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Review

Investigational Bruton’s tyrosine kinase inhibitors for the treatment of rheumatoid arthritis

Pages 891-899 | Received 16 Feb 2016, Accepted 21 Apr 2016, Published online: 09 May 2016

References

  • Rawlings DJ, Witte ON. The Btk subfamily of cytoplasmic tyrosine kinases: structure, regulation and function. Semin Immunol. 1995 Aug;7(4):237–246.
  • Mano H. The Tec family protein-tyrosine kinases: a subset of kinases for a subset of signalings. Int J Hematol. 1999 Jan;69(1):6–12.
  • Readinger JA, Mueller KL, Venegas AM, et al. Tec kinases regulate T-lymphocyte development and function: new insights into the roles of ITK and RLK/TXK. Immunol Rev. 2009 Mar;228(1):93–114.
  • Readinger JA, Mueller KL, Venegas AM, et al. Structures of human Bruton’s tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases. Immunol Rev. 2009;228(1):93–114.
  • Aalipour A, Advani RH. Bruton’s tyrosine kinase inhibitors and their clinical potential in the treatment of B-cell malignancies: focus on ibrutinib. Ther Adv Hematol. 2014 Aug;5(4):121–133.
  • Drake JM, Lee JK, Witte ON. Clinical targeting of mutated and wild-type protein tyrosine kinases in cancer. Mol Cell Biol. 2014 May;34(10):1722–1732.
  • Hussain A, Yu L, Faryal R, et al. TEC family kinases in health and disease–loss-of-function of BTK and ITK and the gain-of-function fusions ITK-SYK and BTK-SYK. Febs J. 2011 Jun;278(12):2001–2010.
  • Kutsch N, Marks R, Ratei R, et al. Role of tyrosine kinase inhibitors in indolent and other mature B-cell neoplasms. Biomark Insights. 2015 Aug 16;10(Suppl3):15–23.
  • Puri KD, Di Paolo JA, Gold MR. B-cell receptor signaling inhibitors for treatment of autoimmune inflammatory diseases and B-cell malignancies. Int Rev Immunol. 2013 Aug;32(4):397–427.
  • Whang JA, Chang BY. Bruton’s tyrosine kinase inhibitors for the treatment of rheumatoid arthritis. Drug Discov Today. 2014 Aug;19(8):1200–1204.
  • Kyttaris VC, Tsokos GC. Targeting lymphocyte signaling pathways as a therapeutic approach to systemic lupus erythematosus. Curr Opin Rheumatol. 2011 Sep;23(5):449–453.
  • Chen JS, Chang LC, Huang SJ, et al. Targeting spleen tyrosine kinase-Bruton’s tyrosine kinase axis for immunologically mediated glomerulonephritis. Biomed Res Int. 2014;2014:814869.
  • Nakou M, Katsikas G, Sidiropoulos P, et al. Rituximab therapy reduces activated B cells in both the peripheral blood and bone marrow of patients with rheumatoid arthritis: depletion of memory B cells correlates with clinical response. Arthritis Res Ther. 2009;11(4):R131.
  • Evans EK, Tester R, Aslanian S, et al. Inhibition of BTK with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013;346(2):219–228.
  • Shi Q, Tebben A, Dyckman AJ, et al. Purine derivatives as potent Bruton’s tyrosine kinase (BTK) inhibitors for autoimmune diseases. Bioorg Med Chem Lett. 2014 May 1;24(9):2206–2211.
  • Liu J, Guiadeen D, Krikorian A, et al. Discovery of 8-amino-imidazo[1,5-a]pyrazines as reversible BTK inhibitors for the treatment of rheumatoid arthritis. ACS Med Chem Lett. 2016;7(2):198–203. doi:10.1021/acsmedchemlett.5b00463.
  • Smith CR, Dougan DR, Komandla M, et al. Fragment-based discovery of a small molecule inhibitor of Bruton’s Tyrosine Kinase. J Med Chem 2015 Jul23;58(14):5437–5444.
  • Xu D, Kim Y, Postelnek J, et al. RN486, a selective Bruton’s tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012;341(1):90–103.
