Current treatment for non-small-cell lung cancer (NSCLC) is epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs). However, relapse due to acquired resistance to first-line and second-line treatment with these drugs is inevitable. A new mutation in the EGFR gene, T790M, is most frequently responsible for disease progression after EGFR-TKI treatment. The results of three phase 1 studies presented at the recent American Society of Clinical Oncology meeting show the promising efficacy of three new compounds in patients with EGFR-mutated NSCLC.