Recently, the third-generation (mutant-selective) irreversible EGFR-tyrosine kinase inhibitors (TKIs) based on an amino pyrimidine scaffold, such as compounds 6 (WZ4002)16, 7 (CO-1686)17 and 8 (AZD9291)18 have demonstrated promising selectivity for EGFRL858R/T790M mutant over WT EGFR, indicating that this strategy is feasible for overcoming EGFR T790M gatekeeper mutation in NSCLC treatment (Fig. 1). The gene discussed is EGFR; the disease is non-small cell lung carcinoma.