Drug intelligence / Profile preview

fostamatinib

Development stage
Approved
Lead developer
Rigel Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Fostamatinib is an orally administered small molecule prodrug that is rapidly converted to its active metabolite, R406. It functions as a spleen tyrosine kinase (SYK) inhibitor. SYK is a non-receptor protein tyrosine kinase that plays a critical role in the intracellular signaling pathways of various immune cells, including macrophages, B cells, and T cells. In immune thrombocytopenia (ITP), autoantibodies bind to platelets, marking them for destruction. These opsonized platelets then engage Fc gamma receptors on the surface of macrophages, triggering a SYK-dependent signaling cascade. By inhibiting SYK, fostamatinib disrupts this pathway, thereby preventing the phagocytosis of antibody-coated platelets and leading to an increase in platelet counts. It is approved for the treatment of chronic ITP in adults who have had an insufficient response to previous treatments. The drug was developed by Rigel Pharmaceuticals.

Brand names
TavalisseTavlesse
Other names
fostamatinib disodiumfostamatinib disodium hexahydrate扶正止痛
02

Targets

SYK (Spleen Tyrosine Kinase)

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