Dyslipidemia is an established risk factor for cardiovascular disease. While statin therapy remains the most important component of dyslipidemia management, a substantial proportion of patients on statin monotherapy fails to achieve guideline-recommended lipid levels. Ezetimibe is a second-line lipid-lowering agent that reduces sterol absorption, and has a favorable effect on lipid profile. This article reviews studies examining the role of ezetimibe on lipid profile, metabolic biomarkers, and cardiovascular outcomes in individuals with metabolic diseases. Special focus is given to studies in patients with dyslipidemia, Type 2 diabetes, and the metabolic syndrome. The controversy surrounding the role of ezetimibe in mitigating atherosclerosis is also highlighted. The article concludes that the ezetimibe-statin combination improves lipid parameters and helps attain guideline-recommended lipid goals in patients with metabolic diseases. However, further research is needed to better understand the role of ezetimibe monotherapy, and the impact of ezetimibe on clinical cardiovascular outcomes.