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Pharmacological Strategies beyond Statins: Ezetimibe and PCSK9 Inhibitors

Dyslipidemia, highly elevated, low-density lipoprotein (LDL) cholesterol, is a major cardiovascular risk factor. Statins have been proven to effectively reduce the risk of atherosclerotic cardiovascular disease (ASCVD) and are recommended as a first-line therapy for the primary and secondary prevent...

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Autores principales: Choi, Jah Yeon, Na, Jin Oh
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Korean Society of Lipidology and Atherosclerosis 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7379114/
https://www.ncbi.nlm.nih.gov/pubmed/32821708
http://dx.doi.org/10.12997/jla.2019.8.2.183
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author Choi, Jah Yeon
Na, Jin Oh
author_facet Choi, Jah Yeon
Na, Jin Oh
author_sort Choi, Jah Yeon
collection PubMed
description Dyslipidemia, highly elevated, low-density lipoprotein (LDL) cholesterol, is a major cardiovascular risk factor. Statins have been proven to effectively reduce the risk of atherosclerotic cardiovascular disease (ASCVD) and are recommended as a first-line therapy for the primary and secondary prevention of ASCVD. However, statins may not be sufficient in decreasing LDL cholesterol levels and pose a significant on-treatment residual risk of major cardiovascular events (i.e., residual cholesterol risk) according to meta-analyses of statin trials. Current guidelines for cholesterol management to achieve additional LDL cholesterol reduction and reduce ASCVD risk recommend two hyperlipidemic agents besides statins. Use of ezetimibe, a cholesterol absorption inhibitor, leads to additional LCL cholesterol reduction and decreased ASCVD risk, when added to statin therapy, without raising significant safety concerns. Furthermore, in combination with a mild-to-moderate statin intensity, ezetimibe is used in situations of statin-associated adverse effects such as myalgia and the combination therapy is relatively safer. Monoclonal antibody of proprotein convertase subtilisin/kexin type 9 (PCSK9), alirocumab, and evolocumab, have been approved to lower LDL cholesterol level. While there are drawbacks to the use of PCSK9 inhibitors, including high cost and adverse events such as injection site reaction, they significantly decreased serum LDL cholesterol levels and thereby ASCVD risks when added to maximally tolerated statin therapy.
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spelling pubmed-73791142020-08-18 Pharmacological Strategies beyond Statins: Ezetimibe and PCSK9 Inhibitors Choi, Jah Yeon Na, Jin Oh J Lipid Atheroscler Review Dyslipidemia, highly elevated, low-density lipoprotein (LDL) cholesterol, is a major cardiovascular risk factor. Statins have been proven to effectively reduce the risk of atherosclerotic cardiovascular disease (ASCVD) and are recommended as a first-line therapy for the primary and secondary prevention of ASCVD. However, statins may not be sufficient in decreasing LDL cholesterol levels and pose a significant on-treatment residual risk of major cardiovascular events (i.e., residual cholesterol risk) according to meta-analyses of statin trials. Current guidelines for cholesterol management to achieve additional LDL cholesterol reduction and reduce ASCVD risk recommend two hyperlipidemic agents besides statins. Use of ezetimibe, a cholesterol absorption inhibitor, leads to additional LCL cholesterol reduction and decreased ASCVD risk, when added to statin therapy, without raising significant safety concerns. Furthermore, in combination with a mild-to-moderate statin intensity, ezetimibe is used in situations of statin-associated adverse effects such as myalgia and the combination therapy is relatively safer. Monoclonal antibody of proprotein convertase subtilisin/kexin type 9 (PCSK9), alirocumab, and evolocumab, have been approved to lower LDL cholesterol level. While there are drawbacks to the use of PCSK9 inhibitors, including high cost and adverse events such as injection site reaction, they significantly decreased serum LDL cholesterol levels and thereby ASCVD risks when added to maximally tolerated statin therapy. Korean Society of Lipidology and Atherosclerosis 2019-09 2019-09-17 /pmc/articles/PMC7379114/ /pubmed/32821708 http://dx.doi.org/10.12997/jla.2019.8.2.183 Text en Copyright © 2019 The Korean Society of Lipid and Atherosclerosis. https://creativecommons.org/licenses/by-nc/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (https://creativecommons.org/licenses/by-nc/4.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review
Choi, Jah Yeon
Na, Jin Oh
Pharmacological Strategies beyond Statins: Ezetimibe and PCSK9 Inhibitors
title Pharmacological Strategies beyond Statins: Ezetimibe and PCSK9 Inhibitors
title_full Pharmacological Strategies beyond Statins: Ezetimibe and PCSK9 Inhibitors
title_fullStr Pharmacological Strategies beyond Statins: Ezetimibe and PCSK9 Inhibitors
title_full_unstemmed Pharmacological Strategies beyond Statins: Ezetimibe and PCSK9 Inhibitors
title_short Pharmacological Strategies beyond Statins: Ezetimibe and PCSK9 Inhibitors
title_sort pharmacological strategies beyond statins: ezetimibe and pcsk9 inhibitors
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7379114/
https://www.ncbi.nlm.nih.gov/pubmed/32821708
http://dx.doi.org/10.12997/jla.2019.8.2.183
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