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Icotinib is a highly selective, first-generation small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It competitively inhibits the ATP binding site of EGFR—including both wild-type and several mutated forms—thereby blocking EGFR-mediated signal transduction pathways that drive cell proliferation and survival in cancer cells. Icotinib is primarily indicated for the treatment of non-small cell lung cancer (NSCLC) with activating EGFR mutations and has demonstrated efficacy as first-line monotherapy in advanced or metastatic disease. The drug was developed by Betta Pharmaceuticals (also known as Zhejiang Betta Pharma), with approval granted in China since 2011 for NSCLC patients harboring somatic EGFR mutations[2][3][5][7].
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