Three generations of EGFR tyrosine kinase inhibitors (TKIs)—namely gefitinib, erlotinib, afatinib, dacomitinib, osimertinib—demonstrated survival benefit over platinum-based chemotherapy and are world-wide approved in the first-line setting of advanced or metastatic EGFR mutant NSCLC, and a fair number of novel compounds are under investigation to prevent or overcome EGFR TKI resistance. The gene discussed is EGFR; the disease is non-small cell lung carcinoma.