Bosutinib for the treatment of chronic myeloid leukemia in chronic phase

Drugs of Today

Volumn 48, Issue 3, 2012, Pages 177-188

  Quintas Cardama A ^a   Kantarjian, H ^a   Cortes, Jorge ^a  

^a UNIVERSITY OF TEXAS   (United States)

Author keywords

BCR ABL1; Bosutinib; Chronic myeloid leukemia; Tyrosine kinase inhibitors

Indexed keywords

ALPHA INTERFERON; BCR ABL PROTEIN; BOSUTINIB; CYTARABINE; CYTOCHROME P450 3A4; DASATINIB; IMATINIB; MOXIFLOXACIN; NILOTINIB;

ABDOMINAL PAIN; ANEMIA; APPETITE; ARTHRALGIA; BACKACHE; CANCER PATIENT; CANCER SURVIVAL; CHRONIC MYELOID LEUKEMIA; CHRONIC MYELOID LEUKEMIA IN CHRONIC PHASE; COUGHING; DIARRHEA; DIZZINESS; DRUG EFFECT; DRUG EXPOSURE; DRUG INDUCED HEADACHE; DRUG SAFETY; EDEMA; EVENT FREE SURVIVAL; FATIGUE; FEVER; GENE MUTATION; HUMAN; HYPOCALCEMIA; HYPOPHOSPHATEMIA; LOW DRUG DOSE; NAUSEA; NEUTROPENIA; NONHUMAN; ORTHOSTATIC HYPOTENSION; PATHOGENESIS; PROGRESSION FREE SURVIVAL; PROTEIN PHOSPHORYLATION; RASH; REVIEW; RHINOPHARYNGITIS; SIDE EFFECT; SINGLE DRUG DOSE; TACHYCARDIA; THROMBOCYTOPENIA; TREATMENT FAILURE; TREATMENT RESPONSE;

ANILINE COMPOUNDS; ANIMALS; CLINICAL TRIALS AS TOPIC; DRUG EVALUATION, PRECLINICAL; HUMANS; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; NITRILES; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRIMIDINES; QUINOLINES; TREATMENT FAILURE;

EID: 84859717516     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.2012.48.3.1750274     Document Type: Review

References (48)

