HP-002 / Helioson Pharmaceutical - LARVOL DELTA

HP-002: A brain-penetrant PROTAC that demonstrated potent anti-proliferation activities on multiple BTK mutant (AACR 2025) - "In lymphoma cells e.g. REC-1 and TMD8, HP-002 demonstrated 2-digit pM IC50 with up to ~10-fold more potent than NX-5948 and BGB-16673. HP-002 is a potent and highly selective BTK degrader against BTK-WT and multiple BTK inhibitor-resistant mutations. Brain penetration was observed in the TMD8 xenograft tumor model with deeper BTK down-regulation on the HP-002 treatment and robust tumor growth inhibition. With no significant safety risk findings in the preliminary rat and NHP DRF studies, HP-002 is currently under IND-enabling development."

Late-breaking abstract • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Oncology • BTK • CRBN • GSPT1 • SALL4