The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells

Arthritis Research and Therapy

Volumn 13, Issue 4, 2011, Pages

  Chang, Betty Y ^a   Huang, Min M ^a   Francesco, Michelle ^a   Chen, Jun ^a   Sokolove, Jeremy ^b,c   Magadala, Padmaja ^a   Robinson, William H ^b,c   Buggy, Joseph J ^a  

^a PHARMACYCLICS INC   (United States)

^b STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c VA PALO ALTO HEALTH CARE SYSTEM   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIRHEUMATIC AGENT; B LYMPHOCYTE ANTIGEN; B LYMPHOCYTE RECEPTOR; BRUTON TYROSINE KINASE; CHEMOKINE; COLLAGEN ANTIBODY; CREMEPHOR; CYTOKINE; DEXAMETHASONE; HISTAMINE; INTERLEUKIN 1BETA; INTERLEUKIN 6; INTERLEUKIN 8; PCI 32765; PROSTAGLANDIN; PROTEIN TYROSINE KINASE INHIBITOR; SALBUTAMOL; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; AGAMMAGLOBULINAEMIA TYROSINE KINASE; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; PYRAZOLE DERIVATIVE; PYRIMIDINE DERIVATIVE;

ANAPHYLAXIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; ARTICULAR CARTILAGE; B LYMPHOCYTE; CALCIUM MOBILIZATION; CELL ASSAY; CELL PROLIFERATION; CONTROLLED STUDY; DRUG DOSE; EFFECTOR CELL; FEMALE; IMMUNE COMPLEX DISEASE; IMMUNOCOMPETENT CELL; IN VITRO STUDY; MACROPHAGE; MALE; MAST CELL DEGRANULATION; MONOCYTE; MOUSE; NONHUMAN; PASSIVE SKIN ANAPHYLAXIS; PATHOGENESIS; RANDOMIZED CONTROLLED TRIAL; RHEUMATOID ARTHRITIS; SYNOVIUM; ANIMAL; ARTHRITIS; BAGG ALBINO MOUSE; DRUG ANTAGONISM; DRUG EFFECT; HUMAN; IMMUNOLOGY; MAST CELL; PATHOLOGY;

ANIMALS; ARTHRITIS, EXPERIMENTAL; ARTHRITIS, RHEUMATOID; B-LYMPHOCYTES; CELL PROLIFERATION; FEMALE; HUMANS; IMMUNE COMPLEX DISEASES; MACROPHAGES; MAST CELLS; MICE; MICE, INBRED BALB C; MONOCYTES; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRAZOLES; PYRIMIDINES;

EID: 79960133279     PISSN: 14786354     EISSN: 14786362     Source Type: Journal    
DOI: 10.1186/ar3400     Document Type: Article

References (49)

