Selgantolimod is an effective and selective toll-like receptor 8 agonists for the treatment of the hepatitis B virus and human immunodeficiency virus infection.

Selgantolimod induces the cellular immune mediators interleukin (IL)-12 and IL-8, as well as the antiviral cytokines tumor necrosis factor-α and interferon-γ in vitro in human peripheral blood mononuclear cells. Selgantolimod-induced cytokines reduce HBV DNA, RNA, and antigen levels in HBV-infected primary human hepatocytes. Selgantolimod activates natural killer and mucosal-associated invariant T cells, stimulates cluster of differentiation (CD)-8+ T-cell proliferation, and increase IFNγ production while lowering programmed cell death protein 1 expression by HBV-specific CD8+-T cells in vitro in peripheral blood mononuclear cells [1].

Selgantolimod (p.o., once-weekly) treatment induces dose-dependent increases in serum IL-12 and IL-1 receptor antagonist (IL-1RA) in cynomolgus monkeys and causes functional cure in the woodchuck model of chronic HBV [1].