The effects of proprotein convertase subtilisin/kexin type 9 inhibitors on lipid metabolism and cardiovascular function

Patchareeya Amput; Christian McSweeney; Siripong Palee; Arintaya Phrommintikul; Siriporn C Chattipakorn; Nipon Chattipakorn

doi:10.1016/j.biopha.2018.10.138

The effects of proprotein convertase subtilisin/kexin type 9 inhibitors on lipid metabolism and cardiovascular function

Biomed Pharmacother. 2019 Jan:109:1171-1180. doi: 10.1016/j.biopha.2018.10.138. Epub 2018 Nov 6.

Authors

Patchareeya Amput¹, Christian McSweeney², Siripong Palee³, Arintaya Phrommintikul³, Siriporn C Chattipakorn⁴, Nipon Chattipakorn⁵

Affiliations

¹ Cardiac Electrophysiology Research and Training Center, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand; Cardiac Electrophysiology Unit, Department of Physiology, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand; Center of Excellence in Cardiac Electrophysiology Research, Chiang Mai University, Chiang Mai 50200, Thailand.
² Cardiac Electrophysiology Research and Training Center, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand; School of Biological Sciences, Faculty of Biology Medicine and Health, The University of Manchester, United Kingdom.
³ Cardiac Electrophysiology Research and Training Center, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand; Center of Excellence in Cardiac Electrophysiology Research, Chiang Mai University, Chiang Mai 50200, Thailand.
⁴ Cardiac Electrophysiology Research and Training Center, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand; Center of Excellence in Cardiac Electrophysiology Research, Chiang Mai University, Chiang Mai 50200, Thailand; Department of Oral Biology and Diagnostic Sciences, Faculty of Dentistry, Chiang Mai University, Chiang Mai 50200, Thailand.
⁵ Cardiac Electrophysiology Research and Training Center, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand; Cardiac Electrophysiology Unit, Department of Physiology, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand; Center of Excellence in Cardiac Electrophysiology Research, Chiang Mai University, Chiang Mai 50200, Thailand. Electronic address: nchattip@gmail.com.

PMID: 30551367
DOI: 10.1016/j.biopha.2018.10.138

Abstract

Low density lipoprotein cholesterol (LDL-C) is a well-established risk factor for cardiovascular disease. Although there are several developed lipid lowering drugs such as statins and fenofibrates, many patients do not achieve an adequate response. Recently, proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors have been developed as a new therapeutic strategy for cholesterol regulation. PCSK9 binds to low density lipoprotein receptors (LDLR) and initiates LDLR degradation, elevating LDL-C. Therefore, PCSK9 inhibition could exert beneficial effects on cardiovascular disease outcomes. This review comprehensively summarizes and discusses the effects of PCSK9 inhibitors on lipid metabolism and cardiovascular function comparatively with current lipid lowering drugs. This review also details essential information regarding the cardiovascular benefits of PCSK9 inhibition which could encourage further clinical studies.

Keywords: Cardiovascular function; Cholesterol; Heart; Low density lipoprotein receptor; Proprotein convertase subtilisin/kexin type 9 inhibitor.

Publication types

Review

MeSH terms

Animals
Cardiovascular Diseases / drug therapy*
Cardiovascular System / drug effects*
Humans
Lipid Metabolism / drug effects*
PCSK9 Inhibitors*
Subtilisins / antagonists & inhibitors*

Substances

PCSK9 Inhibitors
Subtilisins