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DS-1205c + gefitinib is a combination therapy consisting of DS-1205c, a novel, specific, orally bioavailable, small-molecule AXL receptor tyrosine kinase inhibitor (TKI), and gefitinib, an established EGFR TKI. This combination was developed to address resistance to EGFR TKIs in non-small cell lung cancer (NSCLC) patients with EGFR mutations. In preclinical studies, DS-1205c restored TKI antitumor activity in TKI acquired-resistance EGFR-mutant NSCLC tumor xenograft models. The combination aims to prevent, delay, or overcome the onset of resistance to EGFR TKIs by inhibiting the AXL pathway, which is implicated in resistance mechanisms.
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