Inclisiran, Low-Density Lipoprotein Cholesterol and Lipoprotein (a)

Dyslipidemia treatment is of major importance in reducing the risk of atherosclerotic cardiovascular disease (ASCVD), which is still the most common cause of death worldwide. During the last decade, a novel lipid-lowering drug category has emerged, i.e., proprotein convertase subtilisin/kexin type 9...

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Main Authors: Niki Katsiki, Michal Vrablik, Maciej Banach, Ioanna Gouni-Berthold
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:Pharmaceuticals
Subjects:
Online Access:https://www.mdpi.com/1424-8247/16/4/577
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author Niki Katsiki
Michal Vrablik
Maciej Banach
Ioanna Gouni-Berthold
author_facet Niki Katsiki
Michal Vrablik
Maciej Banach
Ioanna Gouni-Berthold
author_sort Niki Katsiki
collection DOAJ
description Dyslipidemia treatment is of major importance in reducing the risk of atherosclerotic cardiovascular disease (ASCVD), which is still the most common cause of death worldwide. During the last decade, a novel lipid-lowering drug category has emerged, i.e., proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors. Apart from the two available anti-PCSK9 monoclonal antibodies (alirocumab and evolocumab), other nucleic acid-based therapies that inhibit or “silence” the expression of PCSK9 are being developed. Among them, inclisiran is the first-in-class small interfering RNA (siRNA) against PCSK9 that has been approved by both the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of hypercholesterolemia. Importantly, inclisiran therapy may improve low-density lipoprotein cholesterol (LDL-C) target achievement by offering a prolonged and significant LDL-C-lowering effect with the administration of only two doses per year. The present narrative review discusses the <b>ORION/VICTORION</b> clinical trial program that has been designed to investigate the impact of inclisiran on atherogenic lipoproteins and major adverse cardiac events in different patient populations. The results of the completed clinical trials are presented, focusing on the effects of inclisiran on LDL-C and lipoprotein (a) (Lp(a)) levels as well as on other lipid parameters such as apolipoprotein B and non-high-density lipoprotein cholesterol (non-HDL-C). Ongoing clinical trials with inclisiran are also discussed.
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spelling doaj.art-4fc927d3b68b4dbb931c05e71e9b4a552023-11-17T20:50:54ZengMDPI AGPharmaceuticals1424-82472023-04-0116457710.3390/ph16040577Inclisiran, Low-Density Lipoprotein Cholesterol and Lipoprotein (a)Niki Katsiki0Michal Vrablik1Maciej Banach2Ioanna Gouni-Berthold3Department of Nutritional Sciences and Dietetics, International Hellenic University, 574 00 Thessaloniki, GreeceThird Department of Medicine-Department of Endocrinology and Metabolism of the First Faculty of Medicine, Charles University and General University Hospital, 121 08 Prague, Czech RepublicDepartment of Preventive Cardiology and Lipidology, Medical University of Lodz and Polish Mother’s Memorial Hospital Research Institute, 93-338 Lodz, PolandCenter for Endocrinology, Diabetes and Preventive Medicine, University of Cologne, Faculty of Medicine and University Hospital Cologne, Kerpener Str. 62, 50937 Cologne, GermanyDyslipidemia treatment is of major importance in reducing the risk of atherosclerotic cardiovascular disease (ASCVD), which is still the most common cause of death worldwide. During the last decade, a novel lipid-lowering drug category has emerged, i.e., proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors. Apart from the two available anti-PCSK9 monoclonal antibodies (alirocumab and evolocumab), other nucleic acid-based therapies that inhibit or “silence” the expression of PCSK9 are being developed. Among them, inclisiran is the first-in-class small interfering RNA (siRNA) against PCSK9 that has been approved by both the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of hypercholesterolemia. Importantly, inclisiran therapy may improve low-density lipoprotein cholesterol (LDL-C) target achievement by offering a prolonged and significant LDL-C-lowering effect with the administration of only two doses per year. The present narrative review discusses the <b>ORION/VICTORION</b> clinical trial program that has been designed to investigate the impact of inclisiran on atherogenic lipoproteins and major adverse cardiac events in different patient populations. The results of the completed clinical trials are presented, focusing on the effects of inclisiran on LDL-C and lipoprotein (a) (Lp(a)) levels as well as on other lipid parameters such as apolipoprotein B and non-high-density lipoprotein cholesterol (non-HDL-C). Ongoing clinical trials with inclisiran are also discussed.https://www.mdpi.com/1424-8247/16/4/577inclisiranatherosclerotic cardiovascular diseaseproprotein convertase subtilisin/kexin type 9 inhibitorlow-density lipoprotein cholesterollipoprotein (a)
spellingShingle Niki Katsiki
Michal Vrablik
Maciej Banach
Ioanna Gouni-Berthold
Inclisiran, Low-Density Lipoprotein Cholesterol and Lipoprotein (a)
Pharmaceuticals
inclisiran
atherosclerotic cardiovascular disease
proprotein convertase subtilisin/kexin type 9 inhibitor
low-density lipoprotein cholesterol
lipoprotein (a)
title Inclisiran, Low-Density Lipoprotein Cholesterol and Lipoprotein (a)
title_full Inclisiran, Low-Density Lipoprotein Cholesterol and Lipoprotein (a)
title_fullStr Inclisiran, Low-Density Lipoprotein Cholesterol and Lipoprotein (a)
title_full_unstemmed Inclisiran, Low-Density Lipoprotein Cholesterol and Lipoprotein (a)
title_short Inclisiran, Low-Density Lipoprotein Cholesterol and Lipoprotein (a)
title_sort inclisiran low density lipoprotein cholesterol and lipoprotein a
topic inclisiran
atherosclerotic cardiovascular disease
proprotein convertase subtilisin/kexin type 9 inhibitor
low-density lipoprotein cholesterol
lipoprotein (a)
url https://www.mdpi.com/1424-8247/16/4/577
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AT ioannagouniberthold inclisiranlowdensitylipoproteincholesterolandlipoproteina