Recent development of BTK-based dual inhibitors in the treatment of cancers.

Bruton's tyrosine kinase (BTK) is a promising target in the treatment of various cancers. Despite the early success of BTK inhibitors in the clinic, these single-target drug therapies have limitations in their clinical applications, such as drug resistance. Several alternative strategies have been developed, including the use of dual inhibitors, to maximize the therapeutic potential of anticancer drugs. In this review, we highlight the scientific background and theoretical basis for developing BTK-based dual inhibitors, as well as the status of these agents in preclinical and clinical studies, and discuss further options in this field. We posit that these advances in BTK-based dual inhibitors confirm their feasibility for the treatment of refractory tumors, including those with drug resistance, and provide a framework for future drug design in this field. Accordingly, we anticipate increasingly rapid progress in the development of novel potent dual inhibitors and advanced clinical research on BTK-based dual inhibitors.