BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: A review

Leukemia Research

Volumn 34, Issue 10, 2010, Pages 1255-1268

  An, Xin ^a,b,c   Tiwari, Amit K ^a   Sun, Yibo ^a   Ding, Pei Rong ^a,b,c   Ashby, Charles R ^a   Chen, Zhe Sheng ^a  

^a ST JOHN'S UNIVERSITY   (United States)

^b SUN YAT SEN UNIVERSITY   (China)

^c SUN YAT SEN UNIVERSITY CANCER CENTER   (China)

Author keywords

BCR ABL; CML; Philadelphia chromosome; TKI

Indexed keywords

4 (3 DIMETHYLAMINO 1 PYRROLIDINYLMETHYL) 3 TRIFLUOROMETHYL N [4 METHYL 3 [[4 (5 PYRIMIDINYL) 2 PYRIMIDINYL]AMINO]PHENYL]BENZAMIDE; 6 (2,6 DICHLOROPHENYL) 2 [3 (HYDROXYMETHYL)ANILINO] 8 METHYLPYRIDO[2,3 D]PYRIMIDIN 7(8H) ONE; [4 [2 CYCLOPENTYL 9 (3 HYDROXYPHENETHYL)PURIN 6 YLAMINO]PHENYL]DIMETHYLPHOSPHINE OXIDE; ABC TRANSPORTER; BCR ABL PROTEIN; BILIRUBIN; BMS 354824; BOSUTINIB; CYCLOPROPANECARBOXYLIC ACID [4 [4 (4 METHYL 1 PIPERAZINYL) 6 (5 METHYL 2H PYRAZOL 3 YLAMINO) 2 PYRIMIDINYLTHIO]PHENYL]AMIDE; CYTARABINE; DASATINIB; DORAMAPIMOD; IMATINIB; INTERFERON; LIVER ENZYME; NILOTINIB; OCTAMER TRANSCRIPTION FACTOR 1; ONO 12380; PROTEIN TYROSINE KINASE INHIBITOR; RECOMBINANT ALPHA INTERFERON; TRIACYLGLYCEROL LIPASE; UNCLASSIFIED DRUG;

ABDOMINAL PAIN; ALLOGENEIC HEMATOPOIETIC STEM CELL TRANSPLANTATION; ANTINEOPLASTIC ACTIVITY; AUTOLOGOUS STEM CELL TRANSPLANTATION; BILIRUBIN BLOOD LEVEL; BLEEDING; BLOOD TOXICITY; BONE MARROW SUPPRESSION; CANCER RESISTANCE; CHROMOSOME ANALYSIS; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; CONGESTIVE HEART FAILURE; CONSTIPATION; DIARRHEA; DOSAGE SCHEDULE COMPARISON; DRUG APPROVAL; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG DOSE ESCALATION; DRUG DOSE INCREASE; DRUG EFFICACY; DRUG ERUPTION; DRUG HYPERSENSITIVITY; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG MEGADOSE; DRUG METABOLISM; DRUG POTENTIATION; DRUG RESPONSE; DRUG SAFETY; DRUG TOLERABILITY; DRUG UPTAKE; DRUG WITHDRAWAL; DYSPNEA; EDEMA; ELECTROLYTE DISTURBANCE; FATIGUE; FLUID RETENTION; FLUORESCENCE IN SITU HYBRIDIZATION; GENE AMPLIFICATION; HEART LEFT VENTRICLE FAILURE; HUMAN; IMMUNOMODULATION; LEUKEMOGENESIS; LOW DRUG DOSE; MUSCLE CRAMP; MUSCULOSKELETAL PAIN; MUTATIONAL ANALYSIS; NAUSEA; NEUTROPENIA; NONHUMAN; OUTCOME ASSESSMENT; OVERALL SURVIVAL; PATIENT COMPLIANCE; PATIENT MONITORING; PHILADELPHIA CHROMOSOME POSITIVE CELL; PLEURA EFFUSION; POINT MUTATION; PRIORITY JOURNAL; PROGNOSIS; PROGRESSION FREE SURVIVAL; PRURITUS; QT PROLONGATION; RECOMMENDED DRUG DOSE; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; REVIEW; RISK BENEFIT ANALYSIS; SIDE EFFECT; SIGNAL TRANSDUCTION; SKIN MANIFESTATION; THROMBOCYTOPENIA; TRIACYLGLYCEROL LIPASE BLOOD LEVEL; UNSPECIFIED SIDE EFFECT; VOMITING;

