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Fostamatinib for the treatment of adult persistent and chronic immune thrombocytopenia: Results of two phase 3, randomized, placebo-controlled trials.

Bussel J, Arnold DM, Grossbard E, Mayer J, TreliƄski J, Homenda W, Hellmann A, Windyga J, Sivcheva L, Khalafallah AA, Zaja F, Cooper N, Markovtsov V, Zayed H, Duliege AM.

Am J Hematol. 2018 Jul;93(7):921-930. doi: 10.1002/ajh.25125. Epub 2018 May 15.


Effects of CYP3A4 Inhibitors Ketoconazole and Verapamil and the CYP3A4 Inducer Rifampicin on the Pharmacokinetic Parameters of Fostamatinib: Results from In Vitro and Phase I Clinical Studies.

Martin P, Gillen M, Millson D, Oliver S, Brealey C, Grossbard EB, Baluom M, Lau D, Sweeny D, Mant T, Craven K.

Drugs R D. 2016 Mar;16(1):81-92. doi: 10.1007/s40268-015-0118-4.


Effects of fostamatinib (R788), an oral spleen tyrosine kinase inhibitor, on health-related quality of life in patients with active rheumatoid arthritis: analyses of patient-reported outcomes from a randomized, double-blind, placebo-controlled trial.

Weinblatt ME, Kavanaugh A, Genovese MC, Jones DA, Musser TK, Grossbard EB, Magilavy DB.

J Rheumatol. 2013 Apr;40(4):369-78. doi: 10.3899/jrheum.120923. Epub 2013 Feb 1.


An oral Syk kinase inhibitor in the treatment of rheumatoid arthritis: a three-month randomized, placebo-controlled, phase II study in patients with active rheumatoid arthritis that did not respond to biologic agents.

Genovese MC, Kavanaugh A, Weinblatt ME, Peterfy C, DiCarlo J, White ML, O'Brien M, Grossbard EB, Magilavy DB.

Arthritis Rheum. 2011 Feb;63(2):337-45. doi: 10.1002/art.30114.


Fostamatinib, a Syk-kinase inhibitor, does not affect methotrexate pharmacokinetics in patients with rheumatoid arthritis.

Baluom M, Samara E, Grossbard EB, Lau DT.

J Clin Pharmacol. 2011 Sep;51(9):1310-8. doi: 10.1177/0091270010381496. Epub 2011 Jan 5.


An oral spleen tyrosine kinase (Syk) inhibitor for rheumatoid arthritis.

Weinblatt ME, Kavanaugh A, Genovese MC, Musser TK, Grossbard EB, Magilavy DB.

N Engl J Med. 2010 Sep 30;363(14):1303-12. doi: 10.1056/NEJMoa1000500. Epub 2010 Sep 22.


Contribution of gut bacteria to the metabolism of the spleen tyrosine kinase (Syk) inhibitor R406 in cynomolgus monkey.

Sweeny DJ, Li W, Grossbard E, Lau DT.

Xenobiotica. 2010 Jun;40(6):415-23. doi: 10.3109/00498251003734244.


Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans: contribution of hepatic and gut bacterial processes to the overall biotransformation.

Sweeny DJ, Li W, Clough J, Bhamidipati S, Singh R, Park G, Baluom M, Grossbard E, Lau DT.

Drug Metab Dispos. 2010 Jul;38(7):1166-76. doi: 10.1124/dmd.110.032151. Epub 2010 Apr 6.


Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen.

McLaughlin J, Markovtsov V, Li H, Wong S, Gelman M, Zhu Y, Franci C, Lang D, Pali E, Lasaga J, Low C, Zhao F, Chang B, Gururaja TL, Xu W, Baluom M, Sweeny D, Carroll D, Sran A, Thota S, Parmer M, Romane A, Clemens G, Grossbard E, Qu K, Jenkins Y, Kinoshita T, Taylor V, Holland SJ, Argade A, Singh R, Pine P, Payan DG, Hitoshi Y.

J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113. doi: 10.1007/s00432-009-0641-1.


JAK3 inhibition significantly attenuates psoriasiform skin inflammation in CD18 mutant PL/J mice.

Chang BY, Zhao F, He X, Ren H, Braselmann S, Taylor V, Wicks J, Payan DG, Grossbard EB, Pine PR, Bullard DC.

J Immunol. 2009 Aug 1;183(3):2183-92. doi: 10.4049/jimmunol.0804063. Epub 2009 Jul 13.


Developmental toxicity associated with receptor tyrosine kinase Ret inhibition in reproductive toxicity testing.

Clemens GR, Schroeder RE, Magness SH, Weaver EV, Lech JW, Taylor VC, Masuda ES, Baluom M, Grossbard EB.

Birth Defects Res A Clin Mol Teratol. 2009 Feb;85(2):130-6. doi: 10.1002/bdra.20505.


Of mice and men: an open-label pilot study for treatment of immune thrombocytopenic purpura by an inhibitor of Syk.

Podolanczuk A, Lazarus AH, Crow AR, Grossbard E, Bussel JB.

Blood. 2009 Apr 2;113(14):3154-60. doi: 10.1182/blood-2008-07-166439. Epub 2008 Dec 18.


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 Nov;58(11):3309-18. doi: 10.1002/art.23992.


An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus.

Bahjat FR, Pine PR, Reitsma A, Cassafer G, Baluom M, Grillo S, Chang B, Zhao FF, Payan DG, Grossbard EB, Daikh DI.

Arthritis Rheum. 2008 May;58(5):1433-44. doi: 10.1002/art.23428.


Inflammation and bone erosion are suppressed in models of rheumatoid arthritis following treatment with a novel Syk inhibitor.

Pine PR, Chang B, Schoettler N, Banquerigo ML, Wang S, Lau A, Zhao F, Grossbard EB, Payan DG, Brahn E.

Clin Immunol. 2007 Sep;124(3):244-57. Epub 2007 May 29.


Immunotoxicity assessment for the novel Spleen tyrosine kinase inhibitor R406.

Zhu Y, Herlaar E, Masuda ES, Burleson GR, Nelson AJ, Grossbard EB, Clemens GR.

Toxicol Appl Pharmacol. 2007 Jun 15;221(3):268-77. Epub 2007 Mar 31.


R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation.

Braselmann S, Taylor V, Zhao H, Wang S, Sylvain C, Baluom M, Qu K, Herlaar E, Lau A, Young C, Wong BR, Lovell S, Sun T, Park G, Argade A, Jurcevic S, Pine P, Singh R, Grossbard EB, Payan DG, Masuda ES.

J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. Epub 2006 Aug 31. Erratum in: J Pharmacol Exp Ther. 2013 May;345(2):326.


Mast cell inhibitor R112 is well tolerated and affects prostaglandin D2 but not other mediators, symptoms, or nasal volumes in a nasal challenge model of allergic rhinitis.

Guyer BJ, Shimamoto SR, Bradhurst AL, Grossbard EB, Dreskin SC, Nelson HS.

Allergy Asthma Proc. 2006 May-Jun;27(3):208-13.


An intranasal Syk-kinase inhibitor (R112) improves the symptoms of seasonal allergic rhinitis in a park environment.

Meltzer EO, Berkowitz RB, Grossbard EB.

J Allergy Clin Immunol. 2005 Apr;115(4):791-6.


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