R788 (Fostamatinib) is an important spleen tyrosine kinase (Syk) inhibitor, showing efficacy against kinase-mediated IgG Fc gamma receptor signaling. R788 inhibits the activation of mast cells, macrophages, and B-cells and related inflammatory responses a
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Tyrosine-protein kinase SYK inhibitor
Product Description
Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3. An inhibitor to spleenic kinase-mediated IgG Fc receptor signaling
1.Braselmann S, Taylor V, Zhao H, Wang S, Sylvain C, Baluom M, Qu K, Herlaar E, Lau A, Young C et al.. (2006) R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation.. J Pharmacol Exp Ther, 319 (3):(998-1008). [PMID:16946104]
2.Sweeny DJ, Li W, Clough J, Bhamidipati S, Singh R, Park G, Baluom M, Grossbard E, Lau DT. (2010) Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans: contribution of hepatic and gut bacterial processes to the overall biotransformation.. Drug Metab Dispos, 38 (7):(1166-76). [PMID:20371637]
3.Kunwar S, Devkota AR, Ghimire DK. (2016) Fostamatinib, an oral spleen tyrosine kinase inhibitor, in the treatment of rheumatoid arthritis: a meta-analysis of randomized controlled trials.. Rheumatol Int, 36 (8):(1077-87). [PMID:27113955]
4.Maringwa J, Kågedal M, Hamrén UW, Martin P, Cox E, Hamrén B. (2015) Pharmacokinetic-pharmacodynamic modeling of fostamatinib efficacy on ACR20 to support dose selection in patients with rheumatoid arthritis (RA).. J Clin Pharmacol, 55 (3):(328-35). [PMID:25280085]
5.Newland A, Lee EJ, McDonald V, Bussel JB. (2018) Fostamatinib for persistent/chronic adult immune thrombocytopenia.. Immunotherapy, 10 (1):(9-25). [PMID:28967793]
6.Niscola P, Scaramucci L, Giovannini M. (2018) Spleen tyrosine kinase inhibition: a new promising approach to chronic and refractory immune thrombocytopenia.. Immunotherapy, 10 (1):(5-7). [PMID:29192558]
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C2401280