Abstract: 【Abstract】 Chronic spontaneous urticaria （CSU） is the most common phenotype of chronic urticaria. To date, second-generation H1 antihistamines （sgAHs） and omalizumab are the main treatment options for CSU. However, a considerable number of CSU patients are resistant to these therapies. Bruton's tyrosine kinase （BTK） inhibitors inhibit the degranulation of mast cells and basophils, as well as the production of antibodies by B cells, possessing a theoretical basis and potential benefits in the treatment of CSU. First-generation BTK inhibitors have been approved for the treatment of B cell-related malignancies, but there is a high risk of adverse reactions due to their poor selectivity. The second-generation BTK inhibitor remibrutinib has high affinity and selectivity for BTK, exhibiting good pharmacokinetic profiles. Phase Ⅱ and Ⅲ clinical trials of remibrutinib for CSU have been completed. Second-generation BTK inhibitors offer a novel treatment option for patients with CSU who do not respond adequately to increased doses of sgAHs. This review summarizes the mechanism of action, pharmacological characteristics, and clinical application of BTK inhibitors.

Key words: Chronic urticaria, Protein-tyrosine kinases, Protein kinase inhibitors, Therapy, Drug-related side effects and adverse reactions, Bruton′s tyrosine kinase inhibitors