Research Progress of PCSK9 Inhibitors in the Treatment of Coronary Heart Disease:Mechanisms of Actio

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Abstract

Coronary heart disease (CHD) remains a chronic disease with high morbidity and mortality worldwide, with atherosclerosis serving as its fundamental pathological basis. Lowering lowdensity lipoprotein cholesterol (LDL-C) continues to be one of the most effective strategies for reducing atherosclerosis and preventing cardiovascular events. Although statins and ezetimibe are widely used in clinical practice, a considerable proportion of high-risk patients still fail to achieve optimal LDL-C control or are unable to tolerate conventional lipid-lowering therapy because of adverse effects. The development of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors has provided a novel and highly effective therapeutic strategy for the secondary prevention of CHD.This review systematically summarizes the physiological functions of PCSK9 and its pathological role in the development of CHD. It further integrates recent advances in PCSK9 inhibitor research, with particular emphasis on the mechanisms of action, pharmacokinetic characteristics, clinical outcomes, safety profiles, and clinical evidence of monoclonal antibodies and small interfering RNA (siRNA)-based agents. In addition, future research directions are discussed from the perspectives of treatment accessibility, long-term efficacy, combination therapy, and the development of novel therapeutic targets. Overall, PCSK9 inhibitors have emerged as a highly promising therapeutic option in the management of CHD. However, their clinical value should not be regarded merely as that of more potent lipid-lowering agents, but should also be explored in the contexts of personalized medicine, inflammation modulation, and long-term cardiovascular protection.

Published
2026-07-16
Issue
Issue 1
Section
Issue 1