Oral agents for lowering lipoprotein(a).

IF 3.8 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Current opinion in lipidology Pub Date : 2024-12-01 Epub Date: 2024-09-25 DOI:10.1097/MOL.0000000000000953
Stephen J Nicholls, Adam J Nelson, Laura F Michael
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Abstract

Purpose of review: To review the development of oral agents to lower Lp(a) levels as an approach to reducing cardiovascular risk, with a focus on recent advances in the field.

Recent findings: Extensive evidence implicates Lp(a) in the causal pathway of atherosclerotic cardiovascular disease and calcific aortic stenosis. There are currently no therapies approved for lowering of Lp(a). The majority of recent therapeutic advances have focused on development of injectable agents that target RNA and inhibit synthesis of apo(a). Muvalaplin is the first, orally administered, small molecule inhibitor of Lp(a), which acts by disrupting binding of apo(a) and apoB, in clinical development. Nonhuman primate and early human studies have demonstrated the ability of muvalaplin to produce dose-dependent lowering of Lp(a). Ongoing clinical trials will evaluate the impact of muvalaplin in high cardiovascular risk and will ultimately need to determine whether this strategy lowers the rate of cardiovascular events.

Summary: Muvalaplin is the first oral agent, developed to lower Lp(a) levels. The ability of muvalaplin to reduce cardiovascular risk remains to be investigated, in order to determine whether it will be a useful agent for the prevention of cardiovascular disease.

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降低脂蛋白(a)的口服药物。
综述目的:回顾降低脂蛋白(a)水平的口服药物的开发情况,以此作为降低心血管风险的一种方法,重点关注该领域的最新进展:大量证据表明,脂蛋白(a)是动脉粥样硬化性心血管疾病和钙化性主动脉瓣狭窄的诱因。目前还没有获准用于降低脂蛋白(a)的疗法。最近的治疗进展大多集中在开发以 RNA 为靶点、抑制载脂蛋白(a)合成的注射剂上。Muvalaplin是第一种口服小分子脂蛋白(a)抑制剂,它通过破坏载脂蛋白(a)和载脂蛋白B的结合发挥作用,目前正处于临床开发阶段。非人灵长类动物和早期人体研究表明,muvalaplin 能够产生剂量依赖性降低脂蛋白(a)。目前正在进行的临床试验将评估muvalaplin对心血管高危人群的影响,并最终确定这一策略是否能降低心血管事件的发生率。摘要:Muvalaplin是首个为降低脂蛋白(a)水平而开发的口服药物。Muvalaplin降低心血管风险的能力仍有待研究,以确定它是否能成为预防心血管疾病的有效药物。
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来源期刊
Current opinion in lipidology
Current opinion in lipidology 医学-内分泌学与代谢
CiteScore
6.70
自引率
4.50%
发文量
64
审稿时长
6-12 weeks
期刊介绍: With its easy-to-digest reviews on important advances in world literature, Current Opinion in Lipidology offers expert evaluation on a wide range of topics from six key disciplines including nutrition and metabolism, genetics and molecular biology, and hyperlipidaemia and cardiovascular disease. Published bimonthly, each issue covers in detail the most pertinent advances in these fields from the previous year. This is supplemented by a section of Bimonthly Updates, which deliver an insight into new developments at the cutting edge of the disciplines covered in the journal.
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