ONO-7475 is a potent inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 at nM range for both AXL and MER.  AXL has been implicated in diverse tumor-promoting processes such as proliferation, migration, invasion, survival, and apoptosis, and therefore considered a promising druggable target to overcome drug resistance for acute myeloid leukemia, pancreatic cancer [2], lung cancer [3], as well as breast cancer [3].  ONO-7475 sensitizes and suppresses the emergence of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells, suggesting that ONO-7475 and osimertinib is a highly potent combination for initial treatment of NSCLC.

ONO-7475 is a potent inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 at nM range for both AXL and MER.  AXL has been implicated in diverse tumor-promoting processes such as proliferation, migration, invasion, survival, and apoptosis, and therefore considered a promising druggable target to overcome drug resistance for acute myeloid leukemia, pancreatic cancer [2], lung cancer [3], as well as breast cancer [3].  ONO-7475 sensitizes and suppresses the emergence of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells, suggesting that ONO-7475 and osimertinib is a highly potent combination for initial treatment of NSCLC.