DWP216

DWP216 is a targeted small molecule inhibitor of TEA domain transcription factor 1 (TEAD1), currently in preclinical development by Daewoong Pharmaceutical. It is specifically designed to treat solid cancers harboring mutations in the NF2 (Neurofibromatosis type 2) tumor suppressor gene. In NF2-mutant tumors, the Hippo signaling pathway is disrupted, leading to the activation of TEAD factors which drive the expression of oncogenic genes. DWP216 selectively inhibits TEAD1 to suppress this pathological gene expression. It is Daewoong's first internally developed anticancer drug and has been noted for having reduced toxicity compared to earlier-generation TEAD inhibitors. The project was presented at the AACR Annual Meeting 2025 and has been recognized as a national new drug development project in South Korea.