Center for Cardiovascular Disease Prevention, Cardiovascular Division, Baylor Scott and White Health Heart Hospital Baylor Plano, Plano, TX, USA.
College of Osteopathic Medicine, Kansas City University, Kansas City, MO, USA.
Curr Atheroscler Rep. 2024 May;26(5):147-152. doi: 10.1007/s11883-024-01199-2. Epub 2024 Mar 27.
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.
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.
在本次综述中，我们将讨论 MK-0616 的早期临床研究数据，并总结其他口服前蛋白转化酶枯草溶菌素 9（PCSK9）抑制剂的临床试验。
单克隆抗体注射抑制 PCSK9 的成功推动了针对 PCSK9 的其他治疗方法的发展，包括口服制剂，其中最先进的是 MK-0616。MK-0616 是一种新型的、口服的大环肽，可与 PCSK9 结合并抑制 PCSK9 与 LDL 受体结合，从而降低血浆 LDL-C 水平。MK-0616 的安全性和疗效的临床试验数据令人鼓舞，报告称其 LDL-C 降低的疗效可与注射用 PCSK9 抑制剂相媲美。正在进行和未来的口服 PCSK9 抑制剂研究将评估这些药物的安全性、疗效和有效性，以及它们在预防心血管疾病事件中的潜在作用。
