Abstract

R788 (fostamatinib disodium) is a prodrug rapidly converted to R406 upon oral administration. R406 is a potent inhibitor of spleen tyrosine kinase, required for the expression of a number of proinflammatory cytokines. R788 has shown efficacy in the control of patients with rheumatoid arthritis not responding to methotrexate, and some degree of response in those failing to respond to biologic agents with a reasonable safety pattern. It shows linear pharmacokinetics at the studied doses and it is not affected by the administration of methotrexate. The clinical applicability of R788 may have an impact in patients with rheumatoid arthritis failing to respond to conventional therapy. Once the Phase III studies are completed, R788 may find a place in the evolving treatment algorithm for rheumatoid arthritis.

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