1. Lindstrom TM, Robinson WH. A multitude of kinases - which are the best targets in treating rheumatoid arthritis?. Rheum Dis Clin North Am 2010, 36:367-383. 10.1016/j.rdc.2010.02.005, 2879404, 20510239.
2. D'Aura Swanson C, Paniagua RT, Lindstrom TM, Robinson WH. Tyrosine kinases as targets for the treatment of rheumatoid arthritis. Nat Rev Rheumatol 2009, 5:317-324. 10.1038/nrrheum.2009.82, 19491913.
3. Firestein GS. Evolving concepts of rheumatoid arthritis. Nature 2003, 423:356-361. 10.1038/nature01661, 12748655.
4. Khan WN. Regulation of B lymphocyte development and activation by Bruton's tyrosine kinase. Immunol Res 2001, 23:147-156. 10.1385/IR:23:2-3:147, 11444380.
5. Conley ME, Dobbs AK, Farmer DM, Kilic S, Paris K, Grigoriadou S, Coustan-Smith E, Howard V, Campana D. Primary B cell immunodeficiencies: comparisons and contrasts. Annu Rev Immunol 2009, 27:199-227. 10.1146/annurev.immunol.021908.132649, 19302039.
6. Tsukada S, Saffran DC, Rawlings DJ, Parolini O, Allen RC, Klisak I, Sparkes RS, Kubagawa H, Mohandas T, Quan S, et al. Deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia. Cell 1993, 72:279-290. 10.1016/0092-8674(93)90667-F, 8425221.
7. Khan WN, Alt FW, Gerstein RM, Malynn BA, Larsson I, Rathbun G, Davidson L, Müller S, Kantor AB, Herzenberg LA. Defective B cell development and function in Btk-deficient mice. Immunity 1995, 3:283-299. 10.1016/1074-7613(95)90114-0, 7552994.
8. Rawlings DJ, Saffran DC, Tsukada S, Largaespada DA, Grimaldi JC, Cohen L, Mohr RN, Bazan JF, Howard M, Copeland NG, et al. Mutation of unique region of Bruton's tyrosine kinase in immunodeficient XID mice. Science 1993, 261:358-361. 10.1126/science.8332901, 8332901.
9. Jongstra-Bilen J, Puig Cano A, Hasija M, Xiao H, Smith CI, Cybulsky MI. Dual functions of Bruton's tyrosine kinase and Tec kinase during Fcgamma receptor-induced signaling and phagocytosis. J Immunol 2008, 181:288-298.
10. Wang XS, Lau HY. Histamine release from human buffy coat-derived mast cells. Int Immunopharmacol 2007, 7:541-546. 10.1016/j.intimp.2006.11.005, 17321478.
11. Hata D, Kawakami Y, Inagaki N, Lantz CS, Kitamura T, Khan WN, Maeda-Yamamoto M, Miura T, Han W, Hartman SE, Yao L, Nagai H, Goldfeld AE, Alt FW, Galli SJ, Witte ON, Kawakami T. Involvement of Bruton's tyrosine kinase in FcepsilonRI-dependent mast cell degranulation and cytokine production. J Exp Med 1998, 187:1235-1247. 10.1084/jem.187.8.1235, 2212237, 9547335.
12. Mukhopadhyay S, Mohanty M, Mangla A, George A, Bal V, Rath S, Ravindran B. Macrophage effector functions controlled by Bruton's tyrosine kinase are more crucial than the cytokine balance of T cell responses for microfilarial clearance. J Immunol 2002, 168:2914-2921.
13. Mangla A, Khare A, Vineeth V, Panday NN, Mukhopadhyay A, Ravindran B, Bal V, George A, Rath S. Pleiotropic consequences of Bruton tyrosine kinase deficiency in myeloid lineages lead to poor inflammatory responses. Blood 2004, 104:1191-1197. 10.1182/blood-2004-01-0207, 15117762.
14. Horwood NJ, Mahon T, McDaid JP, Campbell J, Mano H, Brennan FM, Webster D, Foxwell BM. Bruton's tyrosine kinase is required for lipopolysaccharide-induced tumor necrosis factor alpha production. J Exp Med 2003, 197:1603-1611. 10.1084/jem.20021845, 2193950, 12810683.
15. Jansson L, Holmdahl R. Genes on the X chromosome affect development of collagen-induced arthritis in mice. Clin Exp Immunol 1993, 94:459-465. 1534441, 8252807.
16. Taurog JD, Moutsopoulos HM, Rosenberg YJ, Chused TM, Steinberg AD. CBA/N X-linked B-cell defect prevents NZB B-cell hyperactivity in F1 mice. J Exp Med 1979, 150:31-43. 10.1084/jem.150.1.31, 2185603, 312908.
17. Scribner CL, Hansen CT, Klinman DM, Steinberg AD. The interaction of the xid and me genes. J Immunol 1987, 138:3611-3617.
