Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias

Blood

Volumn 109, Issue 5, 2007, Pages 2112-2120

  Weisberg, Ellen ^a   Catley, Laurie ^a   Wright, Renee D ^a   Moreno, Daisy ^a   Banerji, Lolita ^a   Ray, Arghya ^a   Manley, Paul W ^b   Mestan, Juergen ^b   Fabbro, Doriano ^b   Jiang, Jingrui ^a   Hall Meyers, Elizabeth ^a   Callahan, Linda ^a   DellaGatta, Jamie L ^a   Kung, Andrew L ^a   Griffin, James D ^a  

^a DANA FARBER CANCER INSTITUTE   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

BCR ABL PROTEIN; IMATINIB; NILOTINIB;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; BIOLUMINESCENCE; CELL CYCLE; CELL VIABILITY; CHRONIC MYELOID LEUKEMIA; COMBINATION CHEMOTHERAPY; CYTOTOXICITY; DRUG ACTIVITY; DRUG BINDING; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG POTENTIATION; DRUG SENSITIVITY; GENE EXPRESSION; GENE MUTATION; HUMAN; HUMAN CELL; MONOTHERAPY; MOUSE; NONHUMAN; ONCOGENE; PRIORITY JOURNAL; TREATMENT FAILURE; TREATMENT OUTCOME; TUMOR REGRESSION;

EID: 33847379510     PISSN: 00064971     EISSN: 00064971     Source Type: Journal    
DOI: 10.1182/blood-2006-06-026377     Document Type: Article

References (39)

