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Volumn 12, Issue 3, 2009, Pages 174-185

Fostamatinib, a Syk inhibitor prodrug for the treatment of inflammatory diseases

(1)  Bajpai, M a  

a NONE   (India)

Author keywords

[No Author keywords available]

Indexed keywords

ABT 325; ADALIMUMAB; AKR 501; AMG 714; ATLIZUMAB; B LYMPHOCYTE RECEPTOR; CANAKINUMAB; CYCLOPHOSPHAMIDE; DOXORUBICIN; ELTROMBOPAG; ETANERCEPT; FOSTAMATINIB; GMA 161; INFLIXIMAB; INTERLEUKIN 1; INTERLEUKIN 18; INTERLEUKIN 6; LGD 4665; METHOTREXATE; OCRELIZUMAB; PICEATANNOL; PLACEBO; PREDNISOLONE; PREDNISONE; PROTEIN KINASE SYK INHIBITOR; R 406; RECOMBINANT INTERLEUKIN 1 RECEPTOR BLOCKING AGENT; RITUXIMAB; ROMIPLOSTIM; STEROID; UNCLASSIFIED DRUG; VINCRISTINE;

EID: 62249125407     PISSN: 13697056     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (52)

References (89)
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    • 962289 Treatment of rheumatoid arthritis with a Syk kinase inhibitor: A twelve-week, randomized, placebo-controlled trial. Weinblatt ME, Kavanaugh A, Burgos-Vargas R, Dikranian AH, Medrano-Ramirez G, Morales-Torres JL, Murphy FT, Musser TK, Straniero N, Vicente-Gonzales AV, Grossbard E ARTHRITIS RHEUM 2008 58 11 3309-3318 •• Presents data from a phase II, multicenter, double-blind, randomized, placebo-controlled, dose-escalating clinical trial (NCT00326339) in methotrexate-resistant patients with RA (n = 189) administered fostamatinib (50, 100 and 150 mg po, bid) for 12 weeks. The 100- and 150-mg fostamatinib dose groups resulted in higher ACR20, ACR50, ACR70 and DAS28 response rates than the other two groups. The ACR20 response rates were 38, 32, 65 and 72% in the placebo, 50-, 100- and 150-mg fostamatinib groups, respectively; ACR50 response rates were 19, 17, 49 and 57% in the respective groups; ACR70 response rates were 4, 2, 33 and 40%, respectively, and the DAS28 response rates were 17, 20, 35 and 47%, respectively. Levels of IL-6 and MMP3 were significantly decreased from baseline at doses of 100 and 150 mg, and the onset of effects occurred within 1 week of treatment. Fostamatinib was generally well tolerated. The most common side effects occurred at the 150-mg dose, and were diarrhea (in 45% of patients), neutropenia (15%), dizziness (11%) and high blood pressure (5%).
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