JS116

JS116 is an orally bioavailable, small molecule irreversible covalent inhibitor of the KRAS G12C mutation, developed by Shanghai Junshi Biosciences. KRAS G12C is a specific mutation in the KRAS gene that acts as a common driver in various malignancies, most notably non-small cell lung cancer (NSCLC) and colorectal cancer. JS116 is designed to bind covalently to the cysteine residue of the KRAS G12C protein, trapping it in its inactive GDP-bound state. This action effectively blocks the activation of downstream signaling pathways, such as the MAPK/ERK pathway, which are critical for tumor cell proliferation and survival. The drug received Investigational New Drug (IND) application acceptance from China's National Medical Products Administration (NMPA) in June 2022 for the treatment of advanced solid tumors harboring the KRAS G12C mutation.