cetuximab + fulzerasib

This drug is a combination therapy consisting of fulzerasib, a small molecule KRAS G12C inhibitor, and cetuximab, an anti-epidermal growth factor receptor (EGFR) monoclonal antibody. Fulzerasib irreversibly inhibits the KRAS G12C mutant protein by covalently binding to it and trapping it in its inactive GDP-bound form, thereby blocking downstream signaling pathways that promote tumor growth. Cetuximab targets EGFR to inhibit its activation, which is a known mechanism of resistance to KRAS inhibition. The combination has shown synergistic activity in preclinical models of KRAS G12C-mutated non-small cell lung cancer (NSCLC). Clinically, this chemo- and immunotherapy-free regimen has demonstrated high objective response rates (~80%) and disease control rates (~100%) with manageable safety profiles as first-line treatment for advanced NSCLC harboring the KRAS G12C mutation. It offers potential as a novel frontline standard-of-care option especially for patients who may not tolerate chemotherapy or immunotherapy.

Brand names

Dupert + Erbitux

Other names

fulzerasib plus cetuximabfulzerasib (GFH925) and cetuximab combination