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411325 Rigel and Albany sign asthma/allergy program agreement. Rigel Pharmaceuticals Inc PRESS RELEASE 2001 May 31
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411325 Rigel and Albany sign asthma/allergy program agreement. Rigel Pharmaceuticals Inc PRESS RELEASE 2001 May 31
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62249092699
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455616 Kineret, Amgen's novel treatment for rheumatoid arthritis, offers dramatic improvement in patient function. Amgen Inc Pres Release 2002 June 13
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455616 Kineret, Amgen's novel treatment for rheumatoid arthritis, offers dramatic improvement in patient function. Amgen Inc Pres Release 2002 June 13
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62249182679
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500103 Remicade. Centocor Inc COMPANY WORLD WIDE WEB SITE 2003 August 05
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500103 Remicade. Centocor Inc COMPANY WORLD WIDE WEB SITE 2003 August 05
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62249130466
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553409 Drug datasheet: Enbrel etanercept, Wyeth DRUG DATASHEET WEBSITE 2004 April 30
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553409 Drug datasheet: Enbrel (etanercept). Wyeth DRUG DATASHEET WEBSITE 2004 April 30
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62249180366
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592531 Rigel completes phase I clinical trial of R406 in rheumatoid arthritis. Rigel Pharmaceuticals Inc PRESS RELEASE 2005 March 31
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592531 Rigel completes phase I clinical trial of R406 in rheumatoid arthritis. Rigel Pharmaceuticals Inc PRESS RELEASE 2005 March 31
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0037231533
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602678 Adalimumab, a fully human anti-tumor necrosis factor a monoclonal antibody, for the treatment of rheumatoid arthritis in patients taking concomitant methotrexate: The ARMADA trial. Weinblatt ME, Keystone EC, Furst DE, Moreland LW, Weisman MH, Birbara CA, Teoh LA, Fischkoff SA, Chartash EK ARTHRITIS RHEUM 2003 48 1 35-45
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602678 Adalimumab, a fully human anti-tumor necrosis factor a monoclonal antibody, for the treatment of rheumatoid arthritis in patients taking concomitant methotrexate: The ARMADA trial. Weinblatt ME, Keystone EC, Furst DE, Moreland LW, Weisman MH, Birbara CA, Teoh LA, Fischkoff SA, Chartash EK ARTHRITIS RHEUM 2003 48 1 35-45
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62249113171
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611180 Rigel's productivity on track: HCV and R&D pipeline update. Rigel Pharmaceuticals Inc PRESS RELEASE 2005 July 06
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611180 Rigel's productivity on track: HCV and R&D pipeline update. Rigel Pharmaceuticals Inc PRESS RELEASE 2005 July 06
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634278 Rigel announces presentation of phase I data on R406/788 at the American College of Rheumatology (ACR) annual meeting. Rigel Pharmaceuticals Inc PRESS RELEASE 2005 November 14
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634278 Rigel announces presentation of phase I data on R406/788 at the American College of Rheumatology (ACR) annual meeting. Rigel Pharmaceuticals Inc PRESS RELEASE 2005 November 14
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62249209889
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635953 Ligand announces preliminary revenue estimates For third quarter of fiscal 2005, preliminary results for first and second quarters of fiscal 2005 and filing of 10-K and audited results for fiscal 2004, 2003, and 2002. Ligand Pharmaceuticals Inc PRESS RELEASE 2005 November 18
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635953 Ligand announces preliminary revenue estimates For third quarter of fiscal 2005, preliminary results for first and second quarters of fiscal 2005 and filing of 10-K and audited results for fiscal 2004, 2003, and 2002. Ligand Pharmaceuticals Inc PRESS RELEASE 2005 November 18
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640784 Inhibition of immune thrombocytopenic purpura (ITP) by an orally bioavailable inhibitor of Syk kinase activity. Crow AR, Siragam A, Freedman, Grossard EB, Masuda ES, Pine P, Lazarus AH BLOOD 2005 106 11 Abs 2165
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640784 Inhibition of immune thrombocytopenic purpura (ITP) by an orally bioavailable inhibitor of Syk kinase activity. Crow AR, Siragam A, Freedman, Grossard EB, Masuda ES, Pine P, Lazarus AH BLOOD 2005 106 11 Abs 2165
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62249110538
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641305 An orally bioavailable inhibitor of FLT3 and Syk kinases prevents tumor growth in subcutaneously implanted human tumor xenografts and promotes cell death of FLT3 mutant AML cells. Pine PR, Bahjat R, Chang B, Taylor V, Markovstov V, Hitoshi Y, Grossbard E BLOOD 2005 106 11 Abs 243
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641305 An orally bioavailable inhibitor of FLT3 and Syk kinases prevents tumor growth in subcutaneously implanted human tumor xenografts and promotes cell death of FLT3 mutant AML cells. Pine PR, Bahjat R, Chang B, Taylor V, Markovstov V, Hitoshi Y, Grossbard E BLOOD 2005 106 11 Abs 243
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2942537697
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654479 Efficacy of B-cell-targeted therapy with rituximab in patients with rheumatoid arthritis. Edwards JC, Szczepanski L, Szechinski J, Filipowicz-Sosnowska A, Emery P, Close DR, Stevens RM, Shaw T N ENGL J MED 2004 350 25 2572-2581
