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HSK42360-Na is an orally bioavailable small molecule inhibitor specifically targeting the KRAS G12D mutation, developed by Haisco Pharmaceutical Group. KRAS is a member of the RAS GTPase family that acts as a molecular switch in signaling pathways regulating cell growth; the G12D mutation locks the protein in a constitutive 'on' state, driving malignancy in various solid tumors, most notably pancreatic, colorectal, and lung cancers. HSK42360-Na is designed to selectively bind to the KRAS G12D mutant protein, inhibiting its activity and suppressing downstream oncogenic signaling pathways such as MAPK/ERK. As of early 2024, the drug is undergoing Phase 1 clinical evaluation for the treatment of advanced solid tumors harboring the KRAS G12D mutation.
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