Dasatinib

Drugs of Today

Volumn 43, Issue 1, 2007, Pages 5-12

  Shah, Neil P ^a,b  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b UCSF Hematology Oncology   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALPHA INTERFERON; BCR ABL PROTEIN; CYCLOPROPANECARBOXYLIC ACID [4 [4 (4 METHYL 1 PIPERAZINYL) 6 (5 METHYL 2H PYRAZOL 3 YLAMINO) 2 PYRIMIDINYLTHIO]PHENYL]AMIDE; CYTARABINE; DASATINIB; ERLOTINIB; GEFITINIB; IMATINIB; PROTEIN TYROSINE KINASE;

ACUTE LYMPHOBLASTIC LEUKEMIA; CANCER; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; CYTOPENIA; DRUG DOSE COMPARISON; DRUG DOSE REGIMEN; DRUG MEGADOSE; DRUG SENSITIZATION; ENZYME INHIBITION; HUMAN; LUNG CANCER; LUNG NON SMALL CELL CANCER; NONHUMAN; PANCREAS ADENOCARCINOMA; PLEURA EFFUSION; REVIEW; TREATMENT OUTCOME; TREATMENT RESPONSE;

DRUG EVALUATION, PRECLINICAL; HUMANS; LEUKEMIA, MYELOID, CHRONIC; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRIMIDINES; THIAZOLES;

EID: 33947401102     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.2007.43.1.1050791     Document Type: Review

References (44)

