The status of fostamatinib in the treatment of rheumatoid arthritis

Expert Review of Clinical Immunology

Volumn 8, Issue 7, 2012, Pages 609-615

  Morales Torres, Jorge ^a  

^a Hospital Aranda de la Parra   (Mexico)

Author keywords

fostamatinib; kinase inhibitors; rheumatoid arthritis; SYK kinase

Indexed keywords

CYTOKINE; DISEASE MODIFYING ANTIRHEUMATIC DRUG; FOSTAMATINIB; METHOTREXATE; PAMAPIMOD; PLACEBO; TOFACITINIB; VX 702;

ABDOMINAL PAIN; ALGORITHM; AMINOTRANSFERASE BLOOD LEVEL; ARTICLE; CHRONIC LYMPHATIC LEUKEMIA; CLINICAL TRIAL; COUGHING; CYTOKINE PRODUCTION; DIARRHEA; DIZZINESS; DRUG EFFICACY; DRUG HALF LIFE; DRUG SAFETY; HUMAN; HYPERTENSION; HYPOTHYROIDISM; NAUSEA; NEUTROPENIA; NONHODGKIN LYMPHOMA; NONHUMAN; RHEUMATOID ARTHRITIS; SIDE EFFECT; SINGLE DRUG DOSE; TREATMENT RESPONSE; UPPER RESPIRATORY TRACT INFECTION; URINARY TRACT INFECTION;

ADMINISTRATION, ORAL; ANTIRHEUMATIC AGENTS; ARTHRITIS, RHEUMATOID; CLINICAL TRIALS AS TOPIC; HUMANS; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; OXAZINES; PRODRUGS; PROTEIN-TYROSINE KINASES; PYRIDINES; TREATMENT OUTCOME;

EID: 84867804298     PISSN: 1744666X     EISSN: 17448409     Source Type: Journal    
DOI: 10.1586/eci.12.63     Document Type: Article

References (32)

