Nilotinib: A novel, selective tyrosine kinase inhibitor

Seminars in Oncology

Volumn 38, Issue 1 SUPPL., 2011, Pages

  Blay, Jean Yves ^a   Von Mehren, Margaret ^b  

^a UNIVERSITÉ LYON 1   (France)

^b FOX CHASE CANCER CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BCR ABL PROTEIN; COLONY STIMULATING FACTOR RECEPTOR; DASATINIB; DISCOIDIN; IMATINIB; NILOTINIB; PLATELET DERIVED GROWTH FACTOR ALPHA RECEPTOR; PLATELET DERIVED GROWTH FACTOR BETA RECEPTOR; SORAFENIB; STEM CELL FACTOR RECEPTOR; SUNITINIB;

ARTICLE; AUTOPHOSPHORYLATION; CELL MUTANT; CHRONIC MYELOID LEUKEMIA; CRYSTAL STRUCTURE; DRUG HYPERSENSITIVITY; DRUG RESISTANCE; DRUG TOLERABILITY; DRUG UPTAKE; GASTROINTESTINAL STROMAL TUMOR; HUMAN; NONHUMAN; PIGMENTED VILLONODULAR SYNOVITIS; PRIORITY JOURNAL; STEM CELL; TUMOR CELL LINE;

CLINICAL TRIALS AS TOPIC; HUMANS; NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRIMIDINES;

EID: 79952765838     PISSN: 00937754     EISSN: None     Source Type: Journal    
DOI: 10.1053/j.seminoncol.2011.01.016     Document Type: Article

References (55)

