HSK29116

HSK29116 is an investigational oral small molecule proteolysis-targeting chimera (PROTAC) designed as a Bruton's tyrosine kinase (BTK) degrader. It consists of an E3 ubiquitin ligase binding moiety conjugated to a BTK-binding moiety via a linker. Upon administration, HSK29116 binds to BTK and induces its ubiquitination and subsequent degradation by the proteasome, thereby inhibiting BTK activity and blocking B-cell receptor signaling pathways. This dual mechanism—direct inhibition and targeted degradation—aims to control the progression of various B-cell malignancies, including those with resistance mutations such as C481S in BTK. Developed by Sichuan Haisco Pharmaceutical, it is currently being evaluated in Phase 1 clinical trials for relapsed or refractory B-cell malignancies such as chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), mantle cell lymphoma (MCL), and other advanced B-cell cancers[1][2][4][5][7].