Are tyrosine kinase inhibitors promising for the treatment of systemic sclerosis and other fibrotic diseases?

Swiss Medical Weekly

Volumn 140, Issue SEPTEMBER, 2010, Pages

  Beyer, Christian ^a   Distler, Jor̈g H W ^a   Distler, Oliver ^b  

^a UNIVERSITY OF ERLANGEN NUREMBERG   (Germany)

^b UNIVERSITY HOSPITAL ZURICH   (Switzerland)

Author keywords

Fibrosis; Systemic sclerosis; Tyrosine kinase inhibitors

Indexed keywords

2,3 DIHYDRO 2 OXO 3 (4,5,6,7 TETRAHYDRO 1H INDOL 2 YLMETHYLENE) 1H INDOLE 5 SULFONIC ACID DIMETHYLAMIDE; ABELSON KINASE; BCR ABL PROTEIN; CANERTINIB; CORTICOSTEROID; DASATINIB; ERLOTINIB; GEFITINIB; IMATINIB; LAPATINIB; MATRIX METALLOPROTEINASE; METHOTREXATE; NILOTINIB; PLATELET DERIVED GROWTH FACTOR; PLATELET DERIVED GROWTH FACTOR RECEPTOR; SCLEROPROTEIN; SORAFENIB; SUNITINIB; THROMBOSPONDIN 1; TISSUE INHIBITOR OF METALLOPROTEINASE; VASCULOTROPIN; VATALANIB;

ANGIOGENESIS; ATYPICAL CHRONIC MYELOID LEUKEMIA; BONE MARROW TOXICITY; CELL PROLIFERATION; CHRONIC GRAFT VERSUS HOST DISEASE; CHRONIC MYELOID LEUKEMIA; CONGESTIVE HEART FAILURE; DIARRHEA; DRUG EFFICACY; DRUG TOLERABILITY; EDEMA; EXPERIMENTAL MODEL; FIBROBLAST; FIBROSIS; GASTROINTESTINAL STROMAL TUMOR; HEMANGIOMA; HUMAN; HYPOXIA; INTRACELLULAR SIGNALING; KIDNEY FIBROSIS; LIVER FIBROSIS; LUNG FIBROSIS; MOUSE; MUSCLE CRAMP; MYELOFIBROSIS; NONHUMAN; PROTEIN BLOOD LEVEL; REVIEW; SKIN DEFECT; SKIN FIBROSIS; SYSTEMIC SCLEROSIS; ULCER; WOUND HEALING;

EID: 79958834107     PISSN: 14247860     EISSN: None     Source Type: Journal    
DOI: 10.4414/smw.2010.13050     Document Type: Review

References (46)

