The first-generation EGFR-TKI drugs, including gefitinib (FDA approved, 2003), erlotinib (FDA approved, 2004), and icotinib, are reversible and ATP-competent inhibitors that showed promising results when used in the first-line treatment for NSCLC patients harboring EGFR mutations. This evidence concerns the gene EGFR and non-small cell lung carcinoma.