The long-term clinical benefits of lowering serum lipid levels have been demonstrated in multiple clinical trials in recent years. These include coronary artery disease regression and decreases in the incidence of adverse clinical events, such as myocardial infarction or refractory ischemia. Reductions in overall mortality have also been demonstrated. The health risk of dyslipidemia led the National Cholesterol Education Program expert panel to recommend intervention to bring low-density lipoprotein cholesterol values to within certain goal levels through a variety of interventions. This article reviews the available pharmacologic agents and compares their efficacy, safety, and cost-effectiveness.