GFH603 / GenFleet Therap - LARVOL DELTA

GFH603: A molecular glue-like allosteric activator of the KEAP1-CUL3 E3 ligase complex for targeting NRF2-activated tumors (AACR 2026) - "GFH603 restores KEAP1-CUL3 E3 ligase activity through a molecular glue mechanism, enabling targeted degradation of NRF2 in KEAP1/NFE2L2-mutant tumors. It demonstrates potent efficacy as monotherapy in NRF2-activated squamous cancer models (e.g., ESCC, LUSC) and synergizes with pan-RAS inhibitors in KRAS/KEAP1 co-mutant cells. These findings support GFH603 as a promising therapeutic candidate for overcoming NRF2-driven resistance and addressing a critical unmet need in oncology."

IO biomarker • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Ductal Adenocarcinoma • Solid Tumor • KEAP1 • KRAS • NFE2L2