IMR Press / RCM / Volume 23 / Issue 11 / DOI: 10.31083/j.rcm2311375
Open Access Review
Inclisiran: A New Pharmacological Approach for Hypercholesterolemia
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1 Emergency Department, Clinical and Rehabilitation Cardiology Unit, San Filippo Neri Hospital, ASL Roma 1, 00135 Rome, Italy
2 ANMCO Research Center, Heart Care Foundation, 50121 Florence, Italy
3 Cardiology Department, Interventional Cardiology Unit, Ospedale Santa Corona, 17027 Pietra Ligure, Italy
4 Cardiac Rehabilitation Unit, Rehabilitation Clinic “Villa delle Magnolie", Castel Morrone, 81100 Caserta, Italy
5 CardioThoracic and Vascular Department, San Martino Policlinico Hospital, IRCCS for Oncology and Neurosciences, 16100 Genoa, Italy
6 Department of Biomedical Sciences for Health, IRCCS Ospedale Galeazzi-Sant'Ambrogio, University of Milan, 20161 Milan, Italy
7 Division of Cardiology, Ospedale Santa Maria delle Grazie Pozzuoli, 80078 Napoli, Italy
8 Cardiovascula Department, Clinical and Interventional Cardiology Unit, Istituto Clinico Sant'Ambrogio, 20149 Milan, Italy
9 Dipartimento Cardio-Toraco-Vascolare, U.O.C. Cardiologia, Azienda Ospedaliera San Camillo Forlanini, 00152 Roma, Italy
10 U.O.C. Cardiologia, Ospedale Garibaldi-Nesima, Azienda di Rilievo Nazionale e Alta Specializzazione “Garibaldi", 95122 Catania, Italy
11 De Gasperis Cardio Center, Niguarda Hospital, 20162 Milano, Italy
*Correspondence: doctstefania@hotmail.com (Stefania Angela Di Fusco)
Academic Editor: Brian Tomlinson
Rev. Cardiovasc. Med. 2022, 23(11), 375; https://doi.org/10.31083/j.rcm2311375
Submitted: 22 August 2022 | Revised: 19 September 2022 | Accepted: 21 September 2022 | Published: 3 November 2022
(This article belongs to the Special Issue New Frontiers in Cardiovascular Secondary Prevention)
Copyright: © 2022 The Author(s). Published by IMR Press.
This is an open access article under the CC BY 4.0 license.
Abstract

Therapeutic approaches based on gene silencing technologies represent a new opportunity to manage hypercholesterolemia. Inclisiran is a small interfering RNA that targets proprotein convertase subtilisin/kexin type 9 (PCSK9) mRNA. Clinical studies have demonstrated that inclisiran is effective, safe, and well-tolerated in reducing low-density lipoprotein cholesterol (LDL-C) in patients with familial hypercholesterolemia, atherosclerotic cardiovascular disease, and atherosclerotic cardiovascular disease risk equivalents. A meta-analysis of phase 3 trials demonstrated a 51% reduction in LDL-C levels at 18 months as compared with placebo. Adverse event incidence was found to be comparable in individuals treated with inclisiran and those receiving placebo, though the reactions at the site of injection were more common in patients receiving inclisiran as compared with those receiving placebo. The recommended inclisiran dose is 284 mg administered as a subcutaneous injection to be repeated after three months with a subsequent 6-month maintenance regimen. Overall, since the pharmacological efficacy of inclisiran in LDL-C reduction is comparable to that of monoclonal antibodies against PCSK9, the longer effect duration and the favorable safety profile may favor this newer approach for hypercholesterolemia management.

Keywords
hypercholesterolemia
LDL-cholesterol
inclisiran
siRNA
cardiovascular disease
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