In conclusion, an important effort has been made in order to develop new PCSK9 inhibitors, and, in the future, therapies capable to inhibit PCSK9 expression (oligonucleotide antisense), processing (small molecules), and/or interaction with LDLR (mAbs) could represent a real benefit for the treatment of hypercholesterolemia and associated cardiovascular diseases. This evidence concerns the gene PCSK9 and Hypercholesterolemia.