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靶向甘油三酯:载脂蛋白C3和血管生成素样蛋白3抑制剂的兴起

Targeting Triglycerides: The Rise of Apolipoprotein C3 and Angiopoietin-Like Protein 3 Inhibitors.

作者信息

Mansoor Taha, Nambi Vijay, Parikh Sachin, Misra Arunima, Ismayl Mahmoud, Sullivan Claire, Sperling Laurence, Virani Salim S, Rifai Mahmoud Al, Koshy Santhosh K G, Abramov Dmitry, Minhas Abdul Mannan Khan

机构信息

Department of Internal Medicine, Western Michigan University Homer Stryker M.D. School of Medicine, 1000 Oakland Dr, Kalamazoo, MI, 49008, USA.

Department of Medicine, Section of Cardiology, Baylor College of Medicine, Houston, TX, USA.

出版信息

Am J Cardiovasc Drugs. 2025 Jul 12. doi: 10.1007/s40256-025-00748-7.

Abstract

Hypertriglyceridemia has been proposed as a risk factor for atherosclerotic cardiovascular disease (ASCVD). Triglycerides (TG) are viewed as a marker for remnant cholesterol in triglyceride-rich lipoproteins, as this remnant cholesterol has been identified as a causal risk factor for ASCVD. The limited number of effective treatments for elevated TG has fueled the search for novel pharmacotherapy options, and multiple medication classes are being explored. Apolipoprotein C3 (APOC3) and angiopoietin-like protein 3 (ANGPTL3) are among the most promising targets. Several novel agents utilizing these pathways, including olezarsen, plozasiran, and zodasiran, are currently under development for the management of elevated TG, with olezarsen approved in 2024 for the management of familial chylomicronemia syndrome. This comprehensive review provides updated insights into the development of novel hypertriglyceridemia treatments.

摘要

高甘油三酯血症已被提出作为动脉粥样硬化性心血管疾病(ASCVD)的一个危险因素。甘油三酯(TG)被视为富含甘油三酯脂蛋白中残留胆固醇的标志物,因为这种残留胆固醇已被确定为ASCVD的一个因果危险因素。针对升高的TG的有效治疗方法数量有限,这推动了对新型药物治疗选择的探索,目前正在研究多种药物类别。载脂蛋白C3(APOC3)和血管生成素样蛋白3(ANGPTL3)是最有前景的靶点。几种利用这些途径的新型药物,包括olezarsen、plozasiran和zodasiran,目前正在开发用于治疗升高的TG,olezarsen于2024年被批准用于治疗家族性乳糜微粒血症综合征。这篇综述提供了关于新型高甘油三酯血症治疗方法发展的最新见解。

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