Since US Food and Drug Administration (FDA) approved imatinib for the treatment of chronic myeloid leukemia in 2001, multiple potent and well-tolerated TKIs—targets including EGFR, ALK, ROS1, HER2, NTRK, VEGFR, RET, MET, MEK, FGFR, PDGFR, and KIT—have been emerging and contributing to the significant progress in cancer treatment. This evidence concerns the gene ROS1 and cancer.