CLINICAL TRIALS AS TOPIC; DRUG RESISTANCE, NEOPLASM; FUSION PROTEINS, BCR-ABL; HUMANS; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; PIPERAZINES; POINT MUTATION; PROTEIN KINASE INHIBITORS; PYRIMIDINES; RNA, MESSENGER;

EID: 77955985510     PISSN: 01452126     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.leukres.2010.04.016     Document Type: Review

References (150)

1. Cortes J. Natural history and staging of chronic myelogenous leukemia. Hematol Oncol Clin North Am 2004, 18:569-584. viii.
2. Faderl S., Talpaz M., Estrov Z., Kantarjian H.M. Chronic myelogenous leukemia: biology and therapy. Ann Intern Med 1999, 131:207-219.
3. Bennett J.H. Case of hypertrophy of the spleen and liver in which death took place from suppuration of the blood. Edinb Med Surg J 1845, 64:413-423.
4. Virchow R.W.B. Frorieps Notizen 1845, p. 36.
5. Nowell P.C.H.D. A minute chromosome in human chronic granulocytic leukemia. Science 1960, 132:1497.
6. Erikson J., Griffin C.A., ar-Rushdi A., Valtieri M., Hoxie J., Finan J., et al. Heterogeneity of chromosome 22 breakpoint in Philadelphia-positive (Ph+) acute lymphocytic leukemia. Proc Natl Acad Sci USA 1986, 83:1807-1811.
7. Rowley J.D. Letter: a new consistent chromosomal abnormality in chronic myelogenous leukaemia identified by quinacrine fluorescence and Giemsa staining. Nature 1973, 243:290-293.
8. Deininger M.W., Goldman J.M., Melo J.V. The molecular biology of chronic myeloid leukemia. Blood 2000, 96:3343-3356.
9. Kantarjian H.M., Talpaz M., Giles F., O'Brien S., Cortes J. New insights into the pathophysiology of chronic myeloid leukemia and imatinib resistance. Ann Intern Med 2006, 145:913-923.
10. Sawyers C.L. Chronic myeloid leukemia. N Engl J Med 1999, 340(April (17)):1330-1340.
11. Kantarjian H.M., Giles F., Quintas-Cardama A., Cortes J. Important therapeutic targets in chronic myelogenous leukemia. Clin Cancer Res 2007, 13(February (4)):1089-1097.
12. Sawyers C.L. Signal transduction pathways involved in BCR-ABL transformation. Baillieres Clin Haematol 1997, 10:223-231.
13. Calabretta B., Perrotti D. The biology of CML blast crisis. Blood 2004, 103:4010-4022.
14. Bolin R.W., Robinson W.A., Sutherland J., Hamman R.F. Busulfan versus hydroxyurea in long-term therapy of chronic myelogenous leukemia. Cancer 1982, 50:1683-1686.
15. Interferon alfa versus chemotherapy for chronic myeloid leukemia: a meta-analysis of seven randomized trials: Chronic Myeloid Leukemia Trialists' Collaborative Group. J Natl Cancer Inst 1997, 89:1616-1620.
16. Bonifazi F., de Vivo A., Rosti G., Guilhot F., Guilhot J., Trabacchi E., et al. Chronic myeloid leukemia and interferon-alpha: a study of complete cytogenetic responders. Blood 2001, 98:3074-3081.
17. Ohnishi K., Ohno R., Tomonaga M., Kamada N., Onozawa K., Kuramoto A., et al. A randomized trial comparing interferon-alpha with busulfan for newly diagnosed chronic myelogenous leukemia in chronic phase. Blood 1995, 86:906-916.
18. Silver R.T., Woolf S.H., Hehlmann R., Appelbaum F.R., Anderson J., Bennett C., et al. An evidence-based analysis of the effect of busulfan, hydroxyurea, interferon, and allogeneic bone marrow transplantation in treating the chronic phase of chronic myeloid leukemia: developed for the American Society of Hematology. Blood 1999, 94:1517-1536.
19. Baccarani M., Saglio G., Goldman J., Hochhaus A., Simonsson B., Appelbaum F., et al. Evolving concepts in the management of chronic myeloid leukemia: recommendations from an expert panel on behalf of the European LeukemiaNet. Blood 2006, 108:1809-1820.
