Orally Bioavailable NRF2 Molecular Glue Degrader Effective in KEAP1-Mutant Cancer

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  • Novel HTS Transcriptomics screen identifies initial NRF2 hit
  • Hit and Analog induces an interaction between NRF2 and BTrCP
  • Optimized analogs lead to significant in vivo activity in multiple lung cancer models with very favorable drug-like and safety profiles