GFH375 + GFH276

GFH375 + GFH276 is an investigational combination regimen consisting of GFH375 (also known as VS-7375), an oral, highly selective, non-covalent small-molecule inhibitor targeting both the active (ON) and inactive (OFF) states of the KRAS G12D mutation, and GFH276, an oral molecular-glue Pan RAS (ON) inhibitor that hijacks cyclophilin A (CypA) to target active, GTP-bound RAS proteins. Developed by GenFleet Therapeutics (with Verastem Oncology holding co-development rights for GFH375 outside of Greater China), this combination is being evaluated in a Phase II clinical trial (NCT07784374) for the treatment of patients with locally advanced unresectable or metastatic pancreatic ductal adenocarcinoma (PDAC) harboring a KRAS G12D mutation who have progressed on or are intolerant to at least one prior line of systemic therapy. The combination aims to achieve synergistic anti-tumor efficacy and overcome adaptive or acquired resistance by simultaneously targeting KRAS G12D and broader active RAS proteins.

Other names

GFH375 + GFH276GFH375/GFH276VS-7375 + GFH276VS-7375/GFH276