| Description | Selgantolimod is an effective and selective toll-like receptor 8 agonists for the treatment of the hepatitis B virus and human immunodeficiency virus infection. |
| In vitro | 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]. |
| In vivo | 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]. |
| Synonyms | GS-9688 |
| molecular weight | 293.34 |
| Molecular formula | C14H20FN5O |
| CAS | 2004677-13-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Jules Levin. Efficacy and Safety of Oral TLR8 Agonist Selgantolimod in Virally Suppressed Adult Patients With Chronic Hepatitis B: a Phase 2, Randomized, Double-Blind, Placebo-Controlled, Multicenter Study. 2019 Nov 8-12. 2. Benjamin Ryan. Selgantolimod Shows Promise as Treatment for Hepatitis B. November 18, 2019. 3. Romas Geleziunas, et al. Modulators of toll-like receptors for the treatment of hiv. US20170071944A1. |