Oral PCSK9 Inhibitors

被引：9

作者：

Agarwala, Anandita ^{[1
]}

Asim, Ramsha ^{[2
]}

Ballantyne, Christie M. ^{[3
,4
]}

机构：

[1] Baylor Scott & White Hlth Heart Hosp Baylor Plano, Ctr Cardiovasc Dis Prevent, Cardiovasc Div, Plano, TX USA

[2] Kansas City Univ, Coll Osteopath Med, Kansas City, MO USA

[3] Baylor Coll Med, Dept Med, Sect Cardiovasc Res, One Baylor Plaza,MS BCM285, Houston, TX 77030 USA

[4] Baylor Coll Med, Ctr Cardiometab Dis Prevent, Dept Med, One Baylor Plaza,MS BCM285, Houston, TX 77030 USA

来源：

CURRENT ATHEROSCLEROSIS REPORTS | 2024年 / 26卷 / 05期

关键词：

Lipid-lowering therapy; PCSK9; inhibitors; Drug development; LOW LDL; MUTATIONS; RECEPTOR;

D O I：

10.1007/s11883-024-01199-2

中图分类号：

R6 [外科学];

学科分类号：

1002 ; 100210 ;

摘要：

Purpose of ReviewIn 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 FindingsThe 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.SummaryClinical 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.

引用

页码：147 / 152

页数：6

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