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Science 16 July 2004: Vol. 305. no. 5682, pp. 399 - 401 DOI: 10.1126/science.1099480
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Reports
Overriding Imatinib Resistance with a Novel ABL Kinase Inhibitor
Neil P. Shah,1
Chris Tran,1,2
Francis Y. Lee,3
Ping Chen,3
Derek Norris,3
Charles L. Sawyers1,2*
Resistance to the ABL kinase inhibitor imatinib (STI571 or Gleevec) in chronic myeloid leukemia (CML) occurs through selection for tumor cells harboring BCR-ABL kinase domain point mutations that interfere with drug binding. Crystallographic studies predict that most imatinib-resistant mutants should remain sensitive to inhibitors that bind ABL with less stringent conformational requirements. BMS-354825 is an orally bioavailable ABL kinase inhibitor with two-log increased potency relative to imatinib that retains activity against 14 of 15 imatinib-resistant BCR-ABL mutants. BMS-354825 prolongs survival of mice with BCR-ABLdriven disease and inhibits proliferation of BCR-ABLpositive bone marrow progenitor cells from patients with imatinib-sensitive and imatinib-resistant CML. These data illustrate how molecular insight into kinase inhibitor resistance can guide the design of second-generation targeted therapies.
1 Division of Hematology and Oncology, Department of Medicine, The David Geffen School of Medicine, University of California, Los Angeles, CA, 90095, USA.
2 Howard Hughes Medical Institute, The David Geffen School of Medicine, University of California, Los Angeles, CA, 90095, USA.
3 Bristol-Myers Squibb Oncology, Princeton, NJ, USA.
* To whom correspondence should be addressed. E-mail: csawyers{at}mednet.ucla.edu
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- Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome positive chronic myelogenous leukemia in chronic phase following imatinib resistance and intolerance.
- H. M. Kantarjian, F. Giles, N. Gattermann, K. Bhalla, G. Alimena, F. Palandri, G. J. Ossenkoppele, F.-E. Nicolini, S. G. O'Brien, M. Litzow, et al. (2007)
Blood
110, 3540-3546
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- Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT.
- K. V. Gleixner, M. Mayerhofer, K. Sonneck, A. Gruze, P. Samorapoompichit, C. Baumgartner, F. Y. Lee, K. J. Aichberger, P. W. Manley, D. Fabbro, et al. (2007)
Haematologica
92, 1451-1459
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- How I treat chronic myeloid leukemia in the imatinib era.
- J. M. Goldman (2007)
Blood
110, 2828-2837
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- Interferon-{alpha} or homoharringtonine as salvage treatment for chronic myeloid leukemia patients who acquire the T315I BCR-ABL mutation.
- H. de Lavallade, J. S. Khorashad, H. P. Davis, D. Milojkovic, J. S. Kaeda, J. M. Goldman, J. F. Apperley, and D. Marin (2007)
Blood
110, 2779-2780
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- Dasatinib induces rapid hematologic and cytogenetic responses in adult patients with Philadelphia chromosome positive acute lymphoblastic leukemia with resistance or intolerance to imatinib: interim results of a phase 2 study.
- O. Ottmann, H. Dombret, G. Martinelli, B. Simonsson, F. Guilhot, R. A. Larson, G. Rege-Cambrin, J. Radich, A. Hochhaus, A. M. Apanovitch, et al. (2007)
Blood
110, 2309-2315
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- Bcr-Abl kinase domain mutations, drug resistance, and the road to a cure for chronic myeloid leukemia.
- T. O'Hare, C. A. Eide, and M. W. N. Deininger (2007)
Blood
110, 2242-2249
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- Progressive Thoughts about Progressive Disease.
- N. P. Shah (2007)
Clin. Cancer Res.
13, 5229-5231
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- Pleural Effusion in Patients With Chronic Myelogenous Leukemia Treated With Dasatinib After Imatinib Failure.
- A. Quintas-Cardama, H. Kantarjian, S. O'Brien, G. Borthakur, J. Bruzzi, R. Munden, and J. Cortes (2007)
J. Clin. Oncol.
25, 3908-3914
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- Sorafenib Inhibits the Imatinib-Resistant KITT670I Gatekeeper Mutation in Gastrointestinal Stromal Tumor.
- T. Guo, N. P. Agaram, G. C. Wong, G. Hom, D. D'Adamo, R. G. Maki, G. K. Schwartz, D. Veach, B. D. Clarkson, S. Singer, et al. (2007)
Clin. Cancer Res.
