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Gefitinib + icotinib is a combination of two first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), both used primarily in the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations. Gefitinib and icotinib selectively inhibit the EGFR tyrosine kinase domain, blocking downstream signaling pathways involved in tumor cell proliferation and survival. Both drugs are small molecules that act by competitively binding to the ATP-binding site of EGFR, thereby inhibiting its autophosphorylation and subsequent activation of signal transduction cascades. This combination has been proposed as a potential synergistic regimen for targeting cancer-associated proteins/genes in NSCLC, particularly lung adenocarcinoma[1][2][3][4][5]. Each drug individually has demonstrated efficacy as monotherapy; their combined use is under investigation for enhanced therapeutic benefit.
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