Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 24, Issue 7, Pages -Publisher
MDPI
DOI: 10.3390/ijms24076858
Keywords
hypercholesterolemia; PCSK9 inhibitors; siRNA; inclisiran
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Hypercholesterolemia is an undertreated and underdiagnosed disease that plays a crucial role in atherosclerosis development. In recent years, novel lipid-lowering therapies such as inclisiran, a small interfering RNA (siRNA), have been introduced to address this issue. Inclisiran increases the number of LDL receptors on hepatic cells, potentially lowering plasma LDL cholesterol level and showing promising efficacy for future hypolipemic therapies.
Hypercholesterolemia plays a crucial role in the development of atherosclerosis, but it remains an undertreated and underdiagnosed disease. Taking into consideration the high prevalence of lipid disorders, long duration of the asymptomatic course of the disease, life-threatening complications resulting from inaccurate therapy, and stringent treatment goals concerning LDL cholesterol level in the prevention of cardiovascular events, novel lipid-lowering therapies have been introduced in the last few years. In this article, a drug belonging to the group of small interfering RNA (siRNA) called inclisiran is described. It is a novel molecule that increases the number of LDL receptors (LDLRs) on the surface of hepatic cells by preventing the formation of proprotein convertase subtilisin/kexin type 9 (PCSK9) responsible for the degradation of LDLRs. With great potential for lowering plasma LDL cholesterol level, high liver specificity, comfortable dosing regimen, and good tolerance without significant adverse effects, it could play an important part in future hypolipemic therapies.
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