脂蛋白(a)在动脉粥样硬化性心血管疾病中的作用:当前和新兴疗法综述。

IF 2.9 3区 医学 Q2 PHARMACOLOGY & PHARMACY
Pharmacotherapy Pub Date : 2023-10-01 Epub Date: 2023-07-26 DOI:10.1002/phar.2851
Ibrahim S Alhomoud, Azita Talasaz, Anurag Mehta, Michael S Kelly, Evan M Sisson, John D Bucheit, Roy Brown, Dave L Dixon
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引用次数: 2

摘要

脂蛋白(a)或Lp(a)在结构上类似于低密度脂蛋白(LDL),但不同之处在于它含有糖蛋白载脂蛋白(a)[apo(a)]。由于其促血栓形成和促炎特性,Lp(a)是动脉粥样硬化性心血管疾病(ASCVD)和主动脉瓣狭窄的独立危险因素。Lp(a)水平是由基因决定的,据估计,全球20%-25%的人口Lp(b)水平≥50 mg/dL(或≥125 nmol/L)。饮食和生活方式干预对Lp(a)水平几乎没有影响。脂蛋白单采是唯一被批准的治疗Lp(a)升高的方法,但对患者来说是时间密集型的,效果也不高。降低Lp(a)水平及其相关风险的药理学方法具有重要意义;然而,目前可用的降脂疗法在降低Lp(a)水平方面的有效性有限。尽管他汀类药物是降低低密度脂蛋白胆固醇水平的一线药物,但它们适度增加了Lp(a)水平,并且尚未显示出改变Lp(a)介导的ASCVD风险。Alirocumab、evolocomab和inclisiran可将Lp(a)水平降低20-25%,但这种降低对Lp(a)介导的ASCVD风险的临床意义尚不确定。烟酸还降低Lp(a)水平;然而,其在减轻Lp(a)介导的ASCVD风险方面的有效性尚不清楚,其副作用限制了其利用。关于何时筛查和如何管理Lp(a)升高的个人的建议,在国家和国际指南以及科学声明之间存在很大差异。三种针对Lp(a)的研究化合物,包括小干扰RNA(siRNA)制剂(olpasiran,SLN360)和反义寡核苷酸(pelacarsen),正处于不同的开发阶段。这些化合物阻断信使核糖核酸(信使核糖核酸)翻译成载脂蛋白(a),载脂蛋白是Lp(a)的关键结构成分,从而显著减少肝脏中Lp(b)的合成。本综述的目的是描述目前筛查和管理Lp(a)升高的建议,描述目前可用的降脂疗法对Lp(b)水平的影响,并深入了解针对Lp(c)的新兴疗法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Role of lipoprotein(a) in atherosclerotic cardiovascular disease: A review of current and emerging therapies.

Lipoprotein(a), or Lp(a), is structurally like low-density lipoprotein (LDL) but differs in that it contains glycoprotein apolipoprotein(a) [apo(a)]. Due to its prothrombotic and proinflammatory properties, Lp(a) is an independent risk factor for atherosclerotic cardiovascular disease (ASCVD) and aortic valve stenosis. Lp(a) levels are genetically determined, and it is estimated that 20%-25% of the global population has an Lp(a) level ≥50 mg/dL (or ≥125 nmol/L). Diet and lifestyle interventions have little to no effect on Lp(a) levels. Lipoprotein apheresis is the only approved treatment for elevated Lp(a) but is time-intensive for the patient and only modestly effective. Pharmacological approaches to reduce Lp(a) levels and its associated risks are of significant interest; however, currently available lipid-lowering therapies have limited effectiveness in reducing Lp(a) levels. Although statins are first-line agents to reduce LDL cholesterol levels, they modestly increase Lp(a) levels and have not been shown to change Lp(a)-mediated ASCVD risk. Alirocumab, evolocumab, and inclisiran reduce Lp(a) levels by 20-25%, yet the clinical implications of this reduction for Lp(a)-mediated ASCVD risk are uncertain. Niacin also lowers Lp(a) levels; however, its effectiveness in mitigating Lp(a)-mediated ASCVD risk remains unclear, and its side effects have limited its utilization. Recommendations for when to screen and how to manage individuals with elevated Lp(a) vary widely between national and international guidelines and scientific statements. Three investigational compounds targeting Lp(a), including small interfering RNA (siRNA) agents (olpasiran, SLN360) and an antisense oligonucleotide (pelacarsen), are in various stages of development. These compounds block the translation of messenger RNA (mRNA) into apo(a), a key structural component of Lp(a), thereby substantially reducing Lp(a) synthesis in the liver. The purpose of this review is to describe current recommendations for screening and managing elevated Lp(a), describe the effects of currently available lipid-lowering therapies on Lp(a) levels, and provide insight into emerging therapies targeting Lp(a).

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来源期刊
Pharmacotherapy
Pharmacotherapy 医学-药学
CiteScore
7.80
自引率
2.40%
发文量
93
审稿时长
4-8 weeks
期刊介绍: Pharmacotherapy is devoted to publication of original research articles on all aspects of human pharmacology and review articles on drugs and drug therapy. The Editors and Editorial Board invite original research reports on pharmacokinetic, bioavailability, and drug interaction studies, clinical trials, investigations of specific pharmacological properties of drugs, and related topics.
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