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654479 Efficacy of B-cell-targeted therapy with rituximab in patients with rheumatoid arthritis. Edwards JC, Szczepanski L, Szechinski J, Filipowicz-Sosnowska A, Emery P, Close DR, Stevens RM, Shaw T N ENGL J MED 2004 350 25 2572-2581
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62249099496
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688626 Rigel begins phase II RA trial of R-788. Rigel Pharmaceuticals Inc PRESS RELEASE 2006 September 06
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688626 Rigel begins phase II RA trial of R-788. Rigel Pharmaceuticals Inc PRESS RELEASE 2006 September 06
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62249155842
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733002 Preclinical and early clinical development of an oral inhibitor of Syk kinase. Grossbard E INFLAMM RES 2006 55 Suppl 5 Abs SA42
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733002 Preclinical and early clinical development of an oral inhibitor of Syk kinase. Grossbard E INFLAMM RES 2006 55 Suppl 5 Abs SA42
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15
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33748123744
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737636 Lack of efficacy of a third tumour necrosis factor α antagonist after failure of a soluble receptor and a monoclonal antibody. Solau-Gervais E, Laxenaire N, Cortet B, Dubucquoi S, Duquesnoy B, Flipo RM RHEUMATOLOGY 2006 45 9 1121-1124
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737636 Lack of efficacy of a third tumour necrosis factor α antagonist after failure of a soluble receptor and a monoclonal antibody. Solau-Gervais E, Laxenaire N, Cortet B, Dubucquoi S, Duquesnoy B, Flipo RM RHEUMATOLOGY 2006 45 9 1121-1124
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62249191706
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747256 GMA161 treatment of refractory ITP: Efficacy of Fc-RIII blockade. Bussel JB, Patel V, Dunbar C, Lemery S, Tibbs K, Watts M, Magilavy D BLOOD 2006 108 11 Abs 1074
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747256 GMA161 treatment of refractory ITP: Efficacy of Fc-RIII blockade. Bussel JB, Patel V, Dunbar C, Lemery S, Tibbs K, Watts M, Magilavy D BLOOD 2006 108 11 Abs 1074
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749713 R406, an orally available spleen tyrosine kinase inhibitor blocks Fc receptor signaling and reduces immune complex-mediated inflammation. Braselmann S, Taylor V, Zhao HR, Wang S, Sylvain C, Baluom M, Qu KB, Herlaar E, Lau A, Young C, Wong BR et al J PHARMACOL EXP THER 2006 319 3 998-1008 •• Presents data from in vitro studies that demonstrated that R-406 was a potent inhibitor of FcRε-dependent activation (EC50, 43 nM, the IgE-mediated degranulation of CHMCs and the release of LTC4, cytokines and chemokines (including TNFα and IL-8) were inhibited by R-406. R-406 was selective for the inhibition of Syk activity (IC50, 41 nM; 78% inhibition at 0.3 μM) and inhibited Syk-dependent pathways mediated by FcRγ signaling in human mast cells, macrophages and neutrophils. In mouse arthritis models, R-406 reduced arthritis progression, inflammation and damage to the joints compared with vehicle-treate
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50 = 41 nM; 78% inhibition at 0.3 μM) and inhibited Syk-dependent pathways mediated by FcRγ signaling in human mast cells, macrophages and neutrophils. In mouse arthritis models, R-406 reduced arthritis progression, inflammation and damage to the joints compared with vehicle-treated animals.
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62249167675
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753925 Antibody therapeutics, IBC's Fourth Annual International Conference, Advancing Clinical Development of Therapeutic Antibodies, San Diego, CA, USA. Camacho LH IDDB MEETING REPORT 2006 December 10-14
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753925 Antibody therapeutics - IBC's Fourth Annual International Conference, Advancing Clinical Development of Therapeutic Antibodies, San Diego, CA, USA. Camacho LH IDDB MEETING REPORT 2006 December 10-14
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62249169616
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755759 Rigel starts US phase II study of R-788 for ITP. Rigel Pharmaceuticals Inc PRESS RELEASE 2007 January 08
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755759 Rigel starts US phase II study of R-788 for ITP. Rigel Pharmaceuticals Inc PRESS RELEASE 2007 January 08
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62249118835
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761158 Deregulated Syk inhibits differentiation and induces growth factor-independent proliferation of pre-B cells. Wossning T, Herzog S, Kohler F, Meixlsperger S, Kulathu Y, Mittler G, Abe A, Fuchs U, Borkhardt A, Jumaa H J EXP MED 2006 203 13 2829-2840 • Presents data from an in vitro study in pre-B-cells transformed by the Syk variant TEL-Syk. R-406 reduced the proliferation of tumorigenic pre-B-cells, reduced Syk-induced c-Myc expression and allowed the differentiation of Syk-transformed pre-B-cells into mature B-cells
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761158 Deregulated Syk inhibits differentiation and induces growth factor-independent proliferation of pre-B cells. Wossning T, Herzog S, Kohler F, Meixlsperger S, Kulathu Y, Mittler G, Abe A, Fuchs U, Borkhardt A, Jumaa H J EXP MED 2006 203 13 2829-2840 • Presents data from an in vitro study in pre-B-cells transformed by the Syk variant TEL-Syk. R-406 reduced the proliferation of tumorigenic pre-B-cells, reduced Syk-induced c-Myc expression and allowed the differentiation of Syk-transformed pre-B-cells into mature B-cells.
