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GS-9620 is an orally active TLR7 agonist with EC50 of 291 nM. [1]

Toll-like receptor 7 (TLR7) is a pathogen recognition receptor which plays an important role in the detection of, and the innate immune response to, pathogens. TLR7 signaling is predominantly activated by viral single-stranded RNA and is localized within the endolysosomal compartments of plasmacytoid dendritic cells (pDCs) and B lymphocytes in humans and non-human primates. Activation of pDCs plays an important role in the progress of innate response to viral pathogens and are involved in the majority of type I interferon (IFN) production during the acute phase of an infection by viruses. The induction and secretion of endogenous IFNs, including IFN-α and IFN- β, also induce the development of an efficient adaptive immunological response. Interferons induce the transcription of interferon-stimulated genes (ISGs) which generate an antiviral state within cells, as well as induce the production of other cytokines and chemokines which facilitate intercellular communication and cellular trafficking. GS-9620 could activate TLR7 signaling in immune cells to induce clearance of virus infected cells. [1, 2]

GS-9620 selectively induces IFN-α, cytokines and chemokines. The minimum effective concentrations for IFN-α induction were similar in pDCs and in PBMCs from HCV-positive donors. GS-9620 demonstrates an EC50 of 291 nM for human TLR7, which is 30-fold selectivity over TLR8 with EC50 of 9 μM. [1]

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