Fostamatinib
| 200px Fostamatinib
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| 200px Fostamatinib disodium
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| Names | |
|---|---|
| IUPAC name
[6-({5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]pyrimidin-4-yl}amino)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl]methyl dihydrogen phosphate
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| Other names
Tamatinib fosdium; R-788; NSC-745942; R-935788
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| Identifiers | |
901119-35-5  1025687-58-4 (fostamatinib disodium) |
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| ChEMBL | ChEMBL2103830 |
| ChemSpider | 9846198 |
| 7796 | |
| Jmol 3D model | Interactive image |
| PubChem | 11671467 25008120 (fostamatinib disodium) |
| UNII | SQ8A3S5101 |
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| Properties | |
| C23H26FN6O9P | |
| Molar mass | 580.47 g·mol−1 |
| Vapor pressure | {{{value}}} |
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Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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| Infobox references | |
Fostamatinib is an experimental drug candidate for the treatment of a variety of diseases, originally developed by Rigel Pharmaceuticals. The drug is administered orally as a disodium salt, and is a prodrug of the active compound tamatinib (R-406),[1] which is an inhibitor of the enzyme spleen tyrosine kinase (Syk),[2] hence it is an syk inhibitor.
Clinical trials
Fostamatinib has been in phase II trials for rheumatoid arthritis, autoimmune thrombocytopenia and lymphoma.[1][3]
A phase II study of rheumatoid arthritis patients failing to respond to a biologic agent showed little efficacy as compared to placebo, but the drug was well tolerated. In patients with high inflammatory burden, measured by levels of C-reactive protein, ACR20 was achieved by a significantly higher portion of those in the fostamatinib group (42%) versus the placebo group (26%).[4]
On June 4, 2013, Astra Zeneca announced they were giving up future development on the compound, and terminated their license with Rigel after early results from a Phase IIb study for rheumatoid arthritis. Astra Zeneca is estimated to lose $140 million as part of the contract termination.[5] Rigel is currently conducting two phase III studies on fostamatnib for ITP. Results are expected in the middle of 2016.
External links
- Rigel Pharmaceuticals http://www.rigel.com/rigel/ITP
References
- ↑ 1.0 1.1 Lua error in package.lua at line 80: module 'strict' not found.
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- ↑ Rigel to cut 30 jobs, focus on three drug programs, Sept 5th 2013, http://www.bizjournals.com/sanfrancisco/blog/biotech/2013/09/rigel-fostamatinib-itp-rigl-layoffs.html