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33645867986
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771815 A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. Cha HS, Boyle DL, Inoue T, Schoot R, Tak PP, Pine P, Firestein GS J PHARMACOL EXP THER 2006 317 2 571-578
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771815 A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. Cha HS, Boyle DL, Inoue T, Schoot R, Tak PP, Pine P, Firestein GS J PHARMACOL EXP THER 2006 317 2 571-578
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62249133333
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782440 Rigel's R-788 raises platelet count in phase II ITP trial. Rigel Pharmaceuticals Inc PRESS RELEASE 2007 April 11
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782440 Rigel's R-788 raises platelet count in phase II ITP trial. Rigel Pharmaceuticals Inc PRESS RELEASE 2007 April 11
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825627 MGI Pharma signs agreement for rights to novel treatment for thrombocytopenia. MGI Pharma Inc PRESS RELEASE 2007 August 28
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825627 MGI Pharma signs agreement for rights to novel treatment for thrombocytopenia. MGI Pharma Inc PRESS RELEASE 2007 August 28
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62249109069
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858217 R935788: A phase II, single center, open label, efficacy and safety, ascending dose, pilot study for the treatment of adult immune thrombocytopenic purpura ITP, Bussel JB, Schindler AM, Grossbard EB AM SOC HEMATOL ANN MEET EXPOSITION 2007 49 December 8 Abs 1310
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858217 R935788: A phase II, single center, open label, efficacy and safety, ascending dose, pilot study for the treatment of adult immune thrombocytopenic purpura (ITP). Bussel JB, Schindler AM, Grossbard EB AM SOC HEMATOL ANN MEET EXPOSITION 2007 49 December 8 Abs 1310
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860425 Syk kinase inhibition by R406 inhibits BCR mediated B cell proliferation and interferes with BCR signal transduction in primary tumor samples. Sharman JP, Irish J, Hatton O, Martinez O, Levy R AM SOC HEMATOL ANN MEET EXPOSITION 2007 49 December 11 Abs 802 • Presents data demonstrating R-406 inhibited B-cell receptor-stimulated B-cell proliferation in primary B-cell lymphoma samples, with an IC50 value of 100 nM
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50 value of 100 nM.
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62249100999
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868738 Abbott's Humira (adalimumab) receives FDA approval for moderate to severe chronic plaque psoriasis. Abbott Laboratories PRESS RELEASE 2008 January 18
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868738 Abbott's Humira (adalimumab) receives FDA approval for moderate to severe chronic plaque psoriasis. Abbott Laboratories PRESS RELEASE 2008 January 18
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874487 Disease remission and sustained halting of radiographic progression with combination etanercept and methotrexate in patients with rheumatoid arthritis. van der Heijde D, Klareskog L, Landewe R, Bruyn GAW, Cantagrel A, Durez P, Herrero-Beaumont G, Molad Y, Codreanu C, Valentini G, Zahora R et al ARTHRITIS RHEUM 2007 56 12 3928-3939
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874487 Disease remission and sustained halting of radiographic progression with combination etanercept and methotrexate in patients with rheumatoid arthritis. van der Heijde D, Klareskog L, Landewe R, Bruyn GAW, Cantagrel A, Durez P, Herrero-Beaumont G, Molad Y, Codreanu C, Valentini G, Zahora R et al ARTHRITIS RHEUM 2007 56 12 3928-3939
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31344455373
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892126 Treatment of rheumatoid arthritis. Emery P Br Med J 2006 332 7534 152-155
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892126 Treatment of rheumatoid arthritis. Emery P Br Med J 2006 332 7534 152-155
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0142041982
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891727 Lasker clinical medical research award. TNF defined as a therapeutic target for rheumatoid arthritis and other autoimmune diseases. Feldmann M, Maini RN NAT MED 2003 9 10 1245-1250
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891727 Lasker clinical medical research award. TNF defined as a therapeutic target for rheumatoid arthritis and other autoimmune diseases. Feldmann M, Maini RN NAT MED 2003 9 10 1245-1250
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7044227564
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891738 Updated consensus statement on biological agents, specifically tumour necrosis factor α (TNFα) blocking agents and interleukin-1 receptor antagonist IL-1ra, for the treatment of rheumatic diseases, 2004. Furst DE, Breedveld FC, Kalden JR, Smolen JS, Burmester GR, Bijlsma JW, Dougados M, Emery P, Keystone EC, Klareskog L, Mease PJ ANN RHEUM DIS 2004 63 Suppl 2 2ii-12ii
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891738 Updated consensus statement on biological agents, specifically tumour necrosis factor α (TNFα) blocking agents and interleukin-1 receptor antagonist (IL-1ra), for the treatment of rheumatic diseases, 2004. Furst DE, Breedveld FC, Kalden JR, Smolen JS, Burmester GR, Bijlsma JW, Dougados M, Emery P, Keystone EC, Klareskog L, Mease PJ ANN RHEUM DIS 2004 63 Suppl 2 2ii-12ii
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85173421746
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892231 The use of biological agents in the treatment of rheumatoid arthritis. Fan PT, Leong KH ANN ACAD MED SINGAPORE 2007 36 2 128-134
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892231 The use of biological agents in the treatment of rheumatoid arthritis. Fan PT, Leong KH ANN ACAD MED SINGAPORE 2007 36 2 128-134
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894238 Rigel's R788 shows preclinical activity in type 1 diabetes model. Rigel Pharmaceuticals Inc PRESS RELEASE 2008 April 08
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894238 Rigel's R788 shows preclinical activity in type 1 diabetes model. Rigel Pharmaceuticals Inc PRESS RELEASE 2008 April 08
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900869 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 58 5 1433-1444
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900869 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 58 5 1433-1444
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912576 Preliminary phase 2 results of R788 in lymphoma show benefit in diffuse large B-cell and SLL/CLL. Rigel Pharmaceuticals Inc PRESS RELEASE 2008 June 03 •• Reports data from a phase I/II, multicenter, open-label clinical trial (NCT00446095) in patients with refractory or relapsed B-cell NHL (n, 68) who were administered fostamatinib 200 or 250 mg po, bid, Response rates were observed in 22% of patients with DLBCL, in 10% with follicular NHL, in 55% with CLL/SLL and in 11% with mantle cell lymphoma. Fostamatinib was generally well tolerated; five patients withdrew from the trial because of adverse events, including cytopenia and diarrhea
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912576 Preliminary phase 2 results of R788 in lymphoma show benefit in diffuse large B-cell and SLL/CLL. Rigel Pharmaceuticals Inc PRESS RELEASE 2008 June 03 •• Reports data from a phase I/II, multicenter, open-label clinical trial (NCT00446095) in patients with refractory or relapsed B-cell NHL (n = 68) who were administered fostamatinib (200 or 250 mg po, bid). Response rates were observed in 22% of patients with DLBCL, in 10% with follicular NHL, in 55% with CLL/SLL and in 11% with mantle cell lymphoma. Fostamatinib was generally well tolerated; five patients withdrew from the trial because of adverse events, including cytopenia and diarrhea.