13, 4874-4881
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- The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.
- O. Hantschel, U. Rix, U. Schmidt, T. Burckstummer, M. Kneidinger, G. Schutze, J. Colinge, K. L. Bennett, W. Ellmeier, P. Valent, et al. (2007)
PNAS
104, 13283-13288
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- Oncogenic Activity of Epidermal Growth Factor Receptor Kinase Mutant Alleles Is Enhanced by the T790M Drug Resistance Mutation.
- N. Godin-Heymann, I. Bryant, M. N. Rivera, L. Ulkus, D. W. Bell, D. J. Riese II, J. Settleman, and D. A. Haber (2007)
Cancer Res.
67, 7319-7326
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- Inhibition of heat shock protein 90 prolongs survival of mice with BCR-ABL-T315I-induced leukemia and suppresses leukemic stem cells.
- C. Peng, J. Brain, Y. Hu, A. Goodrich, L. Kong, D. Grayzel, R. Pak, M. Read, and S. Li (2007)
Blood
110, 678-685
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- Kinase domain mutations of BCR-ABL frequently precede imatinib-based therapy and give rise to relapse in patients with de novo Philadelphia-positive acute lymphoblastic leukemia (Ph+ ALL).
- H. Pfeifer, B. Wassmann, A. Pavlova, L. Wunderle, J. Oldenburg, A. Binckebanck, T. Lange, A. Hochhaus, S. Wystub, P. Bruck, et al. (2007)
Blood
110, 727-734
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- Inhibition of the T790M Gatekeeper Mutant of the Epidermal Growth Factor Receptor by EXEL-7647.
- S. B. Gendreau, R. Ventura, P. Keast, A. D. Laird, F. M. Yakes, W. Zhang, F. Bentzien, B. Cancilla, J. Lutman, F. Chu, et al. (2007)
Clin. Cancer Res.
13, 3713-3723
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- Dasatinib or high-dose imatinib for chronic-phase chronic myeloid leukemia after failure of first-line imatinib: a randomized phase 2 trial.
- H. Kantarjian, R. Pasquini, N. Hamerschlak, P. Rousselot, J. Holowiecki, S. Jootar, T. Robak, N. Khoroshko, T. Masszi, A. Skotnicki, et al. (2007)
Blood
109, 5143-5150
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- Dynamics of cytogenetic aberrations in Philadelphia chromosome positive and negative hematopoiesis during dasatinib therapy of chronic myeloid leukemia patients after imatinib failure.
- A. Fabarius, C. Haferlach, M. C. Muller, P. Erben, T. Lahaye, M. Giehl, O. Frank, W. Seifarth, R. Hehlmann, and A. Hochhaus (2007)
Haematologica
92, 834-837
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- Sorafenib Inhibits Imatinib-Resistant KIT and Platelet-Derived Growth Factor Receptor {beta} Gatekeeper Mutants.
- T. Guida, S. Anaganti, L. Provitera, R. Gedrich, E. Sullivan, S. M. Wilhelm, M. Santoro, and F. Carlomagno (2007)
Clin. Cancer Res.
13, 3363-3369
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- Dasatinib induces significant hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in accelerated phase.
- F. Guilhot, J. Apperley, D.-W. Kim, E. O. Bullorsky, M. Baccarani, G. J. Roboz, S. Amadori, C. A. de Souza, J. H. Lipton, A. Hochhaus, et al. (2007)
Blood
109, 4143-4150
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- Instability of BCR-ABL Gene in Primary and Cultured Chronic Myeloid Leukemia Stem Cells.
- X. Jiang, K. M. Saw, A. Eaves, and C. Eaves (2007)
J Natl Cancer Inst
99, 680-693
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- MEK1/2 inhibitors sensitize Bcr/Abl+ human leukemia cells to the dual Abl/Src inhibitor BMS-354/825.
- T. K. Nguyen, M. Rahmani, H. Harada, P. Dent, and S. Grant (2007)
Blood
109, 4006-4015
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- Unraveling CML phase by phase.
- J. Goldman (2007)
Blood
109, 3128
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- Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis.
- J. Cortes, P. Rousselot, D.-W. Kim, E. Ritchie, N. Hamerschlak, S. Coutre, A. Hochhaus, F. Guilhot, G. Saglio, J. Apperley, et al. (2007)
Blood
109, 3207-3213
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