Since the US FDA approved imatinib for the treatment of chronic myeloid leukemia in 2001, multiple potent and well-tolerated TKIs—with targets including EGFR, ALK, ROS1, HER2, NTRK, VEGFR, RET, MET, MEK, FGFR, PDGFR, and KIT—have emerged and contributed to significant progress in cancer treatment. The gene discussed is EGFR; the disease is cancer.