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915976 Rigel initiates two phase 2b clinical trials of R788 in rheumatoid arthritis. Rigel Pharmaceuticals Inc PRESS RELEASE 2008 June 12
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915976 Rigel initiates two phase 2b clinical trials of R788 in rheumatoid arthritis. Rigel Pharmaceuticals Inc PRESS RELEASE 2008 June 12
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917341 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 2008 124 3 244-257
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917341 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 2008 124 3 244-257
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917342 Immunotoxicity assessment for the novel spleen tyrosine kinase inhibitor R406. Zhu YH, Herlaar E, Masuda ES, Burleson GR, Nelson AJ, Grossbard EB, Clemens GR TOXICOL APPL PHARMACOL 2007 221 3 268-277 •• Presents data from a 28-day toxicity study in rats administered R-406 10 or 100 mg/kg/day po, bid, A reversible reduction in lymphocytes, thymic and spleen weight, and bone marrow cellularity was observed at a dose of 100 mg/kg/day. R-406 did not cause any dose-dependent immunotoxicity and did not affect the innate and humoral immune responses
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917342 Immunotoxicity assessment for the novel spleen tyrosine kinase inhibitor R406. Zhu YH, Herlaar E, Masuda ES, Burleson GR, Nelson AJ, Grossbard EB, Clemens GR TOXICOL APPL PHARMACOL 2007 221 3 268-277 •• Presents data from a 28-day toxicity study in rats administered R-406 (10 or 100 mg/kg/day po, bid). A reversible reduction in lymphocytes, thymic and spleen weight, and bone marrow cellularity was observed at a dose of 100 mg/kg/day. R-406 did not cause any dose-dependent immunotoxicity and did not affect the innate and humoral immune responses.
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917343 A phase I randomized, double-blind, placebo-controlled, pharmacokinetic study of R788/406 and methotrexate in sixteen patients with rheumatoid arthritis. Grossbard E, Baluom M, Kivitz AJ ARTHRITIS RHEUM 2006 54 9 Abs 939
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917343 A phase I randomized, double-blind, placebo-controlled, pharmacokinetic study of R788/406 and methotrexate in sixteen patients with rheumatoid arthritis. Grossbard E, Baluom M, Kivitz AJ ARTHRITIS RHEUM 2006 54 9 Abs 939
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62249159584
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917485 Tonic B-cell receptor signaling promotes the survival of diffuse large B-cell lymphomas: Identification of Syk as a rational treatment target. Chen L, Juszczynski P, Hitoshi Y, Chen W, Kutok JL, Shipp MA BLOOD 2006 108 11 71A
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917485 Tonic B-cell receptor signaling promotes the survival of diffuse large B-cell lymphomas: Identification of Syk as a rational treatment target. Chen L, Juszczynski P, Hitoshi Y, Chen W, Kutok JL, Shipp MA BLOOD 2006 108 11 71A
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917491 A multiple dose study of an orally bioavailable inhibitor of SyK-kinase (R406) in human volunteers: Safety, pharmacokinetics (PK) and pharmacodynamics PD, Grossbard E, Mant T, Jurcevic S, Sterba M ARTHRITIS RHEUM 2005 52 9 Abs 1864
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917491 A multiple dose study of an orally bioavailable inhibitor of SyK-kinase (R406) in human volunteers: Safety, pharmacokinetics (PK) and pharmacodynamics (PD). Grossbard E, Mant T, Jurcevic S, Sterba M ARTHRITIS RHEUM 2005 52 9 Abs 1864
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62249094924
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917492 An orally bioavailable inhibitor of Syk kinase (R406) inhibits, dose responsively, human basophil CD63 expression following ex vivo Fcε receptor stimulation. Grossbard E, Mant T, Jurcevic S, Sterba M ARTHRITIS RHEUM 2005 52 9 Abs 1510
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917492 An orally bioavailable inhibitor of Syk kinase (R406) inhibits, dose responsively, human basophil CD63 expression following ex vivo Fcε receptor stimulation. Grossbard E, Mant T, Jurcevic S, Sterba M ARTHRITIS RHEUM 2005 52 9 Abs 1510
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62249111714
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931647 MacroGenics: At-a-glance. MacroGenics Inc COMPANY PUBLICATION 2008 August 05
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931647 MacroGenics: At-a-glance. MacroGenics Inc COMPANY PUBLICATION 2008 August 05
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54949144705
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954882 Ocrelizumab, a humanized monoclonal antibody against CD20 for inflammatory disorders and B-cell malignancies. Hutas G Cur Opin Invest Drugs 2008 9 11 1206-1215
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954882 Ocrelizumab, a humanized monoclonal antibody against CD20 for inflammatory disorders and B-cell malignancies. Hutas G Cur Opin Invest Drugs 2008 9 11 1206-1215
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62249217574
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956196 ACZ885 phase III data show rapid, sustained clinical remission in children and adults suffering from a group of rare, potentially life-threatening autoinflammatory diseases. Novartis AG Pres Release 2008 October 27
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956196 ACZ885 phase III data show rapid, sustained clinical remission in children and adults suffering from a group of rare, potentially life-threatening autoinflammatory diseases. Novartis AG Pres Release 2008 October 27
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62249202477
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958462 Rigel announces third quarter 2008 financial results and clinical update. Rigel Pharmaceuticals Inc PRESS RELEASE 2008 November 03
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958462 Rigel announces third quarter 2008 financial results and clinical update. Rigel Pharmaceuticals Inc PRESS RELEASE 2008 November 03
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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, respective
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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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965443 FDA approves Promacta eltrombopag, the first oral medication to increase platelet production for people with serious blood disorder. GlaxoSmithKline plc PRESS RELEASE 2008 November 20
