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S-1 + gefitinib is a combination therapy consisting of the oral fluoropyrimidine derivative S-1 and the EGFR tyrosine kinase inhibitor gefitinib. This combination has been studied primarily for treating non-small cell lung cancer (NSCLC), particularly in cases with EGFR mutations and acquired resistance to EGFR-TKIs. The combination works through dual mechanisms: gefitinib inhibits EGFR tyrosine kinase activity, blocking downstream signaling cascades that promote cancer cell survival, while S-1 (containing tegafur, gimeracil, and oteracil) provides cytotoxic effects through its active metabolite 5-fluorouracil. Research suggests this combination may be particularly effective in overcoming resistance to EGFR-TKIs in NSCLC with MET amplification.
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