FT-02

FT-02 is a covalent small-molecule inhibitor developed by Fekra Therapeutics that specifically targets the KRAS G12C mutation. KRAS is a GTPase that functions as a molecular switch in cell signaling pathways; the G12C mutation locks the protein in an active state, driving uncontrolled cellular proliferation in various cancers. FT-02 utilizes an acrylamide-bearing platform as a reactive warhead to form a stable, irreversible covalent bond with the cysteine residue at position 12 of the mutant KRAS protein. This binding locks the protein in its inactive GDP-bound conformation, thereby inhibiting downstream oncogenic signaling. The drug is primarily being developed for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC).