Over the past decade, the therapeutic landscape of cholesterol-lowering drugs has rapidly expanded to address the limitations of current therapies, the failure to achieve LDL-C targets, and the need to reduce cardiovascular residual risk. Actually, the innovative cholesterol-lowering drugs available can act on new metabolic pathways involved in LDL-C metabolism. These drugs include enzyme inhibitors, peptides, molecules capable of influencing protein synthesis or gene in the form of antisense oligonucleotides or short interfering RNA, gene therapy, and vaccines.