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Fostamatinib (R778) is a prodrug designed to deliver the active metabolite R406 which is an inhibitor of SYK and is currently under investigation for treatment of RA. The three clinical trials, conducted in healthy subjects, included two ascending dose studies and a formulation study. The first was a single ascending dose of R406, from 80-600mg, the second was a single and multiple dose study of fostamatinib in aqueous solution with single doses from 80-400mg and multiple doses of 160mg twice daily, and the third a study comparing suspension and tablet formulation of fostamatinib. The studies showed that fostamatinib has a rapid and extensive conversion rate to R406 and the PK profile suggests potential for a once- or twice- daily oral administration, with the solid dosage formulation of fostamatinib overcoming the low aqueous solubility of R406.

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