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965443 FDA approves Promacta (eltrombopag), the first oral medication to increase platelet production for people with serious blood disorder. GlaxoSmithKline plc PRESS RELEASE 2008 November 20
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967106 Inhibition of BCR signaling using the Syk inhibitor R406 antagonizes migratory and pro-survival responses in CLL cells. Quiroga MP, Kurtova A, Wierda W, Keating M, Burger JA AM SOC HEMATOL ANN MEET EXPOSITION 2008 50 December 7 Abs 2064
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967106 Inhibition of BCR signaling using the Syk inhibitor R406 antagonizes migratory and pro-survival responses in CLL cells. Quiroga MP, Kurtova A, Wierda W, Keating M, Burger JA AM SOC HEMATOL ANN MEET EXPOSITION 2008 50 December 7 Abs 2064
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969246 Tocilizumab: An interleukin-6 receptor inhibitor for the treatment of rheumatoid arthritis. Plushner SL ANN PHARMACOTHER 2008 42 11 1660-1668
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969246 Tocilizumab: An interleukin-6 receptor inhibitor for the treatment of rheumatoid arthritis. Plushner SL ANN PHARMACOTHER 2008 42 11 1660-1668
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50
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62249184863
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971864 Ligand enters into exclusive license agreement with GlaxoSmithKline to license rights to LGD-4665 and other ligand thrombopoietin (TPO) molecules. Ligand Pharmaceuticals Inc PRESS RELEASE 2008 December 18
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971864 Ligand enters into exclusive license agreement with GlaxoSmithKline to license rights to LGD-4665 and other ligand thrombopoietin (TPO) molecules. Ligand Pharmaceuticals Inc PRESS RELEASE 2008 December 18
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51
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973962 International stem cell corporation discusses recent funding. International Stem Cell Corp PRESS RELEASE 2009 January 05
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973962 International stem cell corporation discusses recent funding. International Stem Cell Corp PRESS RELEASE 2009 January 05
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52
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974875 Syk-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Chen L, Monti S, Juszczynski P, Daley J, Chen W, Witzig TE, Habermann TM, Kutok JL, Shipp MA BLOOD 2008 111 4 2230-2237
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974875 Syk-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Chen L, Monti S, Juszczynski P, Daley J, Chen W, Witzig TE, Habermann TM, Kutok JL, Shipp MA BLOOD 2008 111 4 2230-2237
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974877 Combination of infliximab and methotrexate therapy for early rheumatoid arthritis: A randomized, controlled trial. St Clair EW, van der Heijde DM, Smolen JS, Maini RN, Bathon JM, Emery P, Keystone E, Schiff M, Kalden JR, Wang B, Dewoody K et al ARTHRITIS RHEUM 2004 50 11 3432-3443
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974877 Combination of infliximab and methotrexate therapy for early rheumatoid arthritis: A randomized, controlled trial. St Clair EW, van der Heijde DM, Smolen JS, Maini RN, Bathon JM, Emery P, Keystone E, Schiff M, Kalden JR, Wang B, Dewoody K et al ARTHRITIS RHEUM 2004 50 11 3432-3443
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974885 IL-1αβ blockade prevents cartilage and bone destruction in murine type II collagen-induced arthritis, whereas TNFα blockade only ameliorates joint inflammation. Joosten LA, Helsen MM, Saxne T, van De Loo FA, Heinegard D, van Den Berg WB J IMMUNOL 1999 163 9 5049-5055
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974885 IL-1αβ blockade prevents cartilage and bone destruction in murine type II collagen-induced arthritis, whereas TNFα blockade only ameliorates joint inflammation. Joosten LA, Helsen MM, Saxne T, van De Loo FA, Heinegard D, van Den Berg WB J IMMUNOL 1999 163 9 5049-5055
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974888 Safety and efficacy of rituximab in patients with rheumatoid arthritis refractory to disease modifying antirheumatic drugs and anti-tumor necrosis factor-α treatment. Higashida J, Wun T, Schmidt S, Naguwa SM, Tuscano JM J RHEUMATOL 2005 32 11 2109-2115
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974888 Safety and efficacy of rituximab in patients with rheumatoid arthritis refractory to disease modifying antirheumatic drugs and anti-tumor necrosis factor-α treatment. Higashida J, Wun T, Schmidt S, Naguwa SM, Tuscano JM J RHEUMATOL 2005 32 11 2109-2115
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974890 Lymphoma in rheumatoid arthritis: The effect of methotrexate and anti-tumor necrosis factor therapy in 18,572 patients. Wolfe F, Michaud K ARTHRITIS RHEUM 2004 50 6 1740-1751
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974890 Lymphoma in rheumatoid arthritis: The effect of methotrexate and anti-tumor necrosis factor therapy in 18,572 patients. Wolfe F, Michaud K ARTHRITIS RHEUM 2004 50 6 1740-1751
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974894 Treatment of rheumatoid arthritis with tumor necrosis factor inhibitors may predispose to significant increase in tuberculosis risk: A multicenter active-surveillance report. Gomez-Reino JJ, Carmona L, Valverde VR, Mola EM, Montero MD ARTHRITIS RHEUM 2003 48 8 2122-2127
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974894 Treatment of rheumatoid arthritis with tumor necrosis factor inhibitors may predispose to significant increase in tuberculosis risk: A multicenter active-surveillance report. Gomez-Reino JJ, Carmona L, Valverde VR, Mola EM, Montero MD ARTHRITIS RHEUM 2003 48 8 2122-2127
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974902 The epidemiology of non-Hodgkin's lymphoma. Fisher SG, Fisher RI ONCOGENE 2004 23 38 6524-6534
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974902 The epidemiology of non-Hodgkin's lymphoma. Fisher SG, Fisher RI ONCOGENE 2004 23 38 6524-6534
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974968 Syk-dependent mTOR activation in follicular lymphoma cells. Leseux L, Hamdi SM, Al Saati T, Capilla F, Recher C, Laurent G, Bezombes C BLOOD 2006 108 13 4156-4162