1. Beyer C, Abraham D, Distler JH, Distler O. The pathogenesis of systemic sclerosis. In: Scleroderma - modern aspects of pathogenesis, diagnosis and therapy. Edited by Distler O. Bremen: UNI-MED Verlag AG; 2009: 23-32.
2. Arora A, Scholar EM. Role of tyrosine kinase inhibitors in cancer therapy. J Pharmacol Exp Ther. 2005;315(3):971-9. (Pubitemid 41635382)
3. Ciardiello F, Tortora G: EGFR antagonists in cancer treatment. N Engl J Med. 2008;358(11):1160-74.
4. Distler JH, Distler O. Intracellular tyrosine kinases as novel targets for anti-fibrotic therapy in systemic sclerosis. Rheumatology. (Oxford) 2008;47(Suppl 5):v10-11.
5. Hassoun PM, Mouthon L, Barbera JA, Eddahibi S, Flores SC, Grimminger F, et al. Inflammation, growth factors, and pulmonary vascular remodeling. J Am Coll Cardiol. 2009;54(1 Suppl):S10-19.
6. Daniels CE, Wilkes MC, Edens M, Kottom TJ, Murphy SJ, Limper AH, et al. Imatinib mesylate inhibits the profibrogenic activity of TGF-beta and prevents bleomycin-mediated lung fibrosis. J Clin Invest. 2004;114(9):1308-16. (Pubitemid 40385302)
7. Chen Y, Leask A, Abraham DJ, Pala D, Shiwen X, Khan K, et al. Heparan sulfate-dependent ERK activation contributes to the overexpression of fibrotic proteins and enhanced contraction by scleroderma fibroblasts. Arthritis Rheum. 2008;58(2):577-85. (Pubitemid 351294894)
8. Akhmetshina A, Dees C, Pileckyte M, Maurer B, Axmann R, Jungel A. et al. Dual inhibition of c-abl and PDGF receptor signaling by dasatinib and nilotinib for the treatment of dermal fibrosis. Faseb J. 2008;22(7):2214-22. (Pubitemid 351948641)
9. Distler JH, Jungel A, Huber LC, Schulze-Horsel U, Zwerina J, Gay RE, et al. Imatinib mesylate reduces production of extracellular matrix and prevents development of experimental dermal fibrosis. Arthritis Rheum. 2007;56(1):311-22. (Pubitemid 46106205)
10. Akhmetshina A, Venalis P, Dees C, Busch N, Zwerina J, Schett G, et al. Treatment with imatinib prevents fibrosis in different preclinical models of systemic sclerosis and induces regression of established fibrosis. Arthritis Rheum. 2009;60(1):219-24.
11. Abdollahi A, Li M, Ping G, Plathow C, Domhan S, Kiessling F, et al. Inhibition of platelet-derived growth factor signaling attenuates pulmonary fibrosis. J Exp Med. 2005;201(6):925-35. (Pubitemid 40524462)
12. Wang S, Wilkes MC, Leof EB, Hirschberg R. Imatinib mesylate blocks a non-Smad TGF-beta pathway and reduces renal fibrogenesis in vivo. Faseb J. 2005;19(1):1-11. (Pubitemid 40069914)
13. Yoshiji H, Noguchi R, Kuriyama S, Ikenaka Y, Yoshii J, Yanase K, et al. Imatinib mesylate (STI-571) attenuates liver fibrosis development in rats. Am J Physiol Gastrointest Liver Physiol. 2005;288(5):G907-13. (Pubitemid 40563130)
14. Rajkumar VS, Shiwen X, Bostrom M, Leoni P, Muddle J, Ivarsson M, et al. Platelet-derived growth factor-beta receptor activation is essentialfor fibroblast and pericyte recruitment during cutaneous wound healing. Am J Pathol. 2006;169(6):2254-65. (Pubitemid 351181983)
15. Atallah E, Kantarjian H, Cortes J. Emerging safety issues with imatinib and other Abl tyrosine kinase inhibitors. Clin Lymphoma Myeloma. 2007;7(Suppl 3):S105-12. (Pubitemid 46848464)
16. Druker BJ, Guilhot F, O'Brien SG, Gathmann I, Kantarjian H, Gattermann N, et al. Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia. N Engl J Med. 2006;355(23):2408-17. (Pubitemid 44903745)
17. Distler JH, Distler O. Cardiotoxicity of imatinib mesylate: an extremely rare phenomenon or a major side effect? Ann Rheum Dis. 2007;66(6):836. (Pubitemid 46846711)
18. Kerkela R, Grazette L, Yacobi R, Iliescu C, Patten R, Beahm C, et al. Cardiotoxicity of the cancer therapeutic agent imatinib mesylate. Nat Med. 2006;12(8):908-16. (Pubitemid 44175142)
19. Beham-Schmid C, Apfelbeck U, Sill H, Tsybrovsky O, Hofler G, Haas OA, et al. Treatment of chronic myelogenous leukemia with the tyrosine kinase inhibitor STI571 results in marked regression of bone marrow fibrosis. Blood. 2002;99(1):381-3.
20. Bueso-Ramos CE, Cortes J, Talpaz M, O'Brien S, Giles F, Rios MB, et al. Imatinib mesylate therapy reduces bone marrow fibrosis in patients with chronic myelogenous leukemia. Cancer. 2004;101(2):332-6. (Pubitemid 38890837)
21. Kay J, High WA. Imatinib mesylate treatment of nephrogenic systemic fibrosis. Arthritis Rheum. 2008;58(8):2543-8.
22. Sabnani I, Zucker MJ, Rosenstein ED, Baran DA, Arroyo LH, Tsang P, et al. A novel therapeutic approach to the treatment of scleroderma-associated pulmonary complications: safety and efficacy of combination therapy with imatinib and cyclophosphamide. Rheumatology. (Oxford) 2009;48(1):49-52.
23. Sfikakis PP, Gorgoulis VG, Katsiari CG, Evangelou K, Kostopoulos C, Black CM: Imatinib for the treatment of refractory, diffuse systemic sclerosis. Rheumatology. (Oxford) 2008;47(5):735-7.
24. van Daele PL, Dik WA, Thio HB, van Hal PT, van Laar JA, Hooijkaas H, et al. Is imatinib mesylate a promising drug in systemic sclerosis? Arthritis Rheum. 2008;58(8):2549-52.