18. Satterthwaite AB, Li Z, Witte ON. Btk function in B cell development and response. Semin Immunol 1998, 10:309-316. 10.1006/smim.1998.0123, 9695187.
19. Honigberg LA, Smith AM, Sirisawad M, Verner E, Loury D, Chang B, Li S, Pan Z, Thamm DH, Miller RA, Buggy JJ. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci USA 2010, 107:13075-13080. 10.1073/pnas.1004594107, 2919935, 20615965.
20. Fowler N, Sharman JF, Smith SS, Boyd T, Grant B, Kolibaba KS, Furman RR, Buggy J, Loury D, Hamdy A, Advani R. The Btk inhibitor, PCI-32765, induces durable responses with minimal toxicity in patients with relapsed/refractory B-cell malignancies: results from a phase I study. American Society of Hematology Annual Conference: 19 November, 2010 2010, Orlando, FL. Blood, Abstract 964.
21. Reeder CB, Ansell SM. Novel therapeutic agents for B-cell lymphoma: developing rational combinations. Blood 2011, 117:1453-1462. 10.1182/blood-2010-06-255067, 20978267.
22. Terato K, Hasty KA, Reife RA, Cremer MA, Kang AH, Stuart JM. Induction of arthritis with monoclonal antibodies to collagen. J Immunol 1992, 148:2103-2108.
23. Lappalainen J, Lindstedt KA, Kovanen PT. A protocol for generating high numbers of mature and functional human mast cells from peripheral blood. Clin Exp Allergy 2007, 37:1404-1414. 10.1111/j.1365-2222.2007.02778.x, 17845422.
24. Woolhiser MR, Brockow K, Metcalfe DD. Activation of human mast cells by aggregated IgG through FcgammaRI: additive effects of C3a. Clin Immunol 2004, 110:172-180. 10.1016/j.clim.2003.11.007, 15003814.
25. Irish JM, Czerwinski DK, Nolan GP, Levy R. Altered B-cell receptor signaling kinetics distinguish human follicular lymphoma B cells from tumor-infiltrating nonmalignant B cells. Blood 2006, 108:3135-3142. 10.1182/blood-2006-02-003921, 1895530, 16835385.
26. Munn DH, Cheung NK. Antibody-dependent antitumor cytotoxicity by human monocytes cultured with recombinant macrophage colony-stimulating factor. Induction of efficient antibody-mediated antitumor cytotoxicity not detected by isotope release assays. J Exp Med 1989, 170:511-526. 10.1084/jem.170.2.511, 2189400, 2526848.
27. 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. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther 2006, 319:998-1008. 10.1124/jpet.106.109058, 16946104.
28. Sokolove J, Zhao X, Chandra PE, Robinson WH. Immune complexes containing citrullinated fibrinogen co-stimulate macrophages via toll-like receptor 4 and Fcgamma receptor. Arthritis Rheum 2011, 63(1):53-62.
29. Silva MD, Savinainen A, Kapadia R, Ruan J, Siebert E, Avitahl N, Mosher R, Anderson K, Jaffee B, Schopf L, Chandra S. Quantitative analysis of micro-CT imaging and histopathological signatures of experimental arthritis in rats. Mol Imaging 2004, 3:312-318. 10.1162/1535350042973562, 15802047.
30. Mankin HJ, Dorfman H, Lippiello L, Zarins A. Biochemical and metabolic abnormalities in articular cartilage from osteo-arthritic human hips. II. Correlation of morphology with biochemical and metabolic data. J Bone Joint Surg Am 1971, 53:523-537.
31. Pine PR, Chang B, Schoettler N, Banquerigo ML, Wang S, Lau A, Zhao F, Grossbard EB, Payan DG, Brahn E. Inflammation and bone erosion are suppressed in models of rheumatoid arthritis following treatment with a novel Syk inhibitor. Clin Immunol 2007, 124:244-257. 10.1016/j.clim.2007.03.543, 17537677.
32. Drexler SK, Kong PL, Wales J, Foxwell BM. Cell signalling in macrophages, the principal innate immune effector cells of rheumatoid arthritis. Arthritis Research & Therapy 2008, 10:216. 10.1186/ar2481, 3154440, 21853121.
33. Fluckiger AC, Li Z, Kato RM, Wahl MI, Ochs HD, Longnecker R, Kinet JP, Witte ON, Scharenberg AM, Rawlings DJ. Btk/Tec kinases regulate sustained increases in intracellular Ca2+ following B-cell receptor activation. EMBO J 1998, 17:1973-1985. 10.1093/emboj/17.7.1973, 1170543, 9524120.