1. Druker, B.J., Talpaz, M., Resta, D.J. et al. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med 2001, 344: 1031-7.
2. Heinrich, M.C., Corless, C.L., Demetri, G.D. et al. PDGFRA activating mutations in gastrointestinal stromal tumors. Science 2003, 299: 708-10.
3. Cools, J., DeAngelo, D.J., Gotlib, J. et al. 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 2003, 348: 1201-14.
4. Apperley, J.F., Gardembas, M., Melo, J.V. et al. Response to imatinib mesylate in patients with chronic myeloproliferative diseases with rearrangements of the platelet-derived growth factor receptor beta. N Engl J Med 2002, 347: 481-7.
5. O'Brien, S.G., Guilhot, F., Larson, R.A. 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.
6. Druker, B.J., Guilhot, F., O'Brien, S. et al. Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia. N Engl J Med 2006, 355: 2408-17.
7. Guilhot, F. Sustained durability of responses plus high rates of cytogenetic responses result in long-term benefit for newly diagnosed chronic-phase chronic myeloid leukemia (chronic myeloid leukemia-CP) treated with imatinib (IM) therapy: Update from the IRIS Study. Blood 2004, 104: Abst. 10a.
8. Gorre, M.E., Mohammed, M., Ellwood, K. et al. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science 2001, 293: 876-80.
9. Tamborini, E., Bonadiman, L., Greco, A. et al. A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient. Gastroenterol 2004, 127: 294-9.
10. Pao, W., Wang, T.Y., Riely, G.J. et al. Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med 2005, 2: e73.
11. Kobayashi, S., Boggon, T.J., Dayaram, T. et al. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 2005, 352: 786-92.
12. Schindler, T., Bornmann, W., Pellicena, P., Miller, W.T., Clarkson, B., Kuriyan, J. Structural mechanism for STI-571 inhibition of abelson tyrosine kinase. Science 2000, 289: 1938-42.
13. von Bubnoff, N., Schneller, F., Peschel, C., Duyster, J. BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: A prospective study. Lancet 2002, 359: 487-91.
14. Branford, S., Rudzki, Z., Walsh, S. et al. High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance. Blood 2002, 99: 3472-5.
15. Hofmann, W.K., de Vos, S., Elashoff D. et al. Relation between resistance of Philadelphia-chromosome-positive acute lymphoblastic leukaemia to the tyrosine kinase inhibitor STI571 and gene-expression profiles: A gene-expression study. Lancet 2002, 359: 481-6.
16. Roche-Lestienne, C., Soenen-Cornu, V., Grardel-Duflos, N. et al. Several types of mutations of the Abl gene can be found in chronic myeloid leukemia patients resistant to STI571, and they can pre-exist to the onset of treatment. Blood 2002, 100: 1014-8.
17. Shah, N.P., Nicoll, J.M., Nagar, B. et al. Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2002, 2: 117-5.
18. Al-Ali, H.K., Heinrich, M.C., Lange, T. et al. High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in chronic myeloid leukemia patients with secondary resistance to imatinib. Hematol J 2004, 5: 55-60.
19. Hochhus, A., Kreil, S., Corbin, A.S. et al. Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia 2002, 16: 2190-6.
20. Bhatia, R., Holtz, M., Niu, N. et al. Persistence of malignant hematopoietic progenitors in chronic myelogenous leukemia patients in complete cytogenetic remission following imatinib mesylate treatment. Blood 2003, 101: 4701-7.
21. Graham, S.M., Jorgensen, H.G., Allan, E. et al. Primitive, quiescent, Philadelphia-positive stem cells from patients with chronic myeloid leukemia are insensitive to STI571 in vitro. Blood 2002, 99: 319-25.
22. O'Hare, T., Walters, D.K., Stoffregen, E.P. 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: 4500-5.
23. Shah, N.P., Tran, C., Lee, F.Y., Chen, P., Norris, D., Sawyers, C.L. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 2004, 305: 399-401.
24. Lombardo, L.J., Lee, F.Y., Chen, P. et al. Discovery of N-(2-chloro-6-methyl-phenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1 -yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem 2004, 47: 6658-61.
25. Tokarski, J.S., Newitt, J.A., Chang, C.Y. et al. The structure of dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. Cancer Res 2006, 66: 5790-7.
26. Copland, M., Hamilton, A., Elrick, L.J. et al. Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary chronic myeloid leukemia but does not eliminate the quiescent fraction. Blood 2006, 107: 4532-9.
27. Talpaz, M., Shah, N.P., Kantarjian, H. et al. Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med 2006, 354: 2531-41.
28. Evans, T.R., Morgan, M.J., van den Abbeele, A.D. et al. Phase I dose-escalation study of the SRC and multi-kinase inhibitor BMS-354825 in patients (pts) with GIST and other solid tumors. J Clin Oncol 2005, 23: Abst. 3034.
29. Hochhaus, A., Kantarjian, H., Baccarani M. et al. Dasatinib induces notable hematologic and cytogenetic responses in chronic phase chronic myeloid leukemia after failure of imatinib therapy. Blood 2007, in press.
30. Talpaz, M., Apperley, J.F., Kim, D.W. et al. Dasatinib (D) in patients with accelerated phase chronic myeloid leukemia (AP-chronic myeloid leukemia) who are resistant or intolerant to imatinib: Results of the CA180005 'START-A' study. J Clin Oncol 2006, 24 (Suppl.): 6526.
31. Cortes J., Rousselot, P., Kim, D.W. et al. Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis. Blood 2007, in press.
32. Coutre S., Martinelli, G., Dombret, H. et al. Dasatinib (D) in patients (pts) with chronic myelogenous leukemia (chronic myeloid leukemia) in lymphoid blast crisis (LB-chronic myeloid leukemia) or Philadelphia-chromosome positive acute lymphoblastic leukemia (Ph+ALL) who are imatinib (IM)-resistant (IM-R) or intolerant (IM-I): The CA180015 'START-L' study. J Clin Oncol 2006, 24 (Suppl.): 6528.
33. Hu, Y., Liu, Y., Pelletier, S. et al. Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia. Nat Genet 2004, 36 (5): 453-61.
34. Hochhaus, A., Kim, D.W., Rousselot, P. et al. Dasatinib 50 mg or 70 mg b.i.d. vs. 100 mg or 140 mg q.d. in patients with CML in chronic phase resistant or intolerant to imatinib: Results of the CA180-034 study. Blood 2006, 108: 141, Abst: 166.
35. Kantarjian, H., Ottmann, O., Pasquini, R. et al. Dasatinib 140 mg q.d. vs. 70 mg b.i.d. in advanced phase CML (ABP-CML) or Ph(+) ALL resistant or intolerant to imatinib - Results of the CA180-035 study. Blood 2006, 108: 224a, Abst. 746.
36. Shah, N., Rousselot, P., Pasquini, D. et al. Dasatinib (D) vs high dose Imatinib (IM) in patients (pts) with chronic phase chronic myeloid leukemia (CP-chronic myeloid leukemia) resistant to imatinib. Results of CA180017 START-R randomized trial. J Clin Oncol 2006, 24 (Suppl.): 6507.
37. Burgess, M.R., Skaggs, B.J., Shah, N.P. et al. Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance. Proc Natl Acad Sci USA 2005, 102: 3395-400.
38. O'Hare, T., Walters, D.K., Stoffregen, E.P. 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 (19 Pt 1): 6987-93.
39. Carter, TA.,, Wodicka, L.M., Shah, N.P. et al. Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci USA 2005, 102: 11011-6.
40. Young, M.A., Shah, N.P., Chao, L.H. et al. Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680. Cancer Res 2006, 66: 1007-14.
41. Giles, F.J., Cortes, J.E., Jones, D., Bergstrom, D.A., Kantarjian, H.M., Freedman, S.J. MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation. Blood 2007, 109: 500-2.
42. Shah, N.P., Lee, F.Y., Luo, R., Jiang, Y., Donker, M., Akin, C. Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood 2006, 108: 286-91.
43. Song, L., Morris, M., Bagui, T., Lee, F.Y., Jove, R., Haura, E.B. Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res 2006, 66: 5542-8.
44. Trevino, J.G., Summy, J.M., Lesslie, D.P. et al. Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Am J Pathol 2006, 168: 962-72.