Drug intelligence / Profile preview

Tamatinib

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

Overview

Tamatinib is a small molecule inhibitor of spleen tyrosine kinase (SYK), acting as a potent ATP-competitive (Type I) SYK inhibitor. It is the active metabolite of fostamatinib, which is an approved drug for chronic immune thrombocytopenia. Tamatinib inhibits SYK, a non-receptor tyrosine kinase involved in signal transduction downstream of various immunoreceptors such as the B-cell receptor and Fc receptors. By blocking SYK activity, tamatinib disrupts pathways critical to innate and adaptive immunity, cell adhesion, osteoclast maturation, platelet activation, and vascular development. Its mechanism leads to reduced mast cell degranulation and cytokine release in inflammatory conditions like bronchial asthma and autoimmune diseases such as rheumatoid arthritis. Tamatinib has also shown efficacy in preclinical models for glomerulonephritis and non-Hodgkin lymphoma[1][2][4][6][7].

Other names
R-406R406R 406
02

Targets

SYK (Spleen Tyrosine Kinase)

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