1. Quintas-Cardama, A., Cortes, J. Molecular biology of bcrabl1- positive chronic myeloid leukemia. Blood 2009, 113(8): 1619-30.
2. Gishizky, M.L., Johnson-White, J., Witte, O.N. Efficient transplantation of BCR-ABL-induced chronic myelogenous leukemia-like syndrome in mice. Proc Natl Acad Sci U S A 1993, 90(8): 3755-9. (Pubitemid 23111446)
3. Druker, B.J., Guilhot, F., O'Brien, S.G. 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)
4. Sawyers, C.L., 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(10): 3530-9. (Pubitemid 34534519)
5. Talpaz, M., Silver, R.T., Druker, B.J. et al. Imatinib induces durable hematologic and cytogenetic responses in patients with accelerated phase chronic myeloid leukemia: results of a phase 2 study. Blood 2002, 99(6): 1928-37. (Pubitemid 34525471)
6. Kantarjian, H., Sawyers, C., Hochhaus, A. et al. Hematologic and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia. N Engl J Med 2002, 346(9): 645-52. (Pubitemid 34815868)
7. Nagar, B., Bornmann, W.G., Pellicena, P. et al. Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571). Cancer Res 2002, 62(15): 4236-43. (Pubitemid 34827278)
8. 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(5486): 1938-42.
9. Beran, M., Cao, X., Estrov, Z. et al. Selective inhibition of cell proliferation and BCR-ABL phosphorylation in acute lymphoblastic leukemia cells expressing Mr 190,000 BCR-ABL protein by a tyrosine kinase inhibitor (CGP-57148). Clin Cancer Res 1998, 4(7): 1661-72. (Pubitemid 28304727)
10. Druker, B.J., 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(5): 561-6.
11. Gambacorti-Passerini, C., le Coutre, P., Mologni, L. et al. Inhibition of the ABL kinase activity blocks the proliferation of BCR/ABL+ leukemic cells and induces apoptosis. Blood Cells Mol Dis 1997, 23(3): 380-94. (Pubitemid 28123720)
12. Deininger, M.W., Goldman, J.M., Lydon, N., Melo, J.V. The tyrosine kinase inhibitor CGP57148B selectively inhibits the growth of BCR-ABL-positive cells. Blood 1997, 90(9): 3691-8. (Pubitemid 27473440)
13. 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(11): 994-1004. (Pubitemid 36302244)
14. Deininger, M., O'Brien, S.G., Guilhot, F. et al. International randomized study of interferon vs STI571 (IRIS) 8-year follow up: Sustained survival and low risk for progression or events in patients with newly diagnosed chronic myeloid leukemia in chronic phase (CML-CP) treated with imatinib. Blood [51st Annu Meet Am Soc Hematol (Dec 5-8, New Orleans) 2009] 2009, 114(22): Abst 1126.
15. Apperley, J.F. Part I: mechanisms of resistance to imatinib in chronic myeloid leukaemia. Lancet Oncol 2007, 8(11): 1018-29. (Pubitemid 47629897)
16. 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(5682): 399-401. (Pubitemid 38938156)
17. 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(11): 4500-5. (Pubitemid 40740783)
18. Gorre, M.E., Ellwood-Yen, K., Chiosis, G., Rosen, N., Sawyers, C.L. BCR-ABL point mutants isolated from patients with imatinib mesylate-resistant chronic myeloid leukemia remain sensitive to inhibitors of the BCR-ABL chaperone heat shock protein 90. Blood 2002, 100(8): 3041-4.
19. Soverini, S., Martinelli, G., Rosti, G. et al. ABL mutations in late chronic phase chronic myeloid leukemia patients with upfront cytogenetic resistance to imatinib are associated with a greater likelihood of progression to blast crisis and shorter survival: a study by the GIMEMA Working Party on Chronic Myeloid Leukemia. J Clin Oncol 2005, 23(18): 4100-9. (Pubitemid 46211315)
20. Jabbour, E., Kantarjian, H., Jones, D. et al. Frequency and clinical significance of BCR-ABL mutations in patients with chronic myeloid leukemia treated with imatinib mesylate. Leukemia 2006, 20(10): 1767-73. (Pubitemid 44574988)
21. Jones, D., Luthra, R., Cortes, J. et al. BCR-ABL fusion transcript types and levels and their interaction with secondary genetic changes in determining the phenotype of Philadelphia chromosome-positive leukemias. Blood 2008, 112(13): 5190-2.
22. 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(27): 6658-61. (Pubitemid 40053752)
23. Weisberg, E., Manley, P.W., Breitenstein, W. et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell 2005, 7(2): 129-41. (Pubitemid 40248339)
24. Shah, N.P., Kantarjian, H.M., Kim, D.W. et al. Intermittent target inhibition with dasatinib 100 mg once daily preserves efficacy and improves tolerability in imatinib-resistant and - intolerant chronic-phase chronic myeloid leukemia. J Clin Oncol 2008, 26(19): 3204-12.
25. Kantarjian, H.M., Giles, F.J., Bhalla, K.N., et al. Update on imatinib-resistant chronic myeloid leukemia patients in chronic phase (CML-CP) on nilotinib therapy at 24 months: Clinical response, safety, and long-term outcomes. Blood [51st Annu Meet Am Soc Hematol (Dec 5-8, New Orleans) 2009] 2009, 114(22): Abst 1129.
26. Saglio, G., Kim, D.W., Issaragrisil, S. et al. Nilotinib versus imatinib for newly diagnosed chronic myeloid leukemia. N Engl J Med 2010, 362(24): 2251-9.
