治疗慢性自发性荨麻疹新药:布鲁顿酪氨酸激酶抑制剂瑞米布替尼

doi:10.6040/j.issn.1671-7554.0.2025.1551

摘要/Abstract

摘要： 慢性自发性荨麻疹(chronic spontaneous urticaria, CSU)是一种常见的肥大细胞介导的皮肤疾病,现有抗组胺药对多数患者疗效欠佳,二线治疗药物奥马珠单抗亦存在应答不佳或不能完全缓解的情况,临床仍需安全有效且使用便捷的新药。瑞米布替尼是一种口服、高选择性的布鲁顿酪氨酸激酶(Brutons tyrosine kinase, BTK)抑制剂,于2025年9月30日获美国食品药品监督管理局批准,用于治疗经抗组胺药治疗后仍有症状的成人CSU患者,成为全球首个获批用于CSU的BTK抑制剂;该药亦于2025年11月25日获中国国家药品监督管理局批准上市。其通过不可逆抑制BTK活性,特异性阻断IgE受体交联所致的下游信号转导,抑制肥大细胞与嗜碱性粒细胞脱颗粒,减少组胺等炎症介质释放,从而有效缓解风团与瘙痒症状。Ⅲ期临床研究显示,该药能快速、显著地改善患者症状,并维持52周疗效,安全性良好。但其在不同种族人群中的长期疗效和安全性仍有待进一步观察。本文就瑞米布替尼的作用机制、药动学特征、临床研究及安全性等进行综述,旨在为我国CSU的临床治疗与新药研发提供参考。

关键词: 瑞米布替尼, 慢性自发性荨麻疹, 布鲁顿酪氨酸激酶抑制剂, 口服治疗

Abstract: Chronic spontaneous urticaria(CSU)is a common mast cell-mediated skin disease. However, most patients respond poorly to current antihistamines, and the second-line treatment omalizumab also shows poor response or fails to achieve complete remission. Therefore, safe, effective, and convenient new drugs are still needed. Remibrutinib is an oral, highly selective inhibitor of Bruton's tyrosine kinase(BTK). On September 30, 2025, it was approved by the U.S. Food and Drug Administration for the treatment of adult patients with CSU who remain symptomatic after antihistamine therapy, becoming the first BTK inhibitor globally approved for CSU. The drug was subsequently approved for marketing in China by the National Medical Products Administration on November 25, 2025. By irreversibly inhibiting BTK activity, remibrutinib specifically blocks downstream signal transduction triggered by IgE receptor cross-linking, thereby inhibiting mast cell and basophil degranulation, reducing the release of inflammatory mediators such as histamine, and effectively alleviating wheals and pruritus. Phase III clinical trials have shown that remibrutinib can rapidly and significantly improve patients symptoms and maintain efficacy for up to 52 weeks, with a favorable safety profile. However, its long-term efficacy and safety in different racial populations still require further observation. This article briefly reviews the mechanism of action, pharmacokinetic characteristics, clinical research, and safety of remibrutinib, aiming to provide a reference for the clinical treatment and new drug development of CSU in China.

Key words: Remibrutinib, Chronic spontaneous urticaria, Brutons tyrosine kinase inhibitor, Oral therapy

中图分类号:

R976

黄佩文,王旭东. 治疗慢性自发性荨麻疹新药:布鲁顿酪氨酸激酶抑制剂瑞米布替尼[J]. 山东大学学报 (医学版), 2026, 64(9): 118-124.

HUANG Peiwen, WANG Xudong. A novel drug for chronic spontaneous urticaria: Brutons tyrosine kinase inhibitor remibrutinib[J]. Journal of Shandong University (Health Sciences), 2026, 64(9): 118-124.

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