  • Young WB, Barbosa J, Blomgren P, et al. Discovery of highly potent and selective Bruton’s tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability. Bioorg Med Chem Lett. 2016 Jan 15;26(2):575–579.
  • Byrd JC, Harrington B, O’Brien S, et al. Acalabrutinib (ACP-196) in relapsed chronic lymphocytic leukemia. N Engl J Med. 2016;374:323–332.
  • Covey T, Barf T, Gulrajani M, et al. ACP-196: a novel covalent Bruton’s tyrosine kinase (Btk) inhibitor with improved selectivity and in vivo target coverage in chronic lymphocytic leukemia (CLL) patients. Cancer Res. 2015;75(15Suppl):Abstractnr 2596.
  • Parmar H, Immunology from symptom relief to disease modification, Merck Serono Investor and Analyst Day [ cited 2014 Sep 18]. Available from: http://www.merck.de/company.merck.de/de/images/6_Presentation_Immunology_tcm1613_128736.pdf?Version=.
  • Park JK, Park JA, Lee YJ, et al. THU0499 Hm71224, a novel oral BTK inhibitor, inhibits human immune cell activation: new drug candidate to treat B-cell associated autoimmune diseases. Ann Rheum Dis. 2014;73:355–356.
  • Yang SY, Kim YY, Song JY, et al. HM71224, A novel Btk inhibitor demonstrates potent activities in rodent models of arthritis. Ann Rheum Dis. 2014;73(Suppl2):518–519.
  • Kim YY, Park KT, Lee KH, et al. FRI0380 HM71224, A selective Bruton’s Tyrosine Kinase inhibitor, ameliorates murine lupus development. Ann Rheum Dis. 2015;74:564.
  • Lee J, Son J, Sin HJ, et al. THU0185 Safety, pharmacokinetics and proof-of-mechanism of an oral Bruton’s Tyrosine Kinase inhibitor HM71224 in healthy adult volunteers. Ann Rheum Dis. 2015;74:261.
  • Bradshaw JM, McFarland JM, Paavilainen VO, et al. Prolonged and tunable residence time using reversible covalent kinase inhibitors. Nat Chem Biol. 2015;11(7):525–531.
  • Hill RJ, Smith P, Krishnarajah J, et al. Discovery of PRN1008, a novel, reversible covalent BTK inhibitor in clinical development for rheumatoid arthritis [abstract]. Arthritis Rheumatol. 2015;67((suppl):10.
  • Smith PF, Krishnarajah J, Nunn PA, et al. SAT0232 A phase 1 clinical trial of PRN1008, an oral, reversible, covalent BTK inhibitor demonstrates clinical safety and therapeutic levels of BTK occupancy without sustained systemic exposure. Ann Rheum Dis. 2015;74:742.
  • Madakamutil L. Discovery of a small molecule inhibitor of Bruton’s Tyrosine Kinase (BTK) for autoimmune diseases. 3rd International Conference and Exhibition on Clinical & Cellular Immunology (Immunology Summit-2014); Sep 29–Oct 1 2014; Baltimore, MD. ( see http://www.omicsgroup.com/conferences/ACS/conference/pdfs/12834-Speaker-Pdf-T.pdf)
  • Hirst G, Fragment based drug discovery. Sweating the small stuff is worth it. 5th RSC-BMCS Fragment-Based Drug Discovery Meeting; March 22nd – 24th 2015; Cambridge, UK. ( see http://www.maggichurchouseevents.co.uk/bmcs/Downloads/Fragments%20-%20Tue%201415%20Hirst%20Gavin.pdf)
  • Yoshizawa T, Ariza Y, Ueda Y, et al. Development of a Bruton’s Tyrosine Kinase (Btk) inhibitor, ONO-4059: Efficacy in a Collagen Induced Arthritis (CIA) model indicates potential treatment for Rheumatoid Arthritis (RA). Arthritis Rheum. 2012;64(Suppl 10):1660.
  • Ariza Y, Yoshizawa T, Ueda Y, et al. ONO-4059 – A novel small molecule dual inhibitor of Bruton’s Tyrosine Kinase (Btk) and Tec kinase- suppresses osteoclastic bone resorption and inflammation. Arthritis Rheum. 2013;65(Suppl 10):1824.
  • Goess C, Graff C, Zhang TT, et al. Efficacy of abbv-105, a selective and irreversible inhibitor of Bruton’s Tyrosine Kinase (BTK), in multiple models of inflammation. Arthritis Rheumatol. 2015;67(suppl 10).
