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Inclisiran-new hope in the management of lipid disorders?

Dyrbuś, K, Mariusz, G, Penson, P, Ray, KK and Banach, M (2019) Inclisiran-new hope in the management of lipid disorders? Journal of Clinical Lipidology, 14 (1). pp. 16-27. ISSN 1876-4789

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Drugs reducing plasma concentrations of apolipoprotein-B (ApoB) containing lipoproteins have been demonstrated to reduce the risk of cardiovascular disease (CVD) in both primary and secondary prevention. Despite the demonstrated efficacy of statins and ezetimibe on low-density lipoprotein (LDL) concentration and long-term CVD risk, a large number of patients do not achieve their therapeutic goals. The introduction of monoclonal antibodies against proprotein convertase subtilisin/kexin type 9 (PCSK9) protein was a milestone in the treatment of lipid disorders, as their administration leads to unprecedentedly low LDL-C concentrations. Inclisiran represents an entirely new mechanism of PSCK9 protein inhibition in hepatocytes, targeting the messenger RNA (mRNA) for PCSK9. Its administration is necessary only every 3-6 months, which is an essential advantage over statin and monoclonal antibody therapy. The infrequent administration regimen can increase the number of patients who maintain their therapeutic goals, especially in patients struggling to comply with daily or biweekly pharmacotherapy.

Preclinical studies and Phase I and Phase II clinical trials of inclisiran have demonstrated its tolerability and efficacy in promoting long-term reduction of both PCSK9 protein and LDL-C. The efficacy and safety of inclisiran will continue to be assessed in ongoing and forthcoming trials on larger patient groups. If the results of these trials reflect previously published data, they will add further evidence that inclisiran might be a revolutionary new tool in the pharmacological management of plasma lipids. This review summarizes the currently available literature data on inclisiran with respect to its mechanism of action, effectiveness and safety as a lipid-lowering drug for CVD prevention.

Item Type: Article
Uncontrolled Keywords: 1101 Medical Biochemistry and Metabolomics, 1102 Cardiorespiratory Medicine and Haematology
Subjects: Q Science > QH Natural history > QH301 Biology
R Medicine > RM Therapeutics. Pharmacology
Divisions: Pharmacy & Biomolecular Sciences
Publisher: Elsevier
Date Deposited: 14 Nov 2019 09:18
Last Modified: 04 Sep 2021 08:27
DOI or ID number: 10.1016/j.jacl.2019.11.001
URI: https://researchonline.ljmu.ac.uk/id/eprint/11766
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