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HS-10541 is an orally bioavailable small molecule inhibitor specifically targeting the KRAS G12C mutation, developed by Jiangsu Hansoh Pharmaceutical. KRAS G12C is a common oncogenic driver in various solid tumors, particularly non-small cell lung cancer (NSCLC) and colorectal cancer. HS-10541 works by covalently binding to the cysteine residue of the KRAS G12C protein in its inactive GDP-bound state, thereby locking it in an inactive conformation and inhibiting downstream signaling pathways such as MAPK/ERK. It is currently being evaluated in Phase I clinical trials as a monotherapy and in combination with other anti-cancer agents for patients with advanced solid tumors harboring the KRAS G12C mutation.
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