Bruton’s tyrosine kinase (BTK) inhibitors have revolutionized the treatment landscape for B cell lymphomas such as chronic lymphocytic leukemia (CLL). The first-in-class BTK inhibitor ibrutinib has recently been succeeded by covalent BTK inhibitors that are safer but still face challenges of resistance mutations. The noncovalent BTK inhibitor pirtobrutinib was recently approved for relapsed and refractory CLL, and whether noncovalent BTK inhibitors will supplant covalent BTK inhibitors as upfront treatment options either alone or in combination will be determined. Meanwhile, newer BTK inhibitors and BTK degraders are vying for their place in the potential future landscape of B cell cancers as well as autoimmune diseases. This review will cover the latest progress in BTK inhibitor development and where the field is moving in light of these recent discoveries.

Bruton 的酪氨酸激酶 (BTK) 抑制剂彻底改变了慢性淋巴细胞白血病 (CLL) 等 B 细胞淋巴瘤的治疗格局。一流的 BTK 抑制剂伊布替尼最近被共价 BTK 抑制剂所取代，这些抑制剂更安全，但仍面临耐药突变的挑战​​。非共价 BTK 抑制剂 pirtobrutinib 最近被批准用于治疗复发和难治性 CLL，并且将确定非共价 BTK 抑制剂是否会取代共价 BTK 抑制剂作为单独或联合的前期治疗选择。与此同时，新型 BTK 抑制剂和 BTK 降解剂正在 B 细胞癌症和自身免疫性疾病的未来潜在前景中争夺一席之地。本综述将涵盖 BTK 抑制剂开发的最新进展以及根据这些最新发现该领域的发展方向。