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RG-7795 (previously known as ANA773) is an oral prodrug of a toll-like receptor 7 (TLR7) agonist. Its active metabolite promotes natural killer (NK) cell-mediated anti-tumor response through multiple mechanisms: inducing cytokine secretion, enhancing cytolysis of tumor cells by NK cells, and enhancing antibody-dependent cellular cytotoxicity (ADCC). The drug induces secretion of interferon-alpha (IFN-alpha) and various other cytokines from human peripheral blood mononuclear cells. NK cells activated by this drug mediate anti-tumor activity by directly lysing tumor cells through cytotoxic granule secretion, promoting apoptosis via interferon-gamma production, and enhancing the anti-tumor response of other immune cells. Large amounts of type I interferons are produced by plasmacytoid dendritic cells upon engagement of TLR7, which naturally binds to single-stranded RNA. RG-7795 was initially developed by Anadys Pharmaceuticals and later acquired by Roche. It was investigated for treatment of solid tumors, hepatitis B, and hepatitis C.
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