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The status of fostamatinib in the treatment of rheumatoid arthritis.
- Source :
-
Expert review of clinical immunology [Expert Rev Clin Immunol] 2012 Sep; Vol. 8 (7), pp. 609-15. - Publication Year :
- 2012
-
Abstract
- Fostamatinib (R788) is a prodrug rapidly converted to its active metabolite on oral administration. This (known as R406) is a potent inhibitor of spleen tyrosine kinase, required for the expression of a number of proinflammatory cytokines. Fostamatinib has shown significantly superior efficacy (when compared with placebo) in the control of patients with rheumatoid arthritis not responding to methotrexate in Phase II clinical trials. Treatment emergent adverse events with a higher frequency than in those on placebo included diarrhea, hypertension, urinary tract infections, neutropenia and elevated transaminases. The studied doses have shown a linear pharmacokinetic pattern and the administration of methotrexate does not affect it. Fostamatinib may have a role in the therapy of patients with rheumatoid arthritis with poor response to conventional therapy. If these results are confirmed once Phase III studies are completed, it may find a place in the evolving treatment algorithm for rheumatoid arthritis.
- Subjects :
- Administration, Oral
Aminopyridines
Antirheumatic Agents administration & dosage
Antirheumatic Agents adverse effects
Arthritis, Rheumatoid physiopathology
Clinical Trials as Topic
Humans
Morpholines
Oxazines administration & dosage
Oxazines adverse effects
Prodrugs administration & dosage
Prodrugs adverse effects
Prodrugs therapeutic use
Pyridines administration & dosage
Pyridines adverse effects
Pyrimidines
Syk Kinase
Treatment Outcome
Antirheumatic Agents therapeutic use
Arthritis, Rheumatoid drug therapy
Intracellular Signaling Peptides and Proteins antagonists & inhibitors
Oxazines therapeutic use
Protein-Tyrosine Kinases antagonists & inhibitors
Pyridines therapeutic use
Subjects
Details
- Language :
- English
- ISSN :
- 1744-8409
- Volume :
- 8
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Expert review of clinical immunology
- Publication Type :
- Academic Journal
- Accession number :
- 23078058
- Full Text :
- https://doi.org/10.1586/eci.12.63