Safety of PCSK9 inhibitors

PCSK9 Evolocumab公司 阿利罗库单抗 可欣 耐受性 低密度脂蛋白受体 前蛋白转化酶 医学 药理学 他汀类 胆固醇 内科学 不利影响 载脂蛋白B 脂蛋白 载脂蛋白A1
作者
Grzegorz Grześk,Bednarska Dorota,Łukasz Wołowiec,Anna Wołowiec,Joanna Osiak,Mariusz Kozakiewicz,Joanna Banach
出处
期刊:Biomedicine & Pharmacotherapy [Elsevier BV]
卷期号:156: 113957-113957 被引量:35
标识
DOI:10.1016/j.biopha.2022.113957
摘要

annually in Europe, 4 million people die from cardiovascular diseases, the main cause of which is atherosclerosis. In order to slow down the development of atherosclerotic plaques, the main therapeutic goal is to lower LDL cholesterol (LDL-C) level. Undoubtedly, statins are the basis of lipid-lowering therapy for many years. However, a European study shows that only 43% of statin-taking patients achieved their LDL-C targets. PCSK9 inhibitors are a new group of lipid-lowering drugs whose main point of action is the protein discovered in 2003 - the PCSK9 (proprotein convertase subtilisin/kexin 9). This protein is responsible for reducing the density of LDL receptors on the surface of hepatocytes, which increases the value of LDL-C. The discovery of this protein was soon after the basis for the start of research, thanks to which three monoclonal antibodies against PCSK9 were developed - evolocumab, alirocumab, bococizumab - and inclisiran, an inhibitor of PCSK9 synthesis in the liver. In addition to the mechanism of action of PCSK9 inhibitors, resulting in lowering LDL-C level, a number of pleiotropic mechanisms have also been identified, including effects on metabolic processes and inflammation. Until the registration and introduction of above-mentioned drugs into everyday clinical practice, many studies were carried out, in which, in addition to assessing the effectiveness of treatment, the safety and tolerability of the drug were also examined. The purpose of this review is to summarize information on the safety profile of PCSK9 inhibitors, which may help in making therapeutic decision.
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