Fostamatinib is a prodrug of the spleen tyrosine kinase inhibitor (Syk) R406 and is approved for the treatment of chronic immune thrombocytopenia. It has demonstrated significant reduction in inflammatory mediators such as TNFalpha, IL-1, IL-6, and IL-8 in arthritis models.1 Syk IC50 = 41 nM - Fostamatinib also inhibits Flt3, Lyn, and Lck with similar potency in vitro but displays higher selectivity Syk in cellular assays.2 Significantly inhibits LPS-induced inflammatory response via blocking STAT1/3 signaling.3 Fostamatinib restored myeloid homeostasis in severe COVID-19.4 Displayed synergistic effects with anti-PDL1 therapy against neuroblastoma.5 Fostamatinib induces metabolic reprogramming of acute myeloid leukemia stem cells.6
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