口服 PCSK9 抑制剂。

IF 5.7 2区 医学 Q1 PERIPHERAL VASCULAR DISEASE Current Atherosclerosis Reports Pub Date : 2024-05-01 Epub Date: 2024-03-27 DOI:10.1007/s11883-024-01199-2
Anandita Agarwala, Ramsha Asim, Christie M Ballantyne
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引用次数: 0

摘要

综述的目的:在这篇综述中,我们将讨论 MK-0616 早期临床研究的数据,并总结其他口服丙蛋白转换酶亚基酶/kexin 9 型(PCSK9)抑制剂的临床试验:单克隆抗体注射抑制 PCSK9 的成功推动了更多针对 PCSK9 的疗法的开发,包括口服制剂,其中最先进的是 MK-0616。MK-0616 是一种新型口服大环肽,能与 PCSK9 结合,抑制 PCSK9 与低密度脂蛋白受体的结合,从而降低血浆中的低密度脂蛋白胆固醇水平。有关 MK-0616 安全性和疗效的临床试验数据前景看好,其降低低密度脂蛋白胆固醇的疗效与注射用 PCSK9 抑制剂不相上下。正在进行的和未来的口服 PCSK9 抑制剂开发研究将评估这些药物的安全性、有效性和有效性,以及它们在预防心血管疾病事件中的潜在作用。
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Oral PCSK9 Inhibitors.

Purpose of review: In this review, we will discuss the data from early clinical studies of MK-0616 and summarize clinical trials of other oral proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors.

Recent findings: The success of PCSK9 inhibition with monoclonal antibody injections has fueled the development of additional therapies targeting PCSK9, including oral formulations, the most advanced of which is MK-0616. MK-0616 is a novel, orally administered macrocyclic peptide that binds to PCSK9 and inhibits binding of PCSK9 to the LDL receptor, thereby decreasing plasma levels of LDL-C. Clinical trial data on the safety and efficacy of MK-0616 are promising and report LDL-C-lowering efficacy comparable to that provided by injectable PCSK9 inhibitors. Ongoing and future studies of oral PCSK9 inhibitors in development will evaluate the safety, efficacy, and effectiveness of these agents and their potential role in preventing cardiovascular disease events.

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来源期刊
CiteScore
9.00
自引率
3.40%
发文量
87
审稿时长
6-12 weeks
期刊介绍: The aim of this journal is to systematically provide expert views on current basic science and clinical advances in the field of atherosclerosis and highlight the most important developments likely to transform the field of cardiovascular prevention, diagnosis, and treatment. We accomplish this aim by appointing major authorities to serve as Section Editors who select leading experts from around the world to provide definitive reviews on key topics and papers published in the past year. We also provide supplementary reviews and commentaries from well-known figures in the field. An Editorial Board of internationally diverse members suggests topics of special interest to their country/region and ensures that topics are current and include emerging research.
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