GFS784

GFS784 is a next-generation antibody-drug conjugate (ADC) developed by GenFleet Therapeutics using their proprietary FAScon™ (Functional Antibody and Synergistic conjugate) platform. It consists of the anti-EGFR monoclonal antibody cetuximab conjugated to GF005095, a novel pan-RAS(ON) inhibitor payload, via a cleavable linker with a drug-to-antibody ratio (DAR) of 8. The payload, GF005095, utilizes cyclophilin A to target and inhibit K/H/N-RAS mutants as well as wild-type RAS proteins. GFS784 is designed to leverage the synergy between EGFR targeting and RAS inhibition to overcome resistance mechanisms in RAS-mutant or EGFR-altered tumors, including those resistant to DXd-based ADCs or osimertinib. Preclinical studies have demonstrated potent anti-tumor activity and a significant bystander effect in various cancer models.

Other names

EGFR-panRASi ADC