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Synonyms: R 788 | R-788 | R7935788 | Tavalisse® | Tavlesse®
fostamatinib is an approved drug (FDA (2018), EMA (2020))
Compound class: Synthetic organic
Comment: Fostamatinib is a spleen tyrosine kinase (Syk) inhibitor prodrug. Fostamatinib is administered orally in disodium salt preparations (e.g. PubChem CID 25008120 and fostamatinib disodium hexahydrate CID 24828759). It is rapidly converted to tamatinib by alkaline phosphatases in intestinal enterocytes . Although development in rheumatoid arthritis was discontinued in 2013 due to a lack of observed efficacy, development continued in patients with chronic and persistent immune thrombocytopenia (ITP).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
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. 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]
3. 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]
4. Newland A, Lee EJ, McDonald V, Bussel JB. (2018)
Fostamatinib for persistent/chronic adult immune thrombocytopenia.
Immunotherapy, 10 (1): 9-25. [PMID:28967793]
5. 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]
6. 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]