Lowering Efficacy

Farnier Michel, Konstantinos Tziomalos
European Cardiovascular Disease 2007
Published: June 2007
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Cardiovascular disease (CVD) is the leading cause of morbidity and mortality worldwide.1 The relationship between coronary heart disease (CHD) and elevated low-density lipoprotein cholesterol (LDL-C) levels is well established.2 Several large-scale trials, in both primary and secondary prevention settings, have shown that lowering LDL-C levels using statins substantially reduces cardiovascular mortality.3,4 More importantly, this reduction correlates with the LDL-C level achieved; ‘lower is better3,4.

The need for effective LDL-C-lowering therapy is increasingly important as LDL-C goals become more stringent. The updated National Cholesterol Education Program Adult Treatment Panel III (NCEP ATP III) guidelines recommend an optional goal of <1.8mmol/l (<70mg/dl) for very high-risk patients,4 and the American Heart Association/American College of Cardiology (AHA/ACC) recommended that this LDL-C goal is a 'reasonable' option for patients with CHD.5 Is it therefore 'unreasonable' not to achieve this target? Guidelines for the prevention of CVD issued by the Joint British Societies (JBS2) also define the optimal LDL-C treatment target for high-risk patients as <2.0mmol/l (<77mg/dl).6



Despite the established efficacy of statins, the number of patients on statin monotherapy who achieve and maintain LDL-C levels recommended by current guidelines is suboptimal.7,8 In the Statin Therapies for Elevated Lipid Levels Compared Across Doses to Rosuvastatin (STELLAR) trial, rosuvastatin 10mg, atorvastatin 20mg, simvastatin 20mg and pravastatin 20mg achieved the LDL-C goal of <2.6mmol/l (<100mg/dl) in 53%, 44%, 14% and 3% of patients, respectively.9 At their top doses, rosuvastatin 40mg, atorvastatin 80mg, simvastatin 80mg and pravastatin 40mg daily achieved this LDL-C goal in 80%, 70%, 53% and 8% of patients, respectively.9 Therefore, not all patients reach their LDL-C goals, even with the highest doses of potent statins. It follows that even fewer will reach the LDL-C goal of <1.8mmol/l (<70mg/dl) with statin monotherapy. Furthermore, titration to higher statin dosages has its limitations because of increasing adverse side effects and decreased compliance.10-12

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