• Aliases: R788; tamatinib fosdium; R935788 sodium
    • An oral disodium salt of the SYK kinase inhibitor that inhibits SYK kinase–mediated IgG Fc γ-receptor signaling
    • SYK kinase, widely expressed in hematopoietic cells, is a non-RTK that is involved in coupling-activated immunoreceptors to signal downstream events that mediate proliferation, differentiation, and phagocytosis.
    • Currently in phase 3 trials for ITP
    • Recommended phase 2 dose: 200 mg PO b.i.d.
    • Half-life: 12 to 21 hours
    • Common side effects: Fatigue, nausea/vomiting/diarrhea, thrombocytopenia, hypertension, neutropenia, increased AST
    (Baluom et al., 2013)
    Other topics in Targeted and Immunotherapy Agents