34. Kurosaki T, Kurosaki M. Transphosphorylation of Bruton's tyrosine kinase on tyrosine 551 is critical for B cell antigen receptor function. J Biol Chem 1997, 272:15595-15598. 10.1074/jbc.272.25.15595, 9188445.
35. Wang D, Feng J, Wen R, Marine JC, Sangster MY, Parganas E, Hoffmeyer A, Jackson CW, Cleveland JL, Murray PJ, Ihle JN. Phospholipase Cgamma2 is essential in the functions of B cell and several Fc receptors. Immunity 2000, 13:25-35. 10.1016/S1074-7613(00)00005-4, 10933392.
36. Nimmerjahn F, Ravetch JV. Fcγ receptors as regulators of immune responses. Nature Reviews Immunology 2008, 8:34-47. 10.1038/nri2206, 18064051.
37. Perezdediego R, Lopezgranados E, Pozo M, Rodriguez C, Sabina P, Ferreira A, Fontan G, Garciarodriguez M, Alemany S. Bruton's tyrosine kinase is not essential for LPS-induced activation of human monocytes. J Allergy Clin Immunol 2006, 117:1462-1469. 10.1016/j.jaci.2006.01.037, 16751014.
38. Galli SJ, Kalesnikoff J, Grimbaldeston MA, Piliponsky AM, Williams CM, Tsai M. Mast cells as "tunable" effector and immunoregulatory cells: recent advances. Annu Rev Immunol 2005, 23:749-786. 10.1146/annurev.immunol.21.120601.141025, 15771585.
39. Takai T. Roles of Fc receptors in autoimmunity. Nat Rev Immunol 2002, 2:(8):580-592.
40. Kerner JD, Appleby MW, Mohr RN, Chien S, Rawlings DJ, Maliszewski CR, Witte ON, Perlmutter RM. Impaired expansion of mouse B cell progenitors lacking Btk. Immunity 1995, 3:301-312. 10.1016/1074-7613(95)90115-9, 7552995.
41. Satterthwaite AB, Willis F, Kanchanastit P, Fruman D, Cantley LC, Helgason CD, Humphries RK, Lowell CA, Simon M, Leitges M, Tarakhovsky A, Tedder TF, Lesche R, Wu H, Witte ON. A sensitized genetic system for the analysis of murine B lymphocyte signal transduction pathways dependent on Bruton's tyrosine kinase. Proc Natl Acad Sci USA 2000, 97:6687-6692. 10.1073/pnas.110146697, 18703, 10829070.
42. Amoras AL, Kanegane H, Miyawaki T, Vilela MM. Defective Fc-, CR1- and CR3-mediated monocyte phagocytosis and chemotaxis in common variable immunodeficiency and X-linked agammaglobulinemia patients. J Investig Allergol Clin Immunol 2003, 13:181-188.
43. Ji H, Ohmura K, Mahmood U, Lee DM, Hofhuis FM, Boackle SA, Takahashi K, Holers VM, Walport M, Gerard C, Ezekowitz A, Carroll MC, Brenner M, Weissleder R, Verbeek JS, Duchatelle V, Degott C, Benoist C, Mathis D. Arthritis critically dependent on innate immune system players. Immunity 2002, 16:157-168. 10.1016/S1074-7613(02)00275-3, 11869678.
44. Firestein GS, Corr M. Common mechanisms in immune-mediated inflammatory disease. J Rheumatol Suppl 2005, 73:8-13; discussion 29-30.
45. Kagari T, Tanaka D, Doi H, Shimozato T. Essential role of Fc gamma receptors in anti-type II collagen antibody-induced arthritis. J Immunol 2003, 170:4318-4324.
46. Szalai AJ, Digerness SB, Agrawal A, Kearney JF, Bucy RP, Niwas S, Kilpatrick JM, Babu YS, Volanakis JE. The Arthus reaction in rodents: species-specific requirement of complement. J Immunol 2000, 164:463-468.
47. Ravetch JV. Fundamental Immunology. 2003, 690-700. Paul WE, Lippincott Williams and Wilkins, 5.
48. Shinohara M, Koga T, Okamoto K, Sakaguchi S, Arai K, Yasuda H, Takai T, Kodama T, Morio T, Geha RS, Kitamura D, Kurosaki T, Ellmeier W, Takayanagi H. Tyrosine kinases Btk and Tec regulate osteoclast differentiation by linking RANK and ITAM signals. Cell 2008, 132:794-806. 10.1016/j.cell.2007.12.037, 18329366.
49. Wong BR, Grossbard EB, Payan DG, Masuda ES. Targeting Syk as a treatment for allergic and autoimmune disorders. Expert Opin Investig Drugs 2004, 13:743-762. 10.1517/13543784.13.7.743, 15212616.