Cardio-cerebral vascular diseases due to atherosclerosis are still the leading cause of death worldwide. Low-density lipoprotein cholesterol (LDL-C) and apolipoprotein B have been identified as the primary factors responsible for the atherosclerotic process, with a causal effect. Many drugs aimed at reducing LDL-C levels are already on the market, acting in different ways in terms of mechanism of action, efficacy, and safety. Moreover, new lipid-lowering agents and new technologies in the fields of gene editing and immunotherapy are currently under investigation. A more recent biomarker associated with an increased risk of plaque generation, progression, and subsequent ASCVD is the lipoprotein (a) and, in the next few years, it will be the new target of pharmacological therapy. The aim of this review is to present the landscape of therapies already approved to reduce LDL-C levels, evaluating their efficacy, tolerability, and indications. Moreover, we take a glimpse into the future to evaluate experimental novel therapies to lower LDL-C levels that will be approved in the next few years or are under clinical evaluation.