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Review
. 2024 May;26(5):147-152.
doi: 10.1007/s11883-024-01199-2. Epub 2024 Mar 27.

Oral PCSK9 Inhibitors

Anandita Agarwala  1 , Ramsha Asim  2 , Christie M Ballantyne  3
Affiliations
Review

Oral PCSK9 Inhibitors

Anandita Agarwala et al. Curr Atheroscler Rep. 2024 May.

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. 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.

Keywords: Drug development; Lipid-lowering therapy; PCSK9 inhibitors.

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References

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