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974968 Syk-dependent mTOR activation in follicular lymphoma cells. Leseux L, Hamdi SM, Al Saati T, Capilla F, Recher C, Laurent G, Bezombes C BLOOD 2006 108 13 4156-4162
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975244 Inhibition of spleen tyrosine kinase prevents mast cell activation and airway hyperresponsiveness. Matsubara S, Li G, Takeda K, Loader JE, Pine P, Masuda ES, Miyahara N, Miyahara S, Lucas JJ, Dakhama A, Gelfand EW AM J RESPIR CRIT CARE MED 2006 173 1 56-63
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975244 Inhibition of spleen tyrosine kinase prevents mast cell activation and airway hyperresponsiveness. Matsubara S, Li G, Takeda K, Loader JE, Pine P, Masuda ES, Miyahara N, Miyahara S, Lucas JJ, Dakhama A, Gelfand EW AM J RESPIR CRIT CARE MED 2006 173 1 56-63
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975362 Targeting Syk kinase for the treatment of B-cell lymphoma. Sharman JP, Irish J, Coffey G, Czerwinski D, Hitoshi Y, Levy R AM SOC CLIN ONCOL 2007 25 18S Abs 3600
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975362 Targeting Syk kinase for the treatment of B-cell lymphoma. Sharman JP, Irish J, Coffey G, Czerwinski D, Hitoshi Y, Levy R AM SOC CLIN ONCOL 2007 25 18S Abs 3600
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975916 Treatment of rheumatoid arthritis with a Syk kinase inhibitor: A twelve-week, randomized, placebo-controlled trial. Weinblatt ME, Kavanaugh A, Grossbard E ARTHRITIS RHEUM 2008 58 11 Abs 1189
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975916 Treatment of rheumatoid arthritis with a Syk kinase inhibitor: A twelve-week, randomized, placebo-controlled trial. Weinblatt ME, Kavanaugh A, Grossbard E ARTHRITIS RHEUM 2008 58 11 Abs 1189
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976408 Pro- and anti-inflammatory cytokines in rheumatoid arthritis. Isomaki P, Punnonen J ANN MED 1997 29 6 499-507
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976408 Pro- and anti-inflammatory cytokines in rheumatoid arthritis. Isomaki P, Punnonen J ANN MED 1997 29 6 499-507
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64
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0033997615
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976412 Tyrosine kinase Syk: Essential functions for immunoreceptor signaling. Turner M, Schweighoffer E, Colucci F, Di Santo JP, Tybulewicz VL IMMUNOL TODAY 2000 21 3 148-154
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976412 Tyrosine kinase Syk: Essential functions for immunoreceptor signaling. Turner M, Schweighoffer E, Colucci F, Di Santo JP, Tybulewicz VL IMMUNOL TODAY 2000 21 3 148-154
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65
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976413 Treatment advances in adult immune thrombocytopenic purpura. Huber MR, Kumar S, Tefferi A ANN HEMATOL 2003 82 12 723-737
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976413 Treatment advances in adult immune thrombocytopenic purpura. Huber MR, Kumar S, Tefferi A ANN HEMATOL 2003 82 12 723-737
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66
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976414 Targeting Syk as a treatment for allergic and autoimmune disorders. Wong BR, Grossbard EB, Payan DG, Masuda ES EXPERT OPIN INVEST DRUGS 2004 13 7 743-762
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976414 Targeting Syk as a treatment for allergic and autoimmune disorders. Wong BR, Grossbard EB, Payan DG, Masuda ES EXPERT OPIN INVEST DRUGS 2004 13 7 743-762
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976415 Non-Hodgkin lymphoma: Diagnosis and treatment. Ansell SM, Armitage J MAYO CLIN PROC 2005 80 8 1087-1097
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976415 Non-Hodgkin lymphoma: Diagnosis and treatment. Ansell SM, Armitage J MAYO CLIN PROC 2005 80 8 1087-1097
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976421 Fc receptors in immune thrombocytopenias: A target for immunomodulation? Psaila B, Bussel JB J CLIN INVEST 2008 118 8 2677-2681
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976421 Fc receptors in immune thrombocytopenias: A target for immunomodulation? Psaila B, Bussel JB J CLIN INVEST 2008 118 8 2677-2681
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976422 Targeted treatment and new agents in diffuse large B-cell lymphoma. Leonard JP, Martin P, Barrientos J, Elstrom R SEMIN HEMATOL 2008 45 3 Suppl 2 S11-S16
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976422 Targeted treatment and new agents in diffuse large B-cell lymphoma. Leonard JP, Martin P, Barrientos J, Elstrom R SEMIN HEMATOL 2008 45 3 Suppl 2 S11-S16
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976423 Of mice and men: An open label pilot study for treatment of immune thrombocytopenic purpura (ITP) by an inhibitor of Syk. Podolanczuk A, Lazarus AH, Crow AR, Grossbard E, Bussel JB BLOOD 2008 doi:10.1182/blood-2008-07-166439 • Presents data from a phase II, single-center, open-label, ascending-dose, proof-of-concept clinical trial (NCT00706342) in patients with ITP (n, 16) administered fostamatinib (75 to 175 mg po, bid) for at least 30 days. In 8 patients, stable platelet counts of > 50,000 platelets/μl of blood were observed in > 67% of study visits, and 12 patients responded with a mean peak platelet count of > 100,000 platelets/μl of blood. The primary side effects were gastrointestinal-related symptoms, observed in 5 out of 14 evaluated patients; mild elevations in ALT were observed in 2 patients
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976423 Of mice and men: An open label pilot study for treatment of immune thrombocytopenic purpura (ITP) by an inhibitor of Syk. Podolanczuk A, Lazarus AH, Crow AR, Grossbard E, Bussel JB BLOOD 2008 doi:10.1182/blood-2008-07-166439 • Presents data from a phase II, single-center, open-label, ascending-dose, proof-of-concept clinical trial (NCT00706342) in patients with ITP (n = 16) administered fostamatinib (75 to 175 mg po, bid) for at least 30 days. In 8 patients, stable platelet counts of > 50,000 platelets/μl of blood were observed in > 67% of study visits, and 12 patients responded with a mean peak platelet count of > 100,000 platelets/μl of blood. The primary side effects were gastrointestinal-related symptoms, observed in 5 out of 14 evaluated patients; mild elevations in ALT were observed in 2 patients.
