Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765)

References

• Satterthwaite AB, Witte ON. The role of Bruton's tyrosine kinase in B-cell development and function: a genetic perspective. Immunol Rev 2000;175:120–127.
   PubMed Web of Science ®Google Scholar
• Spaargaren M, Beuling EA, Rurup ML, et al. The B cell antigen receptor controls integrin activity through Btk and PLCgamma2. J Exp Med 2003;198:1539–1550.
   PubMed Web of Science ®Google Scholar
• Ortolano S, Hwang IY, Han SB, et al. Roles for phosphoinositide 3-kinases, Bruton's tyrosine kinase, and Jun kinases in B lymphocyte chemotaxis and homing. Eur J Immunol 2006;36:1285–1295.
   PubMed Web of Science ®Google Scholar
• de Gorter DJ, Beuling EA, Kersseboom R, et al. Bruton's tyrosine kinase and phospholipase Cgamma2 mediate chemokine-controlled B cell migration and homing. Immunity 2007;26:93–104.
   PubMed Web of Science ®Google Scholar
• Genevier HC, Hinshelwood S, Gaspar HB, et al. Expression of Bruton's tyrosine kinase protein within the B cell lineage. Eur J Immunol 1994;24:3100–3105.
   PubMed Web of Science ®Google Scholar
• Rawlings DJ, Saffran DC, Tsukada S, et al. Mutation of unique region of Bruton's tyrosine kinase in immunodeficient XID mice. Science 1993;261:358–361.
   PubMed Web of Science ®Google Scholar
• Vetrie D, Vorechovsky I, Sideras P, et al. The gene involved in X-linked agammaglobulinaemia is a member of the src family of protein-tyrosine kinases. Nature 1993;361:226–233.
   PubMed Web of Science ®Google Scholar
• Tsukada S, Saffran DC, Rawlings DJ, et al. Deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agamma-globulinemia. Cell 1993;72:279–290.
   PubMed Web of Science ®Google Scholar
• Conley ME, Dobbs AK, Farmer DM, et al. Primary B cell immunodeficiencies: comparisons and contrasts. Annu Rev Immunol 2009;27:199–227.
   PubMed Web of Science ®Google Scholar
• Honigberg LA, Smith AM, Sirisawad M, et al. 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.
   PubMed Web of Science ®Google Scholar
• Chang BY, Huang MM, Francesco M, et al. The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther 2011;13:R115.
   PubMed Web of Science ®Google Scholar
• Di Paolo JA, Huang T, Balazs M, et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat Chem Biol 2011;7:41–50.
   PubMed Web of Science ®Google Scholar
• Herman SE, Gordon AL, Hertlein E, et al. Bruton's tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood 2011;117:6287–6296.
   PubMed Web of Science ®Google Scholar
• Ponader S, Chen SS, Buggy JJ, et al. The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo. Blood 2012;119:1182–1189.
   PubMed Web of Science ®Google Scholar
• Advani RH, Buggy JJ, Sharman JP, et al. Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. J Clin Oncol 2013;31:88–94.
   PubMed Web of Science ®Google Scholar
• Gauld SB, Dal Porto JM, Cambier JC. B cell antigen receptor signaling: roles in cell development and disease. Science 2002;296: 1641–1642.
   PubMed Web of Science ®Google Scholar
• Kuppers R. Mechanisms of B-cell lymphoma pathogenesis. Nat Rev Cancer 2005;5:251–262.
   PubMed Web of Science ®Google Scholar
• Burger JA. Nurture versus nature: the microenvironment in chronic lymphocytic leukemia. Hematology Am Soc Hematol Educ Program 2011:96–103.
   PubMed Web of Science ®Google Scholar
• Stevenson FK, Krysov S, Davies AJ, et al. B-cell receptor signaling in chronic lymphocytic leukemia. Blood 2011;118:4313–4320.
   PubMed Web of Science ®Google Scholar
• Woyach JA, Johnson AJ, Byrd JC. The B-cell receptor signaling pathway as a therapeutic target in CLL. Blood 2012;120:1175–1184.
   PubMed Web of Science ®Google Scholar
• Davis RE, Ngo VN, Lenz G, et al. Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma. Nature 2010;463:88–92.
   PubMed Web of Science ®Google Scholar
• Chiorazzi N, Rai KR, Ferrarini M. Chronic lymphocytic leukemia. N Engl J Med 2005;352:804–815.
