Bruton's tyrosine kinase (BTK) inhibitors: an updated patent review (2019-2024).

Introduction: Bruton's tyrosine kinase (BTK) is a critical regulator in the pathogenesis of B-cell malignancies, inflammatory diseases, and autoimmune diseases. In recent years, BTK inhibitors have been a hot topic in drug development, with promising therapeutic prospects. Six BTK inhibitors have been approved, and several (including PROTAC) are undergoing clinical research.

Areas covered: This review provides a comprehensive analysis of BTK inhibitor mechanisms and synthesizes recent advancements documented in patent literature (2019-2024), with particular emphasis on structural innovations and therapeutic applications. Web of Science, PubMed, SciFinder, WIPO, EPO, USPTO and CNIPA databases were used for searching the literature and patents for BTK inhibitors.

Expert opinion: In recent years, many new drug development strategies proposed by medicinal chemists, such as multi-target inhibition, deuterium substitution, macrocyclization, and targeted protein degradation strategy (such as PROTAC), may provide guidance for the development of novel BTK inhibitors and overcome the problems of existing BTK inhibitors. Despite many challenges, BTK inhibitors have great potential in treating cancer and other diseases. With the application of new drug development strategies, the development of the next generation of BTK inhibitors may be promising.