1. B.J. Druker, S. Tamura, and E. Buchdunger Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells Nat Med 2 1996 561 566
2. L.A. Hazlehurst, N.N. Bewry, R.R. Nair, and J. Pinilla-Ibarz Signaling networks associated with BCR-ABL-dependent transformation Cancer Control 16 2009 100 107
3. T. Schindler, W. Bornmann, and P. Pellicena Structural mechanism for STI-571 inhibition of abelson tyrosine kinase Science 289 2000 1938 1942
4. E. Buchdunger, C.L. Cioffi, and N. Law Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors J Pharmacol Exp Ther 295 2000 139 145
5. NCCN2010 NCCN Clinical Practice Guidelines in Oncology. Chronic myelogenous leukemia v.2.2010 http://www.nccn.org/professionals/physician-gls/ PDF/cml.pdf Last accessed Jan 2010
6. A. Hochhaus, and P. La Rosee Imatinib therapy in chronic myelogenous leukemia: strategies to avoid and overcome resistance Leukemia 18 2004 1321 1331 (Pubitemid 39136739)
7. A. Quintas-Cardama, H.M. Kantarjian, and J.E. Cortes Mechanisms of primary and secondary resistance to imatinib in chronic myeloid leukemia Cancer Control 16 2009 122 131
8. E. Weisberg, P. Manley, and J. Mestan AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL Br J Cancer 94 2006 1765 1769 (Pubitemid 43882564)
9. H. Kantarjian, F. Giles, and L. Wunderle Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL N Engl J Med 354 2006 2542 2551 (Pubitemid 43882350)
10. P. le Coutre, O.G. Ottmann, and F. Giles Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is active in patients with imatinib-resistant or -intolerant accelerated-phase chronic myelogenous leukemia Blood 111 2008 1834 1839 (Pubitemid 351451490)
11. FDA 2007 nilotinib National Cancer Institute (2007) FDA Approval for nilotinib http://www.cancer.gov/cancertopics/druginfo/fda-nilotinib Last accessed: Jan 2010
12. G. Saglio, D.W. Kim, and S. Issaragrisil Nilotinib versus imatinib for newly diagnosed chronic myeloid leukemia N Engl J Med 362 2010 2251 2259
13. Tasigna SOPC 2010 Electronic Medicines Compendium Summary of Product Characteristics. Tasigna (nilotinib) 200mg hard capsules. Novartis Last updated 21 Sept 2009 http://emc.medicines.org.uk/medicine/20827/SPC/ Tasigna+200+mg+hard+capsules/#INDICATIONS Last accessed: Jan 2010
14. P.W. Manley, N. Stiefl, and S.W. Cowan-Jacob Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib Bioorg Med Chem 18 2010 6977 6986
15. P.W. Manley, P. Drueckes, and G. Fendrich Extended kinase profile and properties of the protein kinase inhibitor nilotinib Biochim Biophys Acta 2010 1804 445 453
16. M.C. Heinrich, C.L. Corless, and A. Duensing PDGFRA activating mutations in gastrointestinal stromal tumors Science 299 2003 708 710 (Pubitemid 36159485)
17. S. Hirota, K. Isozaki, and Y. Moriyama Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors Science 279 1998 577 580 (Pubitemid 28067289)
18. R.B. West, B.P. Rubin, and M.A. Miller A landscape effect in tenosynovial giant-cell tumor from activation of CSF1 expression by a translocation in a minority of tumor cells Proc Natl Acad Sci U S A 103 2006 690 695 (Pubitemid 43153087)
19. C.D. Blanke, C. Rankin, and G.D. Demetri Phase III randomized, intergroup trial assessing imatinib mesylate at two dose levels in patients with unresectable or metastatic gastrointestinal stromal tumors expressing the kit receptor tyrosine kinase: S0033 J Clin Oncol 26 2008 626 632 (Pubitemid 351264358)
20. E. Weisberg, P.W. Manley, and W. Breitenstein Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl Cancer Cell 7 2005 129 141 (Pubitemid 40248339)
21. Y. Liu, and N.S. Gray Rational design of inhibitors that bind to inactive kinase conformations Nat Chem Biol 2 2006 358 364 (Pubitemid 43936934)
22. B. Nagar, W.G. Bornmann, and P. Pellicena Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571) Cancer Res 62 2002 4236 4243 (Pubitemid 34827278)
23. E. Jabbour, P. Hochhaus, and G. le Coutre Minimal cross-intolerance between nilotinib and imatinib in patients with imatinib-intolerant chronic myelogenous leukemia (CML) in chronic phase (CP) or accelerated phase (AP) [abstract 7063] J Clin Oncol 2008 26
24. M. Golemovic, S. Verstovsek, and F. Giles AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia Clin Cancer Res 11 2005 4941 4947 (Pubitemid 41557215)
25. T. O'Hare, D.K. Walters, and E.P. Stoffregen In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants Cancer Res 65 2005 4500 4505 (Pubitemid 40740783)
26. + CML cells Blood 109 2007 4016 4019 (Pubitemid 46641755)
27. S. Dirnhofer, and S. Leyvraz Current standards and progress in understanding and treatment of GIST Swiss Med Wkly 139 2009 90 102
28. C.L. Corless, and M.C. Heinrich Molecular pathobiology of gastrointestinal stromal sarcomas Annu Rev Pathol 3 2008 557 586 (Pubitemid 351488293)