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71
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976435 The epidemiology of immune thrombocytopenic purpura. Fogarty PF, Segal JB CURR OPIN HEMATOL 2007 14 5 515-519
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976435 The epidemiology of immune thrombocytopenic purpura. Fogarty PF, Segal JB CURR OPIN HEMATOL 2007 14 5 515-519
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976436 Cancer stat fact sheets: Lymphoma. National Cancer Institute WEB SITE 2009 January 14
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976436 Cancer stat fact sheets: Lymphoma. National Cancer Institute WEB SITE 2009 January 14
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976437 Methotrexate. Medicinenet WEB SITE 2008 August 01
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976437 Methotrexate. Medicinenet WEB SITE 2008 August 01
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976459 Rigel Pharmaceuticals pipeline. Rigel Pharmaceuticals Inc COMPANY WORLD WIDE WEB SITE 2009 January 14
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976459 Rigel Pharmaceuticals pipeline. Rigel Pharmaceuticals Inc COMPANY WORLD WIDE WEB SITE 2009 January 14
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978166 The immunomodulatory adapter proteins DAP12 and Fc receptor γ-chain (FcRγ) regulate development of functional osteoclasts through the Syk tyrosine kinase. Mocsai A, Humphrey MB, Van Ziffle JA, Hu Y, Burghardt A, Spusta SC, Majumdar S, Lanier LL, Lowell CA, Nakamura MC PROC NATL ACAD SCI USA 2004 101 16 6158-6163
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978166 The immunomodulatory adapter proteins DAP12 and Fc receptor γ-chain (FcRγ) regulate development of functional osteoclasts through the Syk tyrosine kinase. Mocsai A, Humphrey MB, Van Ziffle JA, Hu Y, Burghardt A, Spusta SC, Majumdar S, Lanier LL, Lowell CA, Nakamura MC PROC NATL ACAD SCI USA 2004 101 16 6158-6163
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978168 Minimization of potential hERG liability in histamine H3 receptor antagonists. Black LA, Liu H, Diaz GJ, Fox GB, Browman KE, Wetter J, Marsh KC, Miller TR, Esbenshade TA, Brioni J, Cowart MD Inflam Res 2008 57 Suppl 1 S45-S46
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978168 Minimization of potential hERG liability in histamine H3 receptor antagonists. Black LA, Liu H, Diaz GJ, Fox GB, Browman KE, Wetter J, Marsh KC, Miller TR, Esbenshade TA, Brioni J, Cowart MD Inflam Res 2008 57 Suppl 1 S45-S46
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979218 Lupus nephritis: Update on pathogenesis and disease mechanisms. Foster MH, Kelley VR SEMIN NEPHROL 1999 19 2 173-181
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979218 Lupus nephritis: Update on pathogenesis and disease mechanisms. Foster MH, Kelley VR SEMIN NEPHROL 1999 19 2 173-181
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979219 Differential expression and molecular associations of Syk in systemic lupus erythematosus T cells. Krishnan S, Juang YT, Chowdhury B, Magilavy A, Fisher CU, Nguyen H, Nambiar MP, Kyttaris V, Weinstein A, Bahjat R, Pine P et al J IMMUNOL 2008 181 11 8145-8152
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979219 Differential expression and molecular associations of Syk in systemic lupus erythematosus T cells. Krishnan S, Juang YT, Chowdhury B, Magilavy A, Fisher CU, Nguyen H, Nambiar MP, Kyttaris V, Weinstein A, Bahjat R, Pine P et al J IMMUNOL 2008 181 11 8145-8152
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979220 Incidence and prevalence of rheumatoid arthritis, based on the 1987 American College of Rheumatology criteria: A systematic review. Alamanos Y, Voulgari PV, Drosos AA SEMIN ARTHRITIS RHEUM 2006 36 3 182-188
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979220 Incidence and prevalence of rheumatoid arthritis, based on the 1987 American College of Rheumatology criteria: A systematic review. Alamanos Y, Voulgari PV, Drosos AA SEMIN ARTHRITIS RHEUM 2006 36 3 182-188
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979221 The progression of erosion and joint space narrowing scores in rheumatoid arthritis during the first twenty-five years of disease. Sharp JT, Wolfe F, Mitchell DM, Bloch DA ARTHRITIS RHEUM 1991 34 6 660-668
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979221 The progression of erosion and joint space narrowing scores in rheumatoid arthritis during the first twenty-five years of disease. Sharp JT, Wolfe F, Mitchell DM, Bloch DA ARTHRITIS RHEUM 1991 34 6 660-668
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979223 The KRN mouse model of inflammatory arthritis. Kyburz D, Corr M SPRINGER SEMIN IMMUNOPATHOL 2003 25 1 79-90
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979223 The KRN mouse model of inflammatory arthritis. Kyburz D, Corr M SPRINGER SEMIN IMMUNOPATHOL 2003 25 1 79-90
