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RXDX-106 is an orally available, selective small molecule inhibitor targeting the receptor tyrosine kinase (RTK) activity of both hepatocyte growth factor receptor (c-Met; HGFR) and the TAM family of RTKs—TYRO3, AXL, and MER. It was developed as a novel immunomodulatory agent with potential antineoplastic activity. By inhibiting these kinases in the tumor microenvironment, RXDX-106 aims to reverse immunosuppression mediated by TAM RTKs and c-Met, thereby enhancing both innate and adaptive immune responses against tumors. Preclinical studies demonstrated that RXDX-106 increases tumor-infiltrating leukocytes and activates macrophages and natural killer cells while potentiating T-cell function. The drug showed anti-tumor efficacy as a single agent and in combination with checkpoint inhibitors in multiple tumor models. Its primary indication was for advanced or metastatic solid tumors[1][5][6][7].
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