27. Kantarjian, H., Shah, N.P., Hochhaus, A. et al. Dasatinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med 2010, 362(24): 2260-70.
28. Kantarjian, H., Shah, N., Cortes, J., et al. Dasatinib or imatinib (IM) in newly diagnosed chronic myeloid leukemia in chronic phase (CML-CP): Two-year follow-up from DASISION. J Clin Oncol [47th Annu Meet Am Soc Clin Oncol (June 3-7, Chicago) 2011] 2011, 29(Suppl.): Abst 6510.
29. Kantarjian, H.M., Hochhaus, A., Saglio, G. et al. Nilotinib versus imatinib for the treatment of patients with newly diagnosed chronic phase, Philadelphia chromosome-positive, chronic myeloid leukaemia: 24-month minimum follow-up of the phase 3 randomised ENESTnd trial. Lancet Oncol 2011, 12(9): 841-51.
30. Boschelli, D.H., Wang, Y.D., Ye, F. et al. Synthesis and Src kinase inhibitory activity of a series of 4-phenylamino-3-quinolinecarbonitriles. J Med Chem 2001, 44(5): 822-33. (Pubitemid 32171678)
31. Boschelli, D.H., Ye, F., Wang, Y.D. et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem 2001, 44(23): 3965-77. (Pubitemid 33051486)
32. Golas, J.M., Arndt, K., Etienne, C. et al. SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res 2003, 63(2): 375-81. (Pubitemid 36152495)
33. Puttini, M., Coluccia, A.M., Boschelli, F. et al. In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells. Cancer Res 2006, 66(23): 11314-22. (Pubitemid 46009962)
34. Boschelli, F., Arndt, K., Gambacorti-Passerini, C. Bosutinib: a review of preclinical studies in chronic myelogenous leukaemia. Eur J Cancer 2010, 46(10): 1781-9.
35. Konig, H., Holyoake, T.L., Bhatia, R. Effective and selective inhibition of chronic myeloid leukemia primitive hematopoietic progenitors by the dual Src/Abl kinase inhibitor SKI-606. Blood 2008, 111(4): 2329-38. (Pubitemid 351451441)
36. Konig, H., Copland, M., Chu, S. Effects of dasatinib on SRC kinase activity and downstream intracellular signaling in primitive chronic myelogenous leukemia hematopoietic cells. Cancer Res 2008, 68(23): 9624-33.
37. Redaelli, S., Piazza, R, Rostagno, R, et al. Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants. J Clin Oncol 2009, 27(3): 469-71.
38. Cortes, J.E., Kantarjian, H.M., Brummendorf, T.H. et al. Safety and efficacy of bosutinib (SKI-606) in chronic phase Philadelphia chromosome-positive CML patients with resistance or intolerance to imatinib. Blood 2011, 118(7): 4567-76.
39. Remsing Rix, L.L., Rix, U., Colinge, J. et al. Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia 2009, 23(3): 477-85.
40. Bantscheff, M., Eberhard, D., Abraham, Y. et al. Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. Nat Biotechnol 2007, 25(9): 1035-44. (Pubitemid 47517638)
41. Abbas, R., Hug, B.A., Leister, C., Gaaloul, M.E., Chalon, S., Sonnichsen, D. A phase I ascending single-dose study of the safety, tolerability, and pharmacokinetics of bosutinib (SKI- 606) in healthy adult subjects. Cancer Chemother Pharmacol 2012, 69(1): 221-7.
42. Abbas, R.A., Hug, B.A., Leister, C., et al. Effect of ketoconazole on the pharmacokinetics of oral bosutinib in healthy subjects. J Clin Pharmacol 2011, 51(12): 1721-7.
43. Abbas, R., Hug, B., Leister, C., Burns, J., Sonnichsen, D. A single dose, crossover, placebo- and moxifloxacin-controlled study to assess the effects of bosutinib (SKI-606) on cardiac repolarization in healthy adult subjects. Haematologica [15th Annu Meet Eur Hematol Assoc (June 10-13, Barcelona) 2010] 2010, 95(Suppl. 2): Abst 0846.
44. Brummendorf, T.H., Cortes, J., Kantarjian, H., et al. Bosutinib (BOS) as third-line therapy for chronic phase (CP) chronic myeloid leukemia (CML) following failure with imatinib (IM) and dasatinib (DAS) or nilotinib (NIL). J Clin Oncol [47th Annu Meet Am Soc Clin Oncol (June 3-7, Chicago) 2011] 2011, 29(Suppl.): Abst 6535.
45. Cortes, J.E., Maru, A., de Souza, C.A., et al. Bosutinib versus imatinib in newly diagnosed chronic phase chronic myeloid leukemia - BELA trial: 24-month follow-up. Blood [53rd Annu Meet Am Soc Hematol (Dec 10-13, San Diego) 2011] 2011, 118(21): Abst 455.
46. Gambacorti-Passerini, C., Cortes, J.E., Harris, P., Powell, C., Countouriotis, A., Kantarjian, H.M. Safety and management of toxicities in the BELA trial of bosutinib versus imatinib in newly diagnosed chronic phase chronic myeloid leukemia. Blood [53rd Annu Meet Am Soc Hematol (Dec 10-13, San Diego) 2011] 2011, 118(21): Abst 1685.
47. Kantarjian, H.M., Giles, F.J., Bhalla, K.N. et al. Nilotinib is effective in patients with chronic myeloid leukemia in chronic phase after imatinib resistance or intolerance: 24-month follow- up results. Blood 2011, 117(4): 1141-5.
48. Hochhaus, A., Baccarani, M., Deininger, M. et al. Dasatinib induces durable cytogenetic responses in patients with chronic myelogenous leukemia in chronic phase with resistance or intolerance to imatinib. Leukemia 2008, 22(6): 1200-6. (Pubitemid 351833788)