1. Deininger MWN, Goldman JM, Melo JV. The molecular biology of chronic myeloid leukemia. Blood. 2000;96:3343-3356.
2. Melo JV, Myint H, Galton DA, Goldman JM. P190BCR-ABL chronic myeloid leukaemia: the missing link with chronic myelomonocytic leukaemia? Leukemia. 1994;8:208-211.
3. Ravandi F, Cortes J, Albitar M, et al. Chronic myelogenous leukaemia with p185BCR-ABL expression: characteristics and clinical significance. Br J Haematol. 1999;107:581-586.
4. Kantarjian HM, Talpaz M. Definition of the accelerated phase of chronic myelogenous leukemia. J Clin Oncol. 1988;6:180-182.
5. O'Dwyer ME, Mauro MJ, Kurilik G, et al. The impact of clonal evolution on response to imatinib mesylate (STI571) in accelerated phase CML. Blood. 2002;100:1628-1633.
6. Druker BJ, Tamura S, Buchdunger E, et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of BCR-ABL positive cells. Nat Med. 1996;2:561-566.
7. Buchdunger E, Matter A, Druker BJ. BCR-ABL inhibition as a modality of CML therapeutics. Biochim Biophys Acta. 2001;1551:M11-M18.
8. O'Brien SG, Guilhot F, Larson RA, et al. Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med. 2003;348:994-1004.
9. Sawyers CL, Hochhaus A, Feldman E, et al. Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a phase II study. Blood. 2002;99:3530-3539.
10. Ottmann OG, Druker BJ, Sawyers CL, et al. A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias. Blood. 2002;100:1965-1971.
11. Gorre ME, Mohammed M, Ellwood K, et al. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science. 2001;293:876-880.
12. Cowan-Jacob SW, Guez V, Griffin JD, et al. Bcr-Abl kinase mutations and drug resistance to imatinib (STI571) in chronic myelogenous leukemia. Mini Rev Med Chem. 2004;4:285-299.
13. le Coutre P, Tassi E, Varella-Garcia M, et al. Induction of resistance to the Abelson inhibitor STI571 in human leukemic cells through gene amplification. Blood. 2000;95:1758-1766.
14. Weisberg E, Griffin JD. Mechanism of resistance to the ABL tyrosine kinase inhibitor STI571 in BCR-ABL-transformed hematopoietic cell lines. Blood. 2000;95:3498-3505.
15. Mahon FX, Deininger MV, Schultheis B, Chabrol Reiffers J, Goldman JM, Melo JV. Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: diverse mechanisms of resistance. Blood. 2000;96:1070-1079.
16. Campbell LJ, Patsouris C, Rayeroux KC, Somana K, Januszewicz EH, Szer J. BCR-ABL amplification in chronic myelocytic leukemia blast crisis following imatinib mesylate administration. Cancer Genet Cytogenet. 2002;139:30-33.
17. Hochhaus A, Kreil S, Corbin AS, et al. Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia. 2002;16:2190-2196.
18. Morel F, Bris MJ, Herry A, et al. Double minutes containing amplified bcr-abl fusion gene in a case of chronic myeloid leukemia treated by imatinib. Eur J Haematol. 2003;70:235-239.
19. Manley PW, Breitenstein W, Bruggen J, et al. Urea-derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases. Bioorg Med Chem Lett. 2004;14:5793-5797.
20. Weisberg E, Manley PW, Breitenstein W, et al. Characterization of AMN107, a selective inhibitor of native and mutant BCR-ABL. Cancer Cell. 2005;7:129-141.
21. Kantarjian H, Giles F, Wunderle L, et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N Eng J Med. 2006;354:2542-2551.
22. Matulonis U, Salgia R, Okuda K, Druker B, Griffin JD. IL-3 and p210 BCR-ABL activate both unique and overlapping pathways of signal transduction in a factor-dependent myeloid cell line. Exp Hematol. 1993;21:1460-1466.
23. Ray A, Cowan-Jacob S, Manley PW, Mestan J, Griffin JD. Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 by a random mutagenesis study [abstract]. Blood. 2005;106:148a.
24. Weisberg E, Boulton C, Kelly LM, et al. Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitors PKC412. Cancer Cell. 2002;1:433-443.
25. Chou T-C, Talalay P. Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv Enz Regul. 1984;22:27-55.
26. Armstrong SA, Kung AL, Mabon ME, et al. Validation of a therapeutic target identified by gene expression based classification. Cancer Cell. 2003;3:173-183.
27. Shah NP, Tran C, Lee FY, Chen P, Norris D, Sawyers CL. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science. 2004:305:399-401.
28. O'Hare T, Walters DK, Stoffregen EP, et al. In vitro activity of BCR-ABL inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005;65:4500-4505.
29. Deininger MWN, Bradeen H, Jia T, et al. Comparison of imatinib, AMN107, and dasatinib in an accelerated cell-based mutagenesis screen [abstract]. Blood. 2005;106:204a.
30. Shah NP, Nicoll JM, Branford S, et al. Molecular analysis of dasatinib resistance mechanisms in CML patients identifies novel BCR-ABL mutations predicted to retain sensitivity to imatinib: rationale for combination tyrosine kinase inhibitor therapy [abstract]. Blood. 2005;106:318a.
31. Von Bubnoff N, Manley PW, Mestan J, Sanger J, Peschel C, Duyster J. BCR-ABL resistance screening predicts a limited spectrum of point mutations to be associated with clinical resistance to the Abl kinase inhibitor nilotinib (AMN107). Blood. 2006;108:1328-1333.
32. Bradeen HA, Eide CA, O'Hare T, et al. Comparison of imatnib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations. Prepublished on June 13, 2006, as DOI 10.1182/blood-2006-02-004580. (Now available as Blood. 2006;108:2332-2338.)
33. Burgess MR, Skaggs BJ, Shah NP, Lee FY, Sawyers CL. Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance. Proc Natl Acad Sci U S A. 2005;102:3395-3400.
34. O'Hare T, Walters DK, Stoffregen EP, et al. Combined Abl inhibitor therapy for minimizing drug resistance in chronic myeloid leukemia: Src/Abl inhibitors are compatible with imatinib. Clin Cancer Res. 2005;11:6987-6993.
35. Azam M, Latek RR, Daley GQ. Mechanism of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL. Cell. 2003;112:831-843.
36. Rourmiantsev S, Shah NP, Gorre ME, et al. Clinical resistance to the kinase inhibitor STI-571 in chronic myeloid leukemia by mutation of Tyr-253 in the Abl kinase domain P-loop. Proc Natl Acad Sci U S A. 2002;99:10700-10705.
37. Schindler T, Bornmann W, Pellicena P, Miller WT, Clarkson B, Kurlyan J. Structural mechanism for STI-571 inhibition of Abelson Tyrosine Kinase. Science. 2000;289:1938-1942.
38. Jorgensen H, Allan E, Jordanides N, Hamilton A, Mountford T. AMN107 appears equipotent and may synergise with imatinib at the CML stem cell level through interaction with ABCG2 [abstract]. Blood. 2005;106:1080a.
39. White DL, Saunders VA, Dang P, et al. 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. 2006;108:697-704.