20. Savage D.G., Antman K.H. Imatinib mesylate-a new oral targeted therapy. N Engl J Med 2002, 346:683-693.
21. Sawyers C.L., Hochhaus A., Feldman E., Goldman J.M., Miller C.B., Ottmann O.G., 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.
22. Gorre M.E., Mohammed M., Ellwood K., Hsu N., Paquette R., Rao P.N., et al. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science 2001, 293:876-880.
23. Weisberg E., Manley P.W., Breitenstein W., Bruggen J., Cowan-Jacob S.W., Ray A., et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell 2005, 7:129-141.
24. 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.
25. Golas J.M., Arndt K., Etienne C., Lucas J., Nardin D., Gibbons J., 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, 63:375-381.
26. Kantarjian H.M., Giles F., Quintas-Cardama A., Cortes J. Important therapeutic targets in chronic myelogenous leukemia. Clin Cancer Res 2007, 13:1089-1097.
27. Holtz M.S., Slovak M.L., Zhang F., Sawyers C.L., Forman S.J., Bhatia R. Imatinib mesylate (STI571) inhibits growth of primitive malignant progenitors in chronic myelogenous leukemia through reversal of abnormally increased proliferation. Blood 2002, 99:3792-3800.
28. Druker B.J., Tamura S., Buchdunger E., Ohno S., Segal G.M., Fanning S., 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.
29. Legros L., Bourcier C., Jacquel A., Mahon F.X., Cassuto J.P., Auberger P., et al. Imatinib mesylate (STI571) decreases the vascular endothelial growth factor plasma concentration in patients with chronic myeloid leukemia. Blood 2004, 104:495-501.
30. Kvasnicka H.M., Thiele J., Staib P., Schmitt-Graeff A., Griesshammer M., Klose J., et al. Reversal of bone marrow angiogenesis in chronic myeloid leukemia following imatinib mesylate (STI571) therapy. Blood 2004, 103:3549-3551.
31. Appel S., Boehmler A.M., Grunebach F., Muller M.R., Rupf A., Weck M.M., et al. Imatinib mesylate affects the development and function of dendritic cells generated from CD34+ peripheral blood progenitor cells. Blood 2004, 103(January (2)):538-544.
32. Taieb J., Maruyama K., Borg C., Terme M., Zitvogel L. Imatinib mesylate impairs Flt3L-mediated dendritic cell expansion and antitumor effects in vivo. Blood 2004, 103(March (5)):1966-1967. [author reply 1967].
33. Appel S., Rupf A., Weck M.M., Schoor O., Brummendorf T.H., Weinschenk T., et al. Effects of imatinib on monocyte-derived dendritic cells are mediated by inhibition of nuclear factor-kappaB and Akt signaling pathways. Clin Cancer Res 2005, 11(March (5)):1928-1940.
34. Wang H., Cheng F., Cuenca A., Horna P., Zheng Z., Bhalla K., et al. Imatinib mesylate (STI-571) enhances antigen-presenting cell function and overcomes tumor-induced CD4+ T-cell tolerance. Blood 2005, 105(February (3)):1135-1143.
35. Wehner R., Wendisch M., Schakel K., Bornhauser M., Platzbecker U., Mohr B., et al. Imatinib mesylate does not impair the immunogenicity of human myeloid blood dendritic cells. Leukemia 2006, 20(September (9)):1629-1632.
36. O'Brien S.G., Guilhot F., Larson R.A., Gathmann I., Baccarani M., Cervantes F., 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.
37. Goldman J.M., Melo J.V. Chronic myeloid leukemia-advances in biology and new approaches to treatment. N Engl J Med 2003, 349:1451-1464.
38. Druker B.J., Talpaz M., Resta D.J., Peng B., Buchdunger E., Ford J.M., et al. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med 2001, 344:1031-1037.
