Fitusiran:首个通过降低血浆抗凝血酶水平来治疗血友病的siRNA疗法。

IF 1.9 Q3 PHARMACOLOGY & PHARMACY
Drug Discoveries and Therapeutics Pub Date : 2025-05-09 Epub Date: 2025-04-13 DOI:10.5582/ddt.2025.01031
Daoran Lu, Fangzhou Dou, Jianjun Gao
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引用次数: 0

摘要

血友病是一种由凝血因子缺乏引起的凝血障碍,主要分为血友病a(因子VIII缺乏)和血友病B(因子IX缺乏)。目前的治疗主要依赖于替代疗法,即患者间歇性或预防性地接受凝血因子浓缩治疗,以达到止血或减轻出血风险。尽管这种方法有效,但也存在局限性,包括高成本导致的治疗可及性欠佳,频繁静脉给药降低了患者的依从性,以及出现血浆抑制剂的患者的治疗失败。这些挑战强调需要新的治疗方法来解决未满足的临床需求。2025年3月28日,美国食品和药物管理局(FDA)批准了用于治疗血友病的小干扰RNA (siRNA)药物fitusiran。这种一流的药物通过靶向抗凝血酶来增强凝血酶活性,无论因子VIII/IX缺乏状态或血浆抑制剂存在与否,都证明了泛血友病的疗效。通过开拓抗凝血酶抑制机制,实现持续的治疗作用,促进精确监测方案,fitusiran有可能重新定义血友病治疗模式。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Fitusiran: The first approved siRNA therapy for hemophilia via reducing plasma antithrombin levels.

Hemophilia is a coagulation disorder caused by deficiencies in clotting factors and is primarily classified into hemophilia A (factor VIII deficiency) and hemophilia B (factor IX deficiency). Current treatment relies predominantly on replacement therapy, where patients receive clotting factor concentrates either episodically or prophylactically to achieve hemostasis or mitigate bleeding risks. Despite its efficacy, this approach presents limitations, including suboptimal treatment accessibility due to high costs, reduced patient compliance from frequent intravenous administration, and therapeutic failure in patients developing plasma inhibitors. These challenges underscore the need for novel therapeutics addressing unmet clinical demands. On March 28, 2025, the US Food and Drug Administration (FDA) approved fitusiran, a small interfering RNA (siRNA) therapeutic for hemophilia. This first-in-class agent demonstrates pan-hemophilia efficacy by targeting antithrombin to enhance thrombin activity, irrespective of factor VIII/IX deficiency status or plasma inhibitor presence. By pioneering a mechanism of antithrombin suppression, enabling sustained therapeutic action, and facilitating precision monitoring protocols, fitusiran has the potential to redefine hemophilia treatment paradigms.

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来源期刊
Drug Discoveries and Therapeutics
Drug Discoveries and Therapeutics PHARMACOLOGY & PHARMACY-
CiteScore
3.20
自引率
3.20%
发文量
51
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