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Inclisiran对心血管健康的影响:作用机制、疗效及未来展望综述

Inclisiran in Cardiovascular Health: A Review of Mechanisms, Efficacy, and Future Prospects.

作者信息

Huang Fanke, Dai Qiuting, Zhou Yilu, Guan Jing, Wu Jingjing, Dong Yanyan, Lv Jianfeng

机构信息

Department of Cardiovascular Medicine, Renhe Hospital Affiliated to Three Gorges University, Yichang, Hubei, China.

出版信息

Med Sci Monit. 2025 Apr 13;31:e946439. doi: 10.12659/MSM.946439.

DOI:10.12659/MSM.946439
PMID:40221828
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12005059/
Abstract

Dyslipidemia is a significant risk factor for cardiovascular disease, and managing low-density lipoprotein cholesterol levels is a crucial strategy for both the prevention and treatment of cardiovascular disease. The active ingredient in the novel lipid-lowering drug, inclisiran, is a new type of small interfering RNA that primarily regulates blood lipid levels by inhibiting the synthesis of proprotein convertase subtilisin type 9 (PCSK9). Enhanced lipid-lowering effects can be achieved following 3 administrations. This article summarizes inclisiran's mechanism of action, efficacy, safety, current research hotspots, clinical applications, and future development prospects, based on the latest literature and research advancements. Through comparative analysis with traditional lipid-lowering drugs, we conclude that inclisiran has promising application prospects and market potential, as it can complement traditional statin therapies to enhance lipid-lowering efficiency. This not only provides convenience to patients but also improves treatment compliance. Its safety profile alleviates patients' concerns and mitigates the impact of negative emotions on their condition. Additionally, the potential applications of inclisiran in oncology have been identified. However, inclisiran also presents certain limitations and challenges. For instance, its long-term safety and efficacy require further investigation in future studies, and its high cost can restrict its widespread adoption and promotion. Furthermore, additional clinical evidence is needed to evaluate its synergistic or antagonistic effects when used in conjunction with other medications.

摘要

血脂异常是心血管疾病的重要危险因素,控制低密度脂蛋白胆固醇水平是预防和治疗心血管疾病的关键策略。新型降脂药物英克西兰的活性成分是一种新型小干扰RNA,主要通过抑制前蛋白转化酶枯草溶菌素9型(PCSK9)的合成来调节血脂水平。给药3次后可增强降脂效果。本文基于最新文献和研究进展,总结了英克西兰的作用机制、疗效、安全性、当前研究热点、临床应用及未来发展前景。通过与传统降脂药物的对比分析,我们得出结论:英克西兰具有广阔的应用前景和市场潜力,因为它可以补充传统他汀类疗法以提高降脂效率。这不仅为患者提供了便利,还提高了治疗依从性。其安全性减轻了患者的担忧,减轻了负面情绪对病情的影响。此外,还确定了英克西兰在肿瘤学方面的潜在应用。然而,英克西兰也存在一定的局限性和挑战。例如,其长期安全性和疗效需要在未来研究中进一步探讨,其高昂的成本可能会限制其广泛应用和推广。此外,还需要更多临床证据来评估其与其他药物联合使用时的协同或拮抗作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdd6/12005059/5d785d4ca310/medscimonit-31-e946439-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdd6/12005059/f0607826290a/medscimonit-31-e946439-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdd6/12005059/5d785d4ca310/medscimonit-31-e946439-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdd6/12005059/f0607826290a/medscimonit-31-e946439-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdd6/12005059/f35846c84892/medscimonit-31-e946439-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdd6/12005059/5d785d4ca310/medscimonit-31-e946439-g003.jpg

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本文引用的文献

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Drugs Context. 2024 Nov 28;13. doi: 10.7573/dic.2023-12-3. eCollection 2024.
2
Zodasiran, an RNAi Therapeutic Targeting ANGPTL3, for Mixed Hyperlipidemia.Zodasiran,一种针对 ANGPTL3 的 RNAi 治疗药物,用于治疗混合性高脂血症。
N Engl J Med. 2024 Sep 12;391(10):913-925. doi: 10.1056/NEJMoa2404147. Epub 2024 May 29.
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Inclisiran administration potently and durably lowers LDL-C over an extended-term follow-up: the ORION-8 trial.依洛尤单抗治疗强效且持久降低 LDL-C:ORION-8 试验。
Cardiovasc Res. 2024 Oct 14;120(12):1400-1410. doi: 10.1093/cvr/cvae109.
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RNA interference in the era of nucleic acid therapeutics.核酸治疗时代的RNA干扰
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Efficacy and Safety of Inclisiran in Asian Patients: Results From ORION-18.inclisiran在亚洲患者中的疗效与安全性:ORION-18研究结果
JACC Asia. 2023 Nov 14;4(2):123-134. doi: 10.1016/j.jacasi.2023.09.006. eCollection 2024 Feb.
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Prevalence and correlates of severe anxiety in patients with first hospitalization for major depressive disorder combined with dyslipidemia: a large sample cross-sectional study.首次因重度抑郁症合并血脂异常住院患者中重度焦虑的患病率及其相关因素:一项大样本横断面研究
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Predicting Clinical Pharmacokinetics/Pharmacodynamics and Impact of Organ Impairment on siRNA-Based Therapeutics Using a Mechanistic Physiologically-Based Pharmacokinetic-Pharmacodynamic Model.利用基于机制的生理药代动力学-药效动力学模型预测基于 siRNA 的治疗药物的临床药代动力学/药效动力学和器官损伤的影响。
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