First-generation EGFR tyrosine kinase inhibitors (TKIs) such as gefitinib (2), imatinib (1), lapatinib (4), and erlotinib (3) have been approved by the US Food and Drug Administration (FDA) for treatment of EGFR-activating mutation-positive NSCLC patients (Figure 1). This evidence concerns the gene EGFR and non-small cell lung carcinoma.