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27-03-2024 | PCSK9 Inhibitor | Review

Oral PCSK9 Inhibitors

Authors: Anandita Agarwala, Ramsha Asim, Christie M. Ballantyne

Published in: Current Atherosclerosis Reports

Abstract

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.

Summary

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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Title: Oral PCSK9 Inhibitors
Authors: Anandita Agarwala
Ramsha Asim
Christie M. Ballantyne
Publication date: 27-03-2024
Publisher: Springer US
Keyword: PCSK9 Inhibitor
Published in: Current Atherosclerosis Reports
Print ISSN: 1523-3804
Electronic ISSN: 1534-6242
DOI: https://doi.org/10.1007/s11883-024-01199-2

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