危子怡, 韩蕊, 谢伊铭, 李芳, 张凡. 靶向Nav1.8的镇痛药物研发进展J. 药学学报, 2026, 61(2): 403-416. DOI: 10.16438/j.0513-4870.2025-0166
引用本文: 危子怡, 韩蕊, 谢伊铭, 李芳, 张凡. 靶向Nav1.8的镇痛药物研发进展J. 药学学报, 2026, 61(2): 403-416. DOI: 10.16438/j.0513-4870.2025-0166
WEI Zi-yi, HAN Rui, XIE Yi-ming, LI Fang, ZHANG Fan. Advances in the development of Nav1.8-targeted analgesicsJ. Acta Pharmaceutica Sinica, 2026, 61(2): 403-416. DOI: 10.16438/j.0513-4870.2025-0166
Citation: WEI Zi-yi, HAN Rui, XIE Yi-ming, LI Fang, ZHANG Fan. Advances in the development of Nav1.8-targeted analgesicsJ. Acta Pharmaceutica Sinica, 2026, 61(2): 403-416. DOI: 10.16438/j.0513-4870.2025-0166

靶向Nav1.8的镇痛药物研发进展

Advances in the development of Nav1.8-targeted analgesics

  • 摘要: 电压门控钠通道亚型Nav1.8主要分布于外周伤害性感觉神经元, 在神经病理性疼痛等多种疼痛的发生与维持中发挥关键调控作用。2025年1月苏泽曲林(suzetrigine), 首个以Nav1.8为靶点的镇痛药物获得美国FDA批准上市, 标志着Nav1.8靶向镇痛药物研发取得重大突破。这一里程碑事件引发了国内外对Nav1.8镇痛抑制剂研发的广泛关注。本文系统综述了Nav1.8的结构特征、生理功能及其系列镇痛药物开发进展, 重点阐述了Nav1.8的电生理特性、疼痛调控机制以及选择性抑制剂的临床研究, 旨在为Nav1.8镇痛药物的开发提供参考。

     

    Abstract: The voltage-gated sodium channel isoform Nav1.8 is predominantly distributed in peripheral injurious sensory neurons and plays a key regulatory role in the development and maintenance of acute and chronic pain and neuropathic pain. In January 2025, suzetrigine, the first analgesic drug targeting Nav1.8, was approved for marketing in the United States FDA, marking a major breakthrough in the development of Nav1.8-targeted pain therapeutics. The successful development of the first analgesic for Nav1.8 has led to a global interest in the development of Nav1.8 analgesic inhibitors. This article reviews the structure, physiological function, and drug development of Nav1.8. We focus on summarizing the electrophysiological properties of Nav1.8, its role in pain, and the clinical studies of selective inhibitors, aiming to provide a reference for the development of Nav1.8 analgesics.

     

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