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979224 Critical role for the tyrosine kinase Syk in signalling through the high affinity IgE receptor of mast cells. Costello PS, Turner M, Walters AE, Cunningham CN, Bauer PH, Downward J, Tybulewicz VL ONCOGENE 1996 13 12 2595-2605
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979224 Critical role for the tyrosine kinase Syk in signalling through the high affinity IgE receptor of mast cells. Costello PS, Turner M, Walters AE, Cunningham CN, Bauer PH, Downward J, Tybulewicz VL ONCOGENE 1996 13 12 2595-2605
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979225 TNF antagonist safety in rheumatoid arthritis: Updated evidence from observational registries. Nasir A, Greenberg JD BULL NYU HOSP JT DIS 2007 65 3 178-181
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979225 TNF antagonist safety in rheumatoid arthritis: Updated evidence from observational registries. Nasir A, Greenberg JD BULL NYU HOSP JT DIS 2007 65 3 178-181
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979226 Are modified-release corticosteroids good therapeutic options for patients with RA? Katz SJ, Russell AS NAT CLIN PRACT RHEUMATOL 2008 4 6 290-291
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979226 Are modified-release corticosteroids good therapeutic options for patients with RA? Katz SJ, Russell AS NAT CLIN PRACT RHEUMATOL 2008 4 6 290-291
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979227 Matrix metalloproteinase knockout studies and the potential use of matrix metalloproteinase inhibitors in the rheumatic diseases. Milner JM, Cawston TE CURR DRUG TARGETS-INFLAMM ALLERGY 2005 4 3 363-375
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979227 Matrix metalloproteinase knockout studies and the potential use of matrix metalloproteinase inhibitors in the rheumatic diseases. Milner JM, Cawston TE CURR DRUG TARGETS-INFLAMM ALLERGY 2005 4 3 363-375
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980023 Fostamatinib disodium (FosD, an oral inhibitor of Syk, is well-tolerated and has significant clinical activity in diffuse large B cell lymphoma (DLBCL) and chronic lymphocytic leukemia SLL/CLL, Friedberg JW, Sharman J, Schaefer-Cutillo J, Johnston PB, De Vos S, LaCasce A, Leonard JP, Cripe LD, Sinha R, Gregory SA, Sweetenham J et al BLOOD 2008 112 11 3-4
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980023 Fostamatinib disodium (FosD), an oral inhibitor of Syk, is well-tolerated and has significant clinical activity in diffuse large B cell lymphoma (DLBCL) and chronic lymphocytic leukemia (SLL/CLL). Friedberg JW, Sharman J, Schaefer-Cutillo J, Johnston PB, De Vos S, LaCasce A, Leonard JP, Cripe LD, Sinha R, Gregory SA, Sweetenham J et al BLOOD 2008 112 11 3-4
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990057 A novel human monoclonal antibody against IL-15 (HuMax-IL15) in patients with active rheumatoid arthritis RA, Results of a double-blind, placebo-controlled phase I/II trial. Baslund B, Tvede N, Danneskiold-Samsoe B, Petersen J, Petersen LJ, Schuurman J, van de Winkel J, Larsson P, Panayi G, McInnes IB AM COLL RHEUMATOL 2003 Abs 1706
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990057 A novel human monoclonal antibody against IL-15 (HuMax-IL15) in patients with active rheumatoid arthritis (RA): Results of a double-blind, placebo-controlled phase I/II trial. Baslund B, Tvede N, Danneskiold-Samsoe B, Petersen J, Petersen LJ, Schuurman J, van de Winkel J, Larsson P, Panayi G, McInnes IB AM COLL RHEUMATOL 2003 Abs 1706
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WO-2006078846 Prodrugs of 2,4-pyrimidinediamine compound, Useful for treating autoimmune diseases eg Hashimoto's thyroiditis and autoimmune hemolytic anemia. Singh R, Bhamidipati S, Masuda E WORLD PATENT Rigel Pharmaceuticals Inc 2008 May 29
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WO-2006078846 Prodrugs of 2,4-pyrimidinediamine compound - Useful for treating autoimmune diseases eg Hashimoto's thyroiditis and autoimmune hemolytic anemia. Singh R, Bhamidipati S, Masuda E WORLD PATENT Rigel Pharmaceuticals Inc 2008 May 29
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WO-2008064274 New disodium salt hydrates of a 2,4-pyrimidinediamine prodrug are Syk kinase inhibitors, Useful for the treatment of eg rheumatoid arthritis. Bhamidipati S, Singh R, Sun T, Masuda E WORLD PATENT Rigel Pharmaceuticals Inc 2006 July 27
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WO-2008064274 New disodium salt hydrates of a 2,4-pyrimidinediamine prodrug are Syk kinase inhibitors - Useful for the treatment of eg rheumatoid arthritis. Bhamidipati S, Singh R, Sun T, Masuda E WORLD PATENT Rigel Pharmaceuticals Inc 2006 July 27
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