中国麻风皮肤病杂志 ›› 2026, Vol. 42 ›› Issue (6): 456-463.doi: 10.12144/zgmfskin202606456

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从肿瘤治疗到免疫治疗：BTK抑制剂的研发和临床应用进展

孙勇虎1,2,张福仁1,2   

  1. 1山东第一医科大学附属皮肤病医院，山东济南，250022；2山东省皮肤病性病防治研究所,山东济南,250022
  • 出版日期:2026-06-15 发布日期:2026-06-04

From cancer treatment to immunotherapy: progress in the research and clinical application of BTK inhibitors

SUN Yonghu1,2, ZHANG Furen1,2   

  1. 1 Dermatology Hospital of Shandong First Medical University, Jinan 250022, China；2 Shandong Provincial Institute of Dermatology and Venereology, Shandong Academy of Medical Sciences, Jinan 250022, China
  • Online:2026-06-15 Published:2026-06-04

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摘要： 布鲁顿酪氨酸激酶（Bruton's tyrosine kinase, BTK）是B细胞受体（B cell receptor, BCR）信号传导的必需蛋白，在B细胞分化和增殖中起关键作用，同时也表达于肥大细胞和嗜碱性粒细胞等髓系细胞。自发现BTK突变导致X连锁无丙种球蛋白血症以来，BTK抑制剂的研发经历了从肿瘤治疗向免疫疾病治疗的重要跨越。目前，BTK抑制剂在B细胞恶性肿瘤中已展现出显著疗效，并逐步拓展至慢性自发性荨麻疹、系统性红斑狼疮及多发性硬化等自身免疫性疾病。本文系统回顾BTK抑制剂的研发历程、分子优化策略及其在免疫疾病领域的应用进展，并分析其在机制与临床层面的优势与挑战。

关键词: 布鲁顿酪氨酸激酶, BTK抑制剂, 荨麻疹, 自身免疫性疾病

Abstract: Bruton's tyrosine kinase (BTK) is an essential protein for B cell receptor (BCR) signaling and plays a key role in B cell differentiation and proliferation. It is also expressed in myeloid cells such as mast cells and basophils. Since the discovery that BTK mutations cause X-linked agammaglobulinemia, the research and development of BTK inhibitors has undergone an important leap from cancer treatment to immune disease treatment. At present, BTK inhibitors have demonstrated significant efficacy in B-cell malignancies and are gradually being extended to autoimmune diseases such as chronic spontaneous urticaria, systemic lupus erythematosus and multiple sclerosis. This article systematically reviews the research and development process of BTK inhibitors, their molecular optimization strategies, and the progress of their application in the field of immune diseases, and analyzes their advantages and challenges at the mechanism and clinical levels.

Key words: Bruton's tyrosine kinase, BTK inhibitors, urticaria, autoimmunity