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Garsorasib + ifebemtinib is a dual-oral combination therapy under clinical development for the treatment of cancers harboring KRAS G12C mutations. Garsorasib (D-1553) is a highly selective small molecule inhibitor targeting the KRAS G12C mutant protein, while ifebemtinib (IN10018) is an orally administered, highly selective focal adhesion kinase (FAK) inhibitor. The combination has demonstrated significant synergistic anti-tumor activity in preclinical and clinical studies by simultaneously inhibiting tumor cell proliferation and disrupting tumor defense mechanisms mediated by FAK signaling. This regimen has shown high response rates and durable efficacy in first-line non-small cell lung cancer (NSCLC) with KRAS G12C mutation as well as improved outcomes over monotherapy in previously treated colorectal cancer with the same mutation. The safety profile of the combination is consistent with each agent alone, without additive toxicities[1][3][7].
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