YLSH003

YLSH003 is an investigational, orally bioavailable small molecule inhibitor specifically targeting the KRAS G12C mutation. Developed by Chengdu Easton Biopharmaceuticals (苑东生物), the drug is designed to covalently and irreversibly bind to the cysteine residue at position 12 of the KRAS protein when it is in its inactive, GDP-bound state. By trapping the mutant KRAS protein in this inactive conformation, YLSH003 effectively blocks the activation of downstream signaling pathways, such as the RAF-MEK-ERK (MAPK) pathway, which are critical for the growth and survival of tumor cells. It is primarily being developed for the treatment of advanced solid tumors harboring the KRAS G12C mutation, including non-small cell lung cancer (NSCLC) and colorectal cancer. As of early 2024, YLSH003 is undergoing Phase 1 clinical evaluation in China to assess its safety, tolerability, and preliminary efficacy.