39. Ottmann O.G., Druker B.J., Sawyers C.L., Goldman J.M., Reiffers J., Silver R.T., 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.
40. Kimura S., Naito H., Segawa H., Kuroda J., Yuasa T., Sato K., et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood 2005, 106:3948-3954.
41. Manley P.W., Cowan-Jacob S.W., Mestan J. Advances in the structural biology, design and clinical development of Bcr-Abl kinase inhibitors for the treatment of chronic myeloid leukaemia. Biochim Biophys Acta 2005, 1754:3-13.
42. Weisberg E., Manley P., Mestan J., Cowan-Jacob S., Ray A., Griffin J.D. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. Br J Cancer 2006, 94:1765-1769.
43. O'Hare T., Walters D.K., Stoffregen E.P., Jia T., Manley P.W., Mestan J., 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.
44. Quintas-Cardama A., Kantarjian H., Cortes J. Flying under the radar: the new wave of BCR-ABL inhibitors. Nat Rev Drug Discov 2007, 6:834-848.
45. O'Hare T., Pollock R., Stoffregen E.P., Keats J.A., Abdullah O.M., Moseson E.M., et al. Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML. Blood 2004, 104:2532-2539.
46. Wisniewski D., Lambek C.L., Liu C., Strife A., Veach D.R., Nagar B., et al. Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinases. Cancer Res 2002, 62:4244-4255.
47. Gumireddy K., Baker S.J., Cosenza S.C., John P., Kang A.D., Robell K.A., et al. A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance. Proc Natl Acad Sci USA 2005, 102:1992-1997.
48. Giles F.J., Cortes J., Jones D., Bergstrom D., Kantarjian H., 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, 109:500-502.
49. O'Brien S. NCCN clinical practice guidelines in oncology: chronic myelogenous leukemia, version 2.2010. [accessed July 2009]. http://www.nccn.org/professionals/physician_gls/PDF/cml.pdf.
50. Baccarani M., Cortes J., Pane F., Niederwieser D., Saglio G., Apperley J., et al. Chronic myeloid leukemia: an update of concepts and management recommendations of European Leukemia Net. J Clin Oncol 2009, 27:6041-6051.
51. Hughes T.P., Kaeda J., Branford S., Rudzki Z., Hochhaus A., Hensley M.L., et al. Frequency of major molecular responses to imatinib or interferon alfa plus cytarabine in newly diagnosed chronic myeloid leukemia. N Engl J Med 2003, 349(October (15)):1423-1432.
52. Hughes T., Branford S. Molecular monitoring of BCR-ABL as a guide to clinical management in chronic myeloid leukaemia. Blood Rev 2006, 20:29-41.
53. Branford S., Cross N.C., Hochhaus A., Radich J., Saglio G., Kaeda J., et al. Rationale for the recommendations for harmonizing current methodology for detecting BCR-ABL transcripts in patients with chronic myeloid leukaemia. Leukemia 2006, 20(November (11)):1925-1930.
54. Druker B.J., Guilhot F., O'Brien S.G., Gathmann I., Kantarjian H., Gattermann N., et al. Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia. N Engl J Med 2006, 355:2408-2417.
55. Press R.D., Galderisi C., Yang R., Rempfer C., Willis S.G., Mauro M.J., et al. A half-log increase in BCR-ABL RNA predicts a higher risk of relapse in patients with chronic myeloid leukemia with an imatinib-induced complete cytogenetic response. Clin Cancer Res 2007, 13:6136-6143.
56. Khorashad J.S., de Lavallade H., Apperley J.F., Milojkovic D., Reid A.G., Bua M., et al. Finding of kinase domain mutations in patients with chronic phase chronic myeloid leukemia responding to imatinib may identify those at high risk of disease progression. J Clin Oncol 2008, 26:4806-4813.
