PCSK9 and Hypercholesterolemia: Therapeutic Approach

Author(s): Milan Obradovic, Bozidarka Zaric, Emina Sudar-Milovanovic, Branislava Ilincic, Edita Stokic, Milan Perovic, Esma R. Isenovic*.

Journal Name: Current Drug Targets

Volume 19 , Issue 9 , 2018

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Graphical Abstract:


Despite the intensive research and progress in modern pharmacotherapy, hypercholesterolemia and related cardiovascular complications remain one of the leading causes of mortality and disability in the modern world. A significant contribution to the treatment of hypercholesterolemia was made by the discovery of proprotein convertase subtilisin/kexin type 9 (PCSK9). This enzyme is responsible for the degradation of the low-density lipoprotein (LDL) receptor (LDLR) found at the surface of the plasma membrane in the liver and directly associated with serum LDL level. Limitations in standard therapy used in the treatment of lipid disorders have led to the development of new drugs, such as an inhibitor of PCSK9. Over the past years, the greatest achievement in discovering the PCSK9 inhibitor was made by designing monoclonal antibodies that disable PCSK9 to bind LDLR and RNA interference to reduce PCSK9 production, but one of the main disadvantages is costeffectiveness. In this review, we will summarize the most recent findings of basic and clinical studies which focus on PCSK9 function, regulation and therapeutic target for the treatment of hypercholesterolemia and associated cardiovascular diseases.

Keywords: PCSK9, PCSK9 and hypercholesterolemia, PCSK9 and CVD, PCSK9 therapy, evolocumab, alirocumab.

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Article Details

Year: 2018
Page: [1058 - 1067]
Pages: 10
DOI: 10.2174/1389450119666171205101401
Price: $58

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