EFTX-G12V

EFTX-G12V is a first-in-class, mutant-selective siRNA therapeutic designed to target the KRAS G12V mutation, which is prevalent in lung, colorectal, and pancreatic cancers. Developed by EnFuego Therapeutics, the drug consists of a fully-modified siRNA conjugated to an EGFR-directed linear ligand. This ligand-conjugation strategy leverages high EGFR expression on tumor cells to facilitate selective delivery of the siRNA payload, minimizing exposure to healthy somatic tissues. EFTX-G12V specifically inhibits the expression of KRAS G12V at both the mRNA and protein levels while sparing wild-type KRAS. Preclinical studies have demonstrated significant anti-tumor activity, inhibition of tumor angiogenesis, and a robust anti-tumor immune response in various xenograft and immunocompetent models.