25. Magro L, Mohty M, Catteau B, Coiteux V, Chevallier P, Terriou L, et al. Imatinib mesylate as salvage therapy for refractory sclerotic chronic graft-versus-host disease. Blood. 2009;114(3):719-22.
26. Olivieri A, Locatelli F, Zecca M, Sanna A, Cimminiello M, Raimondi R, et al. Imatinib for refractory chronic graft-versus-host disease with fibrotic features. Blood. 2009;114(3):709-18.
27. Distler JH, Manger B, Spriewald BM, Schett G, Distler O. Treatment of pulmonary fibrosis for twenty weeks with imatinib mesylate in a patient with mixed connective tissue disease. Arthritis Rheum. 2008;58(8):2538-42.
28. Quintas-Cardama A, Kantarjian H, Cortes J. Imatinib and beyond - exploring the full potential of targeted therapy for CML. Nat Rev Clin Oncol. 2009;6(9):535-43.
29. Maurer B, Busch N, Jüngel A, Gay RE, Schett G, Michel BA, et al. Tyrosine Kinase Inhibitors (TKI) Are Promising Therapeutic Agents for the Proliferative Vasculopathy in SSc [abstract]. Arthritis Rheum. 2009;60(Suppl 10):1263.
30. Skhirtladze C, Distler O, Dees C, Akhmetshina A, Busch N, Venalis P et al: Src kinases in systemic sclerosis: central roles in fibroblast activation and in skin fibrosis. Arthritis Rheum. 2008;58(5):1475-84. (Pubitemid 351705937)
31. Okutani D, Lodyga M, Han B, Liu M. Src protein tyrosine kinase family and acute inflammatory responses. Am J Physiol Lung Cell Mol Physiol. 2006;291(2):L129-41. (Pubitemid 44148096)
32. Distler O, Distler JH, Scheid A, Acker T, Hirth A, Rethage J, et al. Uncontrolled expression of vascular endothelial growth factor and its receptors leads to insufficient skin angiogenesis in patients with systemic sclerosis. Circ Res. 2004;95(1):109-16. (Pubitemid 38931842)
33. Dor Y, Djonov V, Abramovitch R, Itin A, Fishman GI, Carmeliet P, et al. Conditional switching of VEGF provides new insights into adult neovascularization and pro-angiogenic therapy. Embo J. 2002;21(8):1939-47. (Pubitemid 34437191)
34. Drake CJ, Little CD. Exogenous vascular endothelial growth factor induces malformed and hyperfused vessels during embryonic neovascularization. Proc Natl Acad Sci. USA 1995;92(17):7657-61.
35. Sundberg C, Nagy JA, Brown LF, Feng D, Eckelhoefer IA, Manseau EJ, et al. Glomeruloid microvascular proliferation follows adenoviral vascular permeability factor/vascular endothelial growth factor-164 gene delivery. Am J Pathol. 2001;158(3):1145-60. (Pubitemid 32221807)
36. Beyer C, Schett G, Gay S, Distler O, Distler JH. Hypoxia. Hypoxia in the pathogenesis of systemic sclerosis. Arthritis Res Ther. 2009;11(2):220.
37. Distler JH, Jungel A, Pileckyte M, Zwerina J, Michel BA, Gay RE, et al. Hypoxia-induced increase in the production of extracellular matrix proteins in systemic sclerosis. Arthritis Rheum. 2007;56(12):4203-15. (Pubitemid 350262349)
38. Maurer B, Akhmetshina A, Gay RE, Schett G, Michel BA, Detmar M, et al. VEGF Aggravates Skin Fibrosis in Different Animal Models of Systemic Sclerosis (SSc) [abstract]. Arthritis Rheum. 2009;60(Suppl 10):1060.
39. Petit AM, Rak J, Hung MC, Rockwell P, Goldstein N, Fendly B, et al. Neutralizing antibodies against epidermal growth factor and ErbB-2/neu receptor tyrosine kinases down-regulate vascular endothelial growth factor production by tumor cells in vitro and in vivo: angiogenic implications for signal transduction therapy of solid tumors. Am J Pathol. 1997;151(6):1523-30. (Pubitemid 27527914)
40. Liu JY, Morris GF, Lei WH, Corti M, Brody AR. Up-regulated expression of transforming growth factor-alpha in the bronchiolar-alveolar duct regions of asbestos-exposed rats. Am J Pathol. 1996;149(1):205-17. (Pubitemid 26230992)
41. Madtes DK, Busby HK, Strandjord TP, Clark JG. Expression of transforming growth factor-alpha and epidermal growth factor receptor is increased following bleomycin-induced lung injury in rats. Am J Respir Cell Mol Biol. 1994;11(5):540-51.
42. Van Winkle LS, Isaac JM, Plopper CG. Distribution of epidermal growth factor receptor and ligands during bronchiolar epithelial repair from naphthalene-induced Clara cell injury in the mouse. Am J Pathol. 1997;151(2):443-59. (Pubitemid 27330064)
43. Waheed S, D'Angio CT, Wagner CL, Madtes DK, Finkelstein JN, Paxhia A, et al. Transforming growth factor alpha (TGF(alpha)) is increased during hyperoxia and fibrosis. Exp Lung Res. 2002;28(5):361-72. (Pubitemid 34620666)
44. Hardie WD, Davidson C, Ikegami M, Leikauf GD, Le Cras TD, Prestridge A, et al. EGF receptor tyrosine kinase inhibitors diminish transforming growth factor-alpha-induced pulmonary fibrosis. Am J Physiol Lung Cell Mol Physiol. 2008;294(6):L1217-25.
45. Cho HJ, Kang JH, Kim T, Park KK, Kim CH, Lee IS, et al. Suppression of PAI-1 expression through inhibition of the EGFR-mediated signaling cascade in rat kidney fibroblast by ascofuranone. J Cell Biochem. 2009;107(2):335-44.
46. Yamane K, Ihn H, Tamaki K. Epidermal growth factor up-regulates expression of transforming growth factor beta receptor type II in human dermal fibroblasts by phosphoinositide 3-kinase/Akt signaling pathway: Resistance to epidermal growth factor stimulation in scleroderma fibroblasts. Arthritis Rheum. 2003;48(6):1652-66. (Pubitemid 36682374)