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Fulzerasib is a novel, orally active small molecule that acts as a potent and selective covalent inhibitor of KRAS G12C. It irreversibly binds to the mutant KRAS G12C protein at the cysteine residue in codon 12, inhibiting the GTP/GDP exchange and thereby blocking downstream signaling pathways critical for tumor cell proliferation and survival. Fulzerasib has demonstrated significant antitumor activity in patients with advanced non-small cell lung cancer (NSCLC) harboring KRAS G12C mutations and is also being investigated for colorectal cancer. The drug was originally developed by GenFleet Therapeutics and is co-developed and commercialized in China by Innovent Biologics under an exclusive license agreement. In August 2024, it received approval from China's National Medical Products Administration (NMPA) for use in adult patients with advanced NSCLC carrying the KRAS G12C mutation[1][3][4][5][6][7].
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