NYMC Faculty Publications

Antihyperlipidemic Therapies Targeting PCSK9

Author Type(s)

Faculty

DOI

10.1097/CRD.0000000000000014

Journal Title

Cardiology in Review

First Page

140

Last Page

146

Document Type

Article

Publication Date

1-1-2014

Department

Medicine

Keywords

Animals, Humans, Hyperlipidemias, Hypolipidemic Agents, Proprotein Convertase 9, Proprotein Convertases, Randomized Controlled Trials as Topic, Serine Endopeptidases, Translational Research, Biomedical

Disciplines

Medicine and Health Sciences

Abstract

Hyperlipidemia is a major cause of cardiovascular disease despite the availability of first-line cholesterol-lowering agents such as statins. A new therapeutic approach to lowering low-density lipoprotein-cholesterol (LDL-C) acts by blocking LDL-receptor degradation by serum proprotein convertase subtilisin kexin 9 (PCSK9). Human monoclonal antibodies that target PCSK9 and its interaction with the LDL receptor are now in clinical trials (REGN727/SAR23653, AMG145, and RN316). These agents are administered by either subcutaneous or intravenous routes, and have been shown to have major LDL-C and apolipoprotein B effects when combined with statins. A phase III clinical trial program evaluating clinical endpoints is now in progress. Other PCSK9-targeted approaches are in early stages of investigation, including natural inhibitors of PCSK9, RNA interference, and antisense inhibitors.

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