  • Hosoi F, Iguchi S, Yoshiga Y, et al. OP0075 TAS5315, A novel Bruton’s Tyrosine Kinase (BTK) inhibitor, demonstrates potent efficacy in mouse Collagen-Induced Arthritis Model. Ann Rheum Dis. 2015;74(Suppl2):97.
  • Morris S, Laurent A, Jerome L, et al. Pre-clinical development of a novel, potent and selective BTK inhibitor for autoimmune disease and inflammation including arthritis. Arthritis Rheumatol. 2015;67(suppl 10).
  • Chalmers S, Doerner J, Bosanac T, et al. Blockade of immune complex-mediated glomerulonephritis by highly selective inhibition of Bruton’s Tyrosine Kinase. Arthritis Rheumatol. 2015;67(suppl 10).
  • See Hardman & Co, RedX pharma, [2016 Jan 21]. Available from: http://www.hardmanandco.com/system/files/research_papers/Redx Pharma.pdf.
  • Walker V, Guisot NES, Best S, et al. Development of REDX05194, a novel, potent and selective inhibitor of Bruton’s Tyrosine Kinase (BTK) as a potential treatment for B-cell malignancies. Blood. 2015;126(23):4848.
  • Hoffman La Roche Inc, Ono Pharmaceutical Co., Combination therapy of an anti CD20 antibody with A BTK inhibitor. WO2015067586. 2015.
  • 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 U S A. 2010;107(29):13075–13080.
  • Shinohara M, Chang BY, Buggy JJ, et al. The orally available Btk inhibitor ibrutinib (PCI-32765) protects against osteoclast-mediated bone loss. Bone. 2014;60:8–15.
  • Young WB, Barbosa J, Blomgren P, et al. Potent and selective Bruton’s tyrosine kinase inhibitors: discovery of GDC-0834. Bioorg Med Chem Lett. 2015 Mar 15;25(6):1333–1337.
  • Liu L, Di Paolo J, Barbosa J, et al. Antiarthritis effect of a novel Bruton’s tyrosine kinase (BTK) inhibitor in rat CIA and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy. J Pharmacol Exp Ther. 2011;338(1):154–163.
  • Liu L, Halladay JS, Shin Y, et al. Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton’s tyrosine kinase inhibitor. Drug Metab Dispos. 2011;39(10):1840–1849.
  • Sodhi JK, Wong S, Kirkpatrick DS, et al. A novel reaction mediated by human aldehyde oxidase: amide hydrolysis of GDC-0834. Drug Metab Dispos. 2015 Jun;43(6):908–915.
  • Lou Y, Han X, Kuglstatter A, et al. Structure-based drug design of RN486, a potent and selective Bruton’s tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis. J Med Chem 2015 Jan8;58(1):512–516.
  • Mina-Osorio P, Lastant J, Keirstead N, et al. Suppression of glomerulonephritis in lupus prone NZB/W mice by RN486, a selective inhibitor of Bruton’s Tyrosine Kinase. Arthritis Rheum. 2013 Sep;65(9):2380–2391.
  • Lou Y, Sweeney ZK, Kuglstatter A, et al. Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton’s Tyrosine Kinase (BTK) inhibitor scaffold. Bioorg Med Chem Lett. 2015 Jan 15;25(2):367–371.
  • 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(1):41–50.
  • Cohen S, Fleischmann R. Kinase inhibitors: a new approach to rheumatoid arthritis treatment. Curr Opin Rheumatol. 2010 May;22(3):330–335.
  • Kyttaris VC. Kinase inhibitors: a new class of antirheumatic drugs. Drug Des Devel Ther. 2012;6:245–250.
  • Chiron D, Di Liberto M, Martin P, et al. Cell-cycle reprogramming for PI3K inhibition overrides a relapse-specific C481S BTK mutation revealed by longitudinal functional genomics in mantle cell lymphoma. Cancer Discov. 2014;4:1022–1035.
  • Cohen SB, Cheng -T-T, 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. 2009;60(2):335–344.

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