Fostamatinib
 Fostamatinib | |
 Fostamatinib disodium | |
| 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 | |
| Other names
Tamatinib fosdium; R-788; NSC-745942; R-935788 | |
| Identifiers | |
901119-35-5  1025687-58-4 (fostamatinib disodium) | |
| ChEMBL | ChEMBL2103830 |
| ChemSpider | 9846198 |
| 7796 | |
| Jmol interactive 3D | Image |
| PubChem | 11671467 25008120 (fostamatinib disodium) |
| UNII | SQ8A3S5101 |
| |
| |
| Properties | |
| C23H26FN6O9P | |
| Molar mass | 580.47 g·mol−1 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| 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 2 S.P. McAdoo and F.W.K. Tam (2011). "Fostamatinib Disodium". Drugs of the Future 36 (4): 273–280.
- ↑ Braselmann, S; Taylor, V; Zhao, H; Wang, S; Sylvain, C; Baluom, M; Qu, K; Herlaar, E; et al. (2006). "R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation". The Journal of Pharmacology and Experimental Therapeutics 319 (3): 998–1008. doi:10.1124/jpet.106.109058. PMID 16946104.
- ↑ Morales-Torres, Jorge (2010). "R788 (fostamatinib disodium): a novel approach for the treatment of rheumatoid arthritis". International Journal of Clinical Rheumatology 5 (1): 9–15. doi:10.2217/ijr.09.69.
- ↑ "Fostamatinib Shown to Be Safe but Not Effective in Rheumatoid Arthritis Patients Unresponsive to Biologic Agents". Science Daily. Jan 27, 2011. Retrieved Dec 13, 2012.
- ↑ 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