Fostamatinib - CAS 901119-35-5
Catalog number:
901119-35-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C23H26FN6O9P
Molecular Weight:
580.46
COA:
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Targets:
Syk
Description:
Fostamatinib, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibiting Syk but not Lyn, and 5-fold less potent to Flt3.
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Purity:
>98%
Synonyms:
R788
MSDS:
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1.Fostamatinib, an oral spleen tyrosine kinase inhibitor, in the treatment of rheumatoid arthritis: a meta-analysis of randomized controlled trials.
Kunwar S1, Devkota AR2, Ghimire DK3. Rheumatol Int. 2016 Apr 25. [Epub ahead of print]
Fostamatinib is a selective inhibitor of spleen tyrosine kinase which has a role in the pathogenesis of RA. Multiple RCTs have been performed to study the effects of fostamatinib. The objective of this study was to perform a meta-analysis to analyze the efficacy and safety of fostamatinib in the management of RA. We searched PubMed, EMBASE and Cochrane CENTRAL through 11/9/15. Random effect model was used to estimate odds ratio (OR) and 95 % confidence interval. We measured outcomes with efficacy analysis using ACR20/50/70 response criteria and safety with adverse events. Five studies were included in the meta-analysis with total of 2105 patients including 1419 in fostamatinib group and 686 in placebo. Fostamatinib was effective in achieving ACR20, ACR50 and ACR70 responses compared to placebo (48 vs. 32.8 %, OR 1.86, 95 % CI 1.32-2.62, P = 0.0004, I 2 63 %; 26.4 vs. 12.5 %, OR 2.50, 95 % CI 1.93-3.23, P < 0.00001, I 2 0 % and 12.7 vs.
2.Effects of Fostamatinib on the Pharmacokinetics of Oral Contraceptive, Warfarin, and the Statins Rosuvastatin and Simvastatin: Results From Phase I Clinical Studies.
Martin P1, Gillen M2, Ritter J3, Mathews D4, Brealey C5, Surry D5, Oliver S6, Holmes V7, Severin P8, Elsby R6. Drugs R D. 2016 Mar;16(1):93-107. doi: 10.1007/s40268-015-0120-x.
BACKGROUND AND OBJECTIVES: Fostamatinib is a spleen tyrosine kinase inhibitor that has been investigated as therapy for rheumatoid arthritis and immune thrombocytopenic purpura. The present studies assessed the potential for pharmacokinetic interaction between fostamatinib and the commonly prescribed medications oral contraceptive (OC), warfarin, and statins (rosuvastatin, simvastatin) in healthy subjects.
3.Pharmacokinetic Properties of Fostamatinib in Patients With Renal or Hepatic Impairment: Results From 2 Phase I Clinical Studies.
Martin P1, Oliver S2, Gillen M3, Marbury T4, Millson D2. Clin Ther. 2015 Dec 1;37(12):2823-36. doi: 10.1016/j.clinthera.2015.09.016. Epub 2015 Oct 27.
PURPOSE: Phase III trials of fostamatinib, an oral spleen tyrosine kinase inhibitor, in the treatment of rheumatoid arthritis have been completed. Herein, we report the effects of renal and hepatic impairment on the pharmacokinetic (PK) properties of the active metabolite of fostamatinib, R406, in plasma, and on the urinary excretion of R406 and its metabolite N-glucuronide.
4.A phase II trial to evaluate the efficacy of fostamatinib in patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL).
Flinn IW1, Bartlett NL2, Blum KA3, Ardeshna KM4, LaCasce AS5, Flowers CR6, Shustov AR7, Thress KS8, Mitchell P8, Zheng F9, Skolnik JM9, Friedberg JW10. Eur J Cancer. 2016 Feb;54:11-7. doi: 10.1016/j.ejca.2015.10.005. Epub 2015 Dec 18.
PURPOSE: To assess the safety and efficacy of fostamatinib in patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL).
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CAS 901119-35-5 Fostamatinib

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