HP-002

HP-002 is a brain-penetrant, small-molecule proteolysis-targeting chimera (PROTAC) designed to induce the degradation of Bruton's Tyrosine Kinase (BTK). Developed by Shanghai Helioson Pharmaceutical, the drug functions by recruiting the cereblon (CRBN) E3 ubiquitin ligase to the BTK protein, leading to its ubiquitination and subsequent proteasomal degradation. HP-002 exhibits high potency with a DC50 of 0.09 nM and maintains activity against both wild-type BTK and multiple mutations that confer resistance to traditional BTK inhibitors. It is primarily being developed for the treatment of hematologic malignancies, including B-cell lymphomas, and its ability to cross the blood-brain barrier suggests potential utility in treating central nervous system involvements of these cancers.