The role of low-density lipoprotein cholesterol (LDL-C) in the pathophysiology of atherosclerosis is well recognized, and the use of LDL-C lowering medications has led to a significant reduction of cardiovascular risk in both primary and secondary prevention. Statins are the standard of care and their use is supported by extensive evidence demonstrating their effectiveness in lowering LDL-C and in reducing the risk for cardiovascular disease. However, many individuals at risk for cardiovascular disease fail to achieve LDL-C goals. In addition, several patients are intolerant to statins due to side effects, mostly myalgia and weakness, especially at high statin doses. However, until recently, the efficacy of other non-statin LDL-C-lowering drugs was modest, not exceeding a LDL-C reduction of 20%. In view of the above, extensive research is being carried out to identify new LDL-C-lowering agents with an acceptable side effect profile, which, used alone or in combination with statins, would improve our ability to achieve LDL-C goals and reduce cardiovascular risk. This review aims to provide the current evidence regarding the newly approved LDL-C-lowering agents, as well as the clinical and scientific data pertaining to promising new and emerging LDL-C-lowering drugs on the horizon.