XZ116

XZ116 is an orally bioavailable, small molecule inhibitor specifically targeting the KRAS G12C mutation. Developed by Shandong New Era Pharmaceutical, a subsidiary of Lunan Pharmaceutical Group, it is designed to covalently and irreversibly bind to the cysteine residue of the KRAS G12C protein. This binding locks the KRAS protein in its inactive GDP-bound state, thereby preventing the activation of downstream oncogenic signaling pathways, such as the MAPK/ERK pathway, which are critical for tumor cell proliferation and survival. XZ116 is currently undergoing Phase 1 clinical evaluation for the treatment of patients with advanced solid tumors harboring the KRAS G12C mutation, including non-small cell lung cancer and colorectal cancer.