Hyperlipidemia is the best-established risk factor for cardiovascular disease (CVD), the leading cause of death worldwide. Lowering LDL-C levels, primarily with statins has been the cornerstone of lipid-lowering therapy. However, over the past few years, new therapeutic approaches have emerged to reduce the additional residual risk of CVD. This thesis provides a general overview of lipid and lipoprotein metabolisms and their impact on CVD. It also summarized the conventional lipid-lowering drugs and the latest information on the novel treatment approaches for hyperlipidemia that target LDL-C levels and other atherogenic lipid fractions.