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 [6]. 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 ChartsThese 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. ✖ |
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Immunopharmacology Comments |
Fostamatinib is the first selective Syk inhibitor to receive clinical approval, and this approval is for treatment of an autoimmune disorder. |
Immunopharmacology Disease | |||
Disease | X-Refs | Comment | References |
Rheumatoid arthritis |
Disease Ontology:
DOID:7148 OMIM: 180300 |
Phase 3 clinical candidate for RA. | 2 |
Autoimmune thrombocytopenic purpura |
Disease Ontology:
DOID:8924 OMIM: 188030 Orphanet: ORPHA3002 |
Approved drug for ITP. FDA approval granted in April 2018. |