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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Data Availability
No datasets were generated or analysed during the current study.
References
Papers of particular interest, published recently, have been highlighted as: • Of importance
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C.M.B. outlined the manuscript and expanded and updated the text and table. A.A. and R.A. drafted the original text. All authors reviewed the manuscript.
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Dr. Ballantyne reports receiving consulting fees and research grants to his institution from Abbott Diagnostics, Akcea, Amgen, Arrowhead, Esperion, Ionis, Novartis, Novo Nordisk, Merck, Regeneron, and Roche Diagnostics. The other authors report that they have no conflict of interest.
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Agarwala, A., Asim, R. & Ballantyne, C.M. Oral PCSK9 Inhibitors. Curr Atheroscler Rep 26, 147–152 (2024). https://doi.org/10.1007/s11883-024-01199-2
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DOI: https://doi.org/10.1007/s11883-024-01199-2