   PubMed Web of Science ®Google Scholar
• Duhren-von Minden M, Ubelhart R, Schneider D, et al. Chronic lymphocytic leukaemia is driven by antigen-independent cell-autonomous signalling. Nature 2012;489:309–312.
   PubMed Web of Science ®Google Scholar
• Chiorazzi N, Efremov DG. Chronic lymphocytic leukemia: a tale of one or two signals?. Cell Res 2013;23:182–185.
   PubMed Web of Science ®Google Scholar
• Hoogeboom R, van Kessel KP, Hochstenbach F, et al. A mutated B cell chronic lymphocytic leukemia subset that recognizes and responds to fungi. J Exp Med 2013;210:59–70.
   PubMed Web of Science ®Google Scholar
• Binder M, Lechenne B, Ummanni R, et al. Stereotypical chronic lymphocytic leukemia B-cell receptors recognize survival promoting antigens on stromal cells. PLoS One 2010;5:e15992.
   PubMed Web of Science ®Google Scholar
• Chu CC, Catera R, Hatzi K, et al. Chronic lymphocytic leukemia antibodies with a common stereotypic rearrangement recognize nonmuscle myosin heavy chain IIA. Blood 2008;112:5122–5129.
   PubMed Web of Science ®Google Scholar
• Kostareli E, Gounari M, Janus A, et al. Antigen receptor stereotypy across B-cell lymphoproliferations: the case of IGHV4–59/IGKV3–20 receptors with rheumatoid factor activity. Leukemia 2012;26:1127–1131.
   PubMed Web of Science ®Google Scholar
• Hoogeboom R, Wormhoudt TA, Schipperus MR, et al. A novel chronic lymphocytic leukemia subset expressing mutated IGHV3–7-encoded rheumatoid factor B-cell receptors that are functionally proficient. Leukemia 2012 Aug 20. [Epub ahead of print]
   PubMed Web of Science ®Google Scholar
• Herishanu Y, Perez-Galan P, Liu D, et al. The lymph node microenvironment promotes B-cell receptor signaling, NF-kappaB activation, and tumor proliferation in chronic lymphocytic leukemia. Blood 2011;117:563–574.
   PubMed Web of Science ®Google Scholar
• Reth M. Antigen receptors on B lymphocytes. Annu Rev Immunol 1992;10:97–121.
   PubMed Web of Science ®Google Scholar
• Liu W, Meckel T, Tolar P, et al. Intrinsic properties of immuno-globulin IgG1 isotype-switched B cell receptors promote micro-clustering and the initiation of signaling. Immunity 2010;32:778–789.
   PubMed Web of Science ®Google Scholar
• Bernal A, Pastore RD, Asgary Z, et al. Survival of leukemic B cells promoted by engagement of the antigen receptor. Blood 2001;98: 3050–3057.
   PubMed Web of Science ®Google Scholar
• Longo PG, Laurenti L, Gobessi S, et al. The Akt/Mcl-1 pathway plays a prominent role in mediating antiapoptotic signals downstream of the B-cell receptor in chronic lymphocytic leukemia B cells. Blood 2008;111:846–855.
   PubMed Web of Science ®Google Scholar
• 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 2010;115:2578–2585.
   PubMed Web of Science ®Google Scholar
• Dar AC, Shokat KM. The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling. Annu Rev Biochem 2011;80:769–795.
   PubMed Web of Science ®Google Scholar
• Singh J, Petter RC, Kluge AF. Targeted covalent drugs of the kinase family. Curr Opin Chem Biol 2010;14:475–480.
   PubMed Web of Science ®Google Scholar
• Pan Z, Scheerens H, Li SJ, et al. Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. ChemMedChem 2007;2: 58–61.
   PubMed Web of Science ®Google Scholar
• de Rooij MF, Kuil A, Geest CR, et al. The clinically active BTK inhibitor PCI-32765 targets B-cell receptor- and chemokine-controlled adhesion and migration in chronic lymphocytic leukemia. Blood 2012;119:2590–2594.
   PubMed Web of Science ®Google Scholar
• Schwamb J, Feldhaus V, Baumann M, et al. B-cell receptor triggers drug sensitivity of primary CLL cells by controlling glucosylation of ceramides. Blood 2012;120:3978–3985.
   PubMed Web of Science ®Google Scholar
• Yang Y, Shaffer AL 3rd, Emre NC, et al. Exploiting synthetic lethality for the therapy of ABC diffuse large B cell lymphoma. Cancer Cell 2012;21:723–737.
