Inhibition of proprotein convertase subtilisin/kexin type 9 (PCSK9) A new approach to lipid lowering treatment

E. Klouras, E. Liberopoulos, M. Elisaf



Cardiovascular disease is the single most common cause of death worldwide, hence its prevention constitutes a strategic target for the improvement of life expectancy and quality of life. Statins are an essential element of lipid lowering treatment for decades with undisputable benefits. However, there are patients who cannot tolerate statins or cannot achieve the goal of lipid lowering treatment only by statins. Studying people with genetically high or low cholesterol levels and the analysis of their genome has led to the discovery of the proprotein convertase subtilisin/kexin type 9 (PCSK9) protein. The important contribution of the PCSK9 to the catabolism of the low density lipoprotein (LDL) receptor renders it as the main regulator in cholesterol metabolism, thus making it an attractive target for the development of new drugs. Inhibiting the PCSK9 protein by using monoclonal antibodies is the most advanced approach, given that it achieves an additional reduction of LDL cholesterol by 50-60%, while having an excellent safety profile. While waiting for more studies to be completed, it seems that we are witnessing a revolution in the fields of lipid lowering treatment and prevention of cardiovascular disease.

Keywords: protein PCSK9, LDL cholesterol, dyslipidemia, monoclonal antibody