Lipid-lowering interventions targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): an emerging chapter in lipid-lowering therapy

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Abstract

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a serine protease that is mainly expressed in the liver but can also be found in the intestine and kidneys. PCSK9 promotes the degradation of low density lipoprotein receptors (LDLR) by reducing their recycling and targeting the receptors for lysosomal destruction, thereby decreasing the rate of removal of LDL-cholesterol from the circulation. Thus, interventions targeting PCSK9 by reducing its expression may lead to significant reductions of LDL-cholesterol and possibly decrease cardiovascular risk. The present review aims to present and discuss the current clinical and scientific data pertaining to lipid-lowering interventions targeting PCSK9.

Keywords: AT04A vaccine, low density lipoprotein cholesterol, LDL-C, low density lipoprotein receptors, LDLR, proprotein convertase subtilisin/kexin type 9, PCSK9, small interfering RNA, siRNA.

Citation: Kosmas CE, DeJesus E, Morcelo R, Garcia F, Montan PD, Guzman E. Lipid-lowering interventions targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): an emerging chapter in lipid-lowering therapy. Drugs in Context 2017; 6: 212511. DOI: 10.7573/dic.212511

Disclosure and potential conflicts of interest: Constantine E. Kosmas is a member of the Dyslipidemia Speaker Bureau of Amgen, Inc. The International Committee of Medical Journal Editors (ICMJE) Potential Conflicts of Interests form for the authors are available for download at http://www.drugsincontext.com/wp-content/uploads/2017/11/dic.212511-COI.pdf

Copyright: Copyright © 2017 Kosmas CE, DeJesus E, Morcelo R, Garcia F, Montan PD, Guzman E. Distributed under the terms of the Creative Commons License Deed CC BY NC ND 4.0, which allows anyone to copy, distribute, and transmit the article provided it is properly attributed in the manner specified below. No commercial use without permission.

Correct attribution: Copyright © 2017 Kosmas CE, DeJesus E, Morcelo R, Garcia F, Montan PD, Guzman E. https://doi.org/10.7573/dic.212511. Published by Drugs in Context under Creative Commons License Deed CC BY NC ND 4.0.

Article URL: http://www.drugsincontext.com/lipid-lowering-interventions-targeting-proprotein-convertase-subtilisinkexin-type-9-pcsk9-an-emerging-chapter-in-lipid-lowering-therapy

Correspondence: Constantine E Kosmas, MD, PhD, 168-24 Powells Cove Blvd, Beechhurst, NY 11357, USA. cekosmas1@gmail.com

Provenance: invited; externally peer reviewed.

Submitted: 16 October 2017; Peer review comments to author: 20 October 2017; Revised manuscript received: 24 October 2017; Accepted: 24 October 2017; Publication date: 22 November 2017.

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