Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

Non-small-cell lung cancers with activating mutations in the epidermal growth factor receptor (EGFR) often show a clinical response to EGFR kinase inhibitors but tend to develop drug-resistance mutations, including the gatekeeper T790M mutation. Here, a new class of EGFR inhibitors is developed; these agents are 30- to 100-fold more potent against EGFR with the T790M mutation, and up to 100-fold less potent against wild-type EGFR, than current EGFR inhibitors