29. K.G. Roberts, A.F. Odell, and E.M. Byrnes Resistance to c-KIT kinase inhibitors conferred by V654A mutation Mol Cancer Ther 6 2007 1159 1166 (Pubitemid 46554587)
30. C. Cullinane, A. Natoli, and Y. Hui Preclinical evaluation of nilotinib efficacy in an imatinib-resistant KIT-driven tumor model Mol Cancer Ther 9 2010 1461 1468
31. N.P. Agaram, M.P. Laquaglia, and B. Ustun Molecular characterization of pediatric gastrointestinal stromal tumors Clin Cancer Res 14 2008 3204 3215
32. C.R. Antonescu, P. Besmer, and T. Guo Acquired resistance to imatinib in gastrointestinal stromal tumor occurs through secondary gene mutation Clin Cancer Res 11 2005 4182 4190 (Pubitemid 40791584)
33. T. Guo, N.P. Agaram, and G.C. Wong Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor Clin Cancer Res 13 2007 4874 4881 (Pubitemid 47294795)
34. L.L. Chen, J.C. Trent, and E.F. Wu A missense mutation in KIT kinase domain 1 correlates with imatinib resistance in gastrointestinal stromal tumors Cancer Res 64 2004 5913 5919 (Pubitemid 39129383)
35. S. Verstovsek, F.J. Giles, and A. Quintas-Cardama Activity of AMN107, a novel aminopyrimidine tyrosine kinase inhibitor, against human FIP1L1-PDGFR-alpha-expressing cells Leuk Res 30 2006 1499 1505 (Pubitemid 44573482)
36. J. Cools, D.J. DeAngelo, and J. Gotlib A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome N Engl J Med 348 2003 1201 1214 (Pubitemid 36359296)
37. E. Weisberg, R.D. Wright, and J. Jiang Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity Gastroenterology 131 2006 1734 1742 (Pubitemid 44958515)
38. E.H. Stover, J. Chen, and B.H. Lee The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo Blood 106 2005 3206 3213 (Pubitemid 41565920)
39. N. von Bubnoff, S.P. Gorantla, S. Thone, C. Peschel, and J. Duyster The FIP1L1-PDGFRA T674I mutation can be inhibited by the tyrosine kinase inhibitor AMN107 (nilotinib) Blood 107 2006 4970 4971 (Pubitemid 43882655)
40. J. Thomas, L. Wang, R.E. Clark, and M. Pirmohamed Active transport of imatinib into and out of cells: implications for drug resistance Blood 104 2004 3739 3745 (Pubitemid 39564452)
41. D.L. White, V.A. Saunders, and P. Dang OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib Blood 108 2006 697 704 (Pubitemid 44061372)
42. H. Prenen, G. Guetens, and G. de Boeck Cellular uptake of the tyrosine kinase inhibitors imatinib and AMN107 in gastrointestinal stromal tumor cell lines Pharmacology 77 2006 11 16
43. D.L. White, V.A. Saunders, S.R. Quinn, P.W. Manley, and T.P. Hughes Imatinib increases the intracellular concentration of nilotinib, which may explain the observed synergy between these drugs Blood 109 2007 3609 3610 (Pubitemid 46572560)
44. E. Weisberg, L. Catley, and R.D. Wright Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias Blood 109 2007 2112 2120 (Pubitemid 46348213)
45. H. Burger, H. van Tol, and M. Brok Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps Cancer Biol Ther 4 2005 747 752 (Pubitemid 41351174)
46. A. Hamada, H. Miyano, H. Watanabe, and H. Saito Interaction of imatinib mesilate with human P-glycoprotein J Pharmacol Exp Ther 307 2003 824 828 (Pubitemid 37310701)
47. F.X. Mahon, F. Belloc, and V. Lagarde MDR1 gene overexpression confers resistance to imatinib mesylate in leukemia cell line models Blood 101 2003 2368 2373 (Pubitemid 36304670)
48. W.M. Mendenhall, C.M. Mendenhall, and J.D. Reith Pigmented villonodular synovitis Am J Clin Oncol 29 2006 548 550 (Pubitemid 44915288)
49. J.Y. Blay, H. El Sayadi, P. Thiesse, J. Garret, and I. Ray-Coquard Complete response to imatinib in relapsing pigmented villonodular synovitis/tenosynovial giant cell tumor (PVNS/TGCT) Ann Oncol 19 2008 821 822 (Pubitemid 351461057)
50. P.A. Cassier, and J.Y. Blay Imatinib mesylate for the treatment of gastrointestinal stromal tumor Expert Rev Anticancer Ther 10 2010 623 634
51. V. Ravi, W. Wang, and D.M. Araujo Imatinib in the treatment of tenosynovial giant-cell tumor and pigmented villonodular synovitis [abstract 10011] J Clin Oncol 2010 28
52. G.D. Demetri, A.T. van Oosterom, and C.R. Garrett Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial Lancet 368 2006 1329 1338 (Pubitemid 44528723)
53. G.D. Demetri, P.G. Casali, and J.Y. Blay A phase I study of single-agent nilotinib or in combination with imatinib in patients with imatinib-resistant gastrointestinal stromal tumors Clin Cancer Res 15 2009 5910 5916
54. M. Montemurro, P. Schoffski, and P. Reichardt Nilotinib in the treatment of advanced gastrointestinal stromal tumours resistant to both imatinib and sunitinib Eur J Cancer 45 2009 2293 2297
55. S. Verstovsek, C. Akin, and T. Manshouri Effects of AMN107, a novel aminopyrimidine tyrosine kinase inhibitor, on human mast cells bearing wild-type or mutated codon 816 c-kit Leuk Res 30 2006 1365 1370 (Pubitemid 44307328)