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Arch Hellen Med, 32(1), January-February 2015, 77-84


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

E. Klouras, E. Liberopoulos, M. Elisaf
Department of Internal Medicine, University of Ioannina, Medical School, Ioannina, Greece

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 have been an essential element of lipid lowering treatment for decades, with undisputable results. Some patients, however, either cannot tolerate statins or cannot achieve the goal of lipid lowering by statins alone. The study of people with genetically high or low cholesterol levels and 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 in the catabolism of the low density lipoprotein (LDL) receptor renders it the main regulator in the metabolism of cholesterol, thus making it an attractive target for the development of new lipid lowering drugs. Inhibition of the PCSK9 protein by the use of monoclonal antibodies is the most advanced approach. This achieves an additional reduction of LDL cholesterol by 50% while having a good safety profile. Pending the completion of further studies, it already appears that we are witnessing a revolution in the field of lipid lowering treatment and prevention of cardiovascular disease.

Key words: Dyslipidemia, LDL cholesterol, Monoclonal antibody, Protein PCSK9.

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