Description
Fostamatinib (R788) is a prodrug of the active metabolite R406, which is a potent, ATP-competitive inhibitor of Syk kinase with Ki/IC50 of 30/41nM; dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56nM, inhibits all phosphorylation events downstream of Syk signaling; specifically inhibits FcgammaR signaling in human mast cells, macrophages, and neutrophils. R788 can inhibit local inflammatory injury mediated by immune complexes; reduces immune complex-mediated inflammation in arthritis models. Rheumatoid Arthritis Phase 3 Clinical