INCB081776

INCB081776 is an orally available, potent, and selective small molecule inhibitor of the receptor tyrosine kinases Axl and MerTK. It was developed as an antineoplastic agent with immunomodulatory properties. By inhibiting both Axl and MerTK signaling pathways—key drivers of tumor cell survival, proliferation, metastasis, and therapeutic resistance—INCB081776 aims to suppress tumor growth directly while also modulating the tumor immune microenvironment to enhance anti-tumor immunity. Preclinical studies have shown that it can induce a pro-inflammatory immune response within tumors and increase the efficacy of checkpoint inhibitors such as anti-PD-L1 antibodies. The drug entered phase 1 clinical trials for advanced solid tumors but development has since been discontinued[1][2][3][4][5][6][7].