1. MacGregor AJ, Silman AJ. Classification and epidemiology. In: Rheumatology (4th Edition). Hochberg MC, Silman AJ, Smolen JS, Weinblatt ME, Weisman MH (Eds). Mosby Elsevier, Philadelphia, PA, USA, 755-761 (2008).
2. Saag KG, Teng GG, Patkar NM et al. American College of Rheumatology. American College of Rheumatology 2008 recommendations for the use of nonbiologic and biologic disease-modifying antirheumatic drugs in rheumatoid arthritis. Arthritis Rheum. 59(6), 762-784 (2008). (Pubitemid 351847559)
3. McInnes IB, Schett G. The pathogenesis of rheumatoid arthritis. N. Engl. J. Med. 365(23), 2205-2219 (2011).
4. Wong BR, Grossbard EB, Payan DG, Masuda ES. Targeting SYK as a treatment for allergic and autoimmune disorders. Expert Opin. Investig. Drugs 13(7), 743-762 (2004). (Pubitemid 39028928)
5. Cha HS, Boyle DL, Inoue T et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J. Pharmacol. Exp. Ther. 317(2), 571-578 (2006).
6. Braselmann S, Taylor V, Zhao H et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J. Pharmacol. Exp. Ther. 319(3), 998-1008 (2006).
7. Pine PR, Chang B, Schoettler N et al. Inflammation and bone erosion are suppressed in models of rheumatoid arthritis following treatment with a novel SYK inhibitor. Clin. Immunol. 124(3), 244-257 (2007). (Pubitemid 47247604)
8. Sweeny DJ, Li W, Clough J et al. 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. Drug Metab. Dispos. 38(7), 1166-1176 (2010).
9. Baluom M, Grossbard EB, Lau DT. Pharmacokinetics of fostamatinib, a novel SYK inhibitor in healthy human subjects following single and multiple oral dosing. Ann. Rheum. Dis. 70(Suppl. 3), 601 (2011).
10. Baluom M, Samara E, Grossbard EB, Lau DT. Fostamatinib, a SYK-kinase inhibitor, does not affect methotrexate pharmacokinetics in patients with rheumatoid arthritis. J. Clin. Pharmacol. 51(9), 1310-1318 (2011).
11. Weinblatt ME, Kavanaugh A, Burgos-Vargas R et al. Treatment of rheumatoid arthritis with a SYK kinase inhibitor: A twelve-week, randomized, placebo-controlled trial. Arthritis Rheum. 58(11), 3309-3318 (2008).
12. Weinblatt ME, Kavanaugh A, Genovese MC, Musser TK, Grossbard EB, Magilavy DB. An oral spleen tyrosine kinase (SYK) inhibitor for rheumatoid arthritis. N. Engl. J. Med. 363(14), 1303-1312 (2010).
13. Genovese MC, Kavanaugh A, Weinblatt ME et al. 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. Arthritis Rheum. 63(2), 337-345 (2011).
14. Weinblatt ME, Kavanaugh A, Jones DA et al. Effects of the oral SYK inhibitor, fostamatinib (R788), on health-related quality of life in a Phase II study of active rheumatoid arthritis. Arthritis Rheum. 63(Suppl.), 420 (2011).
15. Kavanaugh A, Weinblatt ME, Genovese MC et al. Longer-term safety of fostamatinib (R788) in patients with rheumatoid arthritis. Analysis of clinical trial data from up to 2 years of exposure. Arthritis Rheum. 63(Suppl.), 2594 (2011).
16. Tak PP, Kalden Jr. Advances in rheumatology: new targeted therapeutics. Arthritis Res. Ther. 13(Suppl. 1), S5 (2011).
17. Agarwal SK. Biologic agents for rheumatoid arthritis: An update for managed care professionals. J. Manag. Care Pharm. 17(Suppl. 9b), S14-S18 (2011).
18. Bajpai M, Chopra P, Dastidar SG, Ray A. Spleen tyrosine kinase: A novel target for therapeutic intervention of rheumatoid arthritis. Expert Opin. Investig. Drugs 17(5), 641-659 (2008). (Pubitemid 351843609)
19. Bajpai M. Fostamatinib, a SYK inhibitor prodrug for the treatment of inflammatory diseases. IDrugs 12(3), 174-185 (2009).
20. Morales-Torres J. R788 (fostamatinib disodium): A novel approach for the treatment of rheumatoid arthritis. Int. J. Clin. Rheumatology. 5, 9-15 (2010).
21. Cohen S. Small molecular therapies for rheumatoid arthritis: where do we stand? Expert Opin. Investig. Drugs 21(1), 23-31 (2012).
22. Pesu M, Laurence A, Kishore N, Zwillich SH, Chan G, O'Shea JJ. Therapeutic targeting of Janus kinases. Immunol. Rev. 223, 132-142 (2008). (Pubitemid 351986189)
23. Kremer JM, Bloom BJ, Breedveld FC et al. The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebocontrolled Phase IIa trial of three dosage levels of CP-690,550 versus placebo. Arthritis Rheum. 60(7), 1895-1905 (2009).
24. Cohen SB, Cheng TT, Chindalore V et al. Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis. Arthritis Rheum. 60(2), 335-344 (2009).
25. Damjanov N, Kauffman RS, Spencer-Green GT. Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebocontrolled clinical studies. Arthritis Rheum. 60(5), 1232-1241 (2009).
26. Karcher SC, Laufer SA. Successful structure-based design of recent p38 MAP kinase inhibitors. Curr. Top. Med. Chem. 9(7), 655-676 (2009).
27. Psaila B, Bussel JB. Fc receptors in immune thrombocytopenias: A target for immunomodulation? J. Clin. Invest. 118(8), 2677-2681 (2008).
28. Podolanczuk A, Lazarus AH, Crow AR, Grossbard E, Bussel JB. Of mice and men: An open-label pilot study for treatment of immune thrombocytopenic purpura by an inhibitor of SYK. Blood 113(14), 3154-3160 (2009).
29. Bahjat FR, Pine PR, Reitsma A et al. An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus. Arthritis Rheum. 58(5), 1433-1444 (2008). (Pubitemid 351705932)
30. Smith J, McDaid JP, Bhangal G et al. A spleen tyrosine kinase inhibitor reduces the severity of established glomerulonephritis. J. Am. Soc. Nephrol. 21(2), 231-236 (2010).
31. Friedberg JW, Sharman J, Sweetenham J et al. Inhibition of SYK with fostamatinib disodium has significant clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia. Blood 115(13), 2578-2585 (2010).
32. Efremov DG, Laurenti L. The SYK kinase as a therapeutic target in leukemia and lymphoma. Expert Opin. Investig. Drugs 20(5), 623-636 (2011).