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LY3300054 + LY3381916 is a combination of two investigational immuno-oncology agents developed by Eli Lilly. LY3300054 is a monoclonal antibody targeting programmed death-ligand 1 (PD-L1), functioning as an immune checkpoint inhibitor. LY3381916 is an orally available, highly selective, and potent small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1). The combination was designed to enhance anti-tumor immune responses by simultaneously blocking PD-L1-mediated T cell inhibition and IDO1-mediated immunosuppression in the tumor microenvironment. Clinical studies evaluated this combination in patients with advanced solid tumors, including triple-negative breast cancer, non-small cell lung cancer, and renal cell carcinoma. The clinical activity observed was limited; the most prominent adverse events were related to liver toxicity. The development program for this combination has been terminated[1][2][3][5][7].
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