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DS-1205 is an investigational, highly selective small-molecule inhibitor of the receptor tyrosine kinase AXL. It is being developed primarily for the treatment of cancers characterized by abnormal AXL expression and activation, which are associated with poor prognosis and resistance to other therapies. The drug has been studied in combination with EGFR tyrosine kinase inhibitors (TKIs) such as gefitinib and osimertinib for metastatic or unresectable EGFR-mutated non-small cell lung cancer (NSCLC), aiming to overcome or delay acquired resistance to these agents. Preclinical studies have shown that DS-1205 can restore antitumor activity in TKI-resistant models by inhibiting AXL signaling pathways[1][2][6][9]. Clinical trials have demonstrated that oral administration of DS-1205c (a clinical formulation) is generally well tolerated when combined with EGFR TKIs[6][9]. The drug was originally developed by Daiichi Sankyo and later licensed to AnHeart Therapeutics (now part of Nuvation Bio)[3].
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