   PubMed Web of Science ®Google Scholar
• Tai YT, Chang BY, Kong SY, et al. Bruton tyrosine kinase inhibition is a novel therapeutic strategy targeting tumor in the bone marrow microenvironment in multiple myeloma. Blood 2012;120:1877–1887.
   PubMed Web of Science ®Google Scholar
• Burger JA, Montserrat E. Coming full circle: 70 years of chronic lymphocytic leukemia cell redistribution, from glucocorticoids to inhibitors of B cell receptor signaling. Blood 2013;121:1501–1509.
   PubMed Web of Science ®Google Scholar
• Cheson BD, Byrd JC, Rai KR, et al. Novel targeted agents and the need to refine clinical end points in chronic lymphocytic leukemia. J Clin Oncol 2012;30:2820–2822.
   PubMed Web of Science ®Google Scholar
• Hoellenriegel J, Meadows SA, Sivina M, et al. The phosphoinositide 3’-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood 2011;118:3603–3612.
   PubMed Web of Science ®Google Scholar
• Byrd JC, Furman RR, Coutre SE, et al. The Bruton's tyrosine kinase (BTK) inhibitor ibrutinib (PCI-32765) promotes high response rate, durable remissions, and is tolerable in treatment naïve (TN) and relapsed or refractory (RR) chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) patients including patients with high-risk (HR) disease: new and updated results of 116 patients in a phase Ib/II study. Blood 2012;120(Suppl. 1): Abstract 189.
   Google Scholar
• Wang M, Rule SA, Martin P, et al. Interim Results of an international, multicenter, phase 2 study of Bruton's tyrosine kinase (BTK) inhibitor, ibrutinib (PCI-32765), in relapsed or refractory mantle cell lymphoma (MCL): durable efficacy and tolerability with longer follow-up. Blood 2012;120(Suppl. 1): Abstract 904.
   Google Scholar
• Kubo T, Uchida Y, Watanabe Y, et al. Augmented TLR9-induced Btk activation in PIR-B-deficient B-1 cells provokes excessive autoantibody production and autoimmunity. J Exp Med 2009;206:1971–1982.
   PubMed Web of Science ®Google Scholar
• Kil LP, de Bruijn MJ, van Nimwegen M, et al. Btk levels set the threshold for B-cell activation and negative selection of autoreactive B cells in mice. Blood 2012;119:3744–3756.
   PubMed Web of Science ®Google Scholar
• Hutcheson J, Vanarsa K, Bashmakov A, et al. Modulating proximal cell signaling by targeting Btk ameliorates humoral autoimmunity and end-organ disease in murine lupus. Arthritis Res Ther 2012;14:R243.
   PubMed Web of Science ®Google Scholar
• Shinohara M, Koga T, Okamoto K, et al. Tyrosine kinases Btk and Tec regulate osteoclast differentiation by linking RANK and ITAM signals. Cell 2008;132:794–806.
   PubMed Web of Science ®Google Scholar
• Farooqui M, Lozier JN, Valdez J, et al. Ibrutinib (PCI 32765) rapidly improves platelet counts in chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) patients and has minimal effects on platelet aggregation. Blood 2012;120(Suppl. 1): Abstract 1789.
   Google Scholar
• Burger JA, Keating MJ, Wierda WG, et al. The Btk inhibitor ibrutinib (PCI-32765) in combination with rituximab is well tolerated and displays profound activity in high-risk chronic lymphocytic leukemia (CLL) patients. Blood 2012;120 (Suppl. 1): Abstract 187.
   Google Scholar
• Liu J, Fitzgerald ME, Berndt MC, et al. Bruton tyrosine kinase is essential for botrocetin/VWF-induced signaling and GPIb-dependent thrombus formation in vivo. Blood 2006;108:2596–2603.
   PubMed Web of Science ®Google Scholar
• Quek LS, Bolen J, Watson SP. A role for Bruton's tyrosine kinase (Btk) in platelet activation by collagen. Curr Biol 1998;8:1137–1140.
   PubMed Web of Science ®Google Scholar
• Jackson SP, Cranmer S, Mangin P, et al. Are Erk, Btk, and PECAM-1 major players in GPIb signaling?. The challenge of unraveling signaling events downstream of platelet GPIb. Blood 2007;109:846–847; discussion 847–848.
   Google Scholar