57. Hughes T., Saglio G., Branford S., Soverini S., Kim D.W., Muller M.C., et al. Impact of baseline BCR-ABL mutations on response to nilotinib in patients with chronic myeloid leukemia in chronic phase. J Clin Oncol 2009, 27:4204-4210.
58. Barnes D.J., Palaiologou D., Panousopoulou E., Schultheis B., Yong A.S., Wong A., et al. Bcr-Abl expression levels determine the rate of development of resistance to imatinib mesylate in chronic myeloid leukemia. Cancer Res 2005, 65:8912-8919.
59. Polakova K.M., Polivkova V., Rulcova J., Klamova H., Jurcek T., Dvorakova D., et al. Constant BCR-ABL transcript level >or =0.1% (IS) in patients with CML responding to imatinib with complete cytogenetic remission may indicate mutation analysis. Exp Hematol 2010, 38(January (1)):20-26.
60. Wang L., Knight K., Lucas C., Clark R.E. The role of serial BCR-ABL transcript monitoring in predicting the emergence of BCR-ABL kinase mutations in imatinib-treated patients with chronic myeloid leukemia. Haematologica 2006, 91:235-239.
61. Press R.D., Willis S.G., Laudadio J., Mauro M.J., Deininger M.W. Determining the rise in BCR-ABL RNA that optimally predicts a kinase domain mutation in patients with chronic myeloid leukemia on imatinib. Blood 2009, 114(September (13)):2598-2605.
62. Talpaz M., Silver R.T., Druker B.J., Goldman J.M., Gambacorti-Passerini C., Guilhot F., 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, 99:1928-1937.
63. Kantarjian H., Sawyers C., Hochhaus A., Guilhot F., Schiffer C., Gambacorti-Passerini C., et al. Hematologic and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia. N Engl J Med 2002, 346:645-652.
64. Hochhaus A., O'Brien S.G., Guilhot F., Druker B.J., Branford S., Foroni L., et al. Six-year follow-up of patients receiving imatinib for the first-line treatment of chronic myeloid leukemia. Leukemia 2009, 23:1054-1061.
65. Cortes J., Giles F., O'Brien S., Thomas D., Garcia-Manero G., Rios M.B., et al. Result of high-dose imatinib mesylate in patients with Philadelphia chromosome-positive chronic myeloid leukemia after failure of interferon-alpha. Blood 2003, 102:83-86.
66. Kantarjian H., Talpaz M., O'Brien S., Garcia-Manero G., Verstovsek S., Giles F., et al. High-dose imatinib mesylate therapy in newly diagnosed Philadelphia chromosome-positive chronic phase chronic myeloid leukemia. Blood 2004, 103:2873-2878.
67. Cortes J., Baccarani M., Guilhot F. A phase III, randomized, open-label study of 400mg versus 800mg of imatinib mesylate (IM) in patients (pts) with newly diagnosed, previously untreated chronic myeloid leukemia in chronic phase (CML-CP) using molecular endpoints: 1-year results of TOPS (tyrosine kinase inhibitor optimization and selectivity) study. ASH Annual Meeting Abstracts, vol. 112 2008, 335.
68. Baranska M., Lewandowski K., Gniot M., Iwola M., Lewandowska M., Komarnicki M. Dasatinib treatment can overcome imatinib and nilotinib resistance in CML patient carrying F359I mutation of BCR-ABL oncogene. J Appl Genet 2008, 49:201-203.
69. Talpaz M., Shah N.P., Kantarjian H., Donato N., Nicoll J., Paquette R., et al. Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med 2006, 354:2531-2541.
70. Hochhaus A., Kantarjian H.M., Baccarani M., Lipton J.H., Apperley J.F., Druker B.J., et al. Dasatinib induces notable hematologic and cytogenetic responses in chronic-phase chronic myeloid leukemia after failure of imatinib therapy. Blood 2007, 109:2303-2309.
71. Hochhaus A., Baccarani M., Deininger M., Apperley J.F., Lipton J.H., Goldberg S.L., et al. Dasatinib induces durable cytogenetic responses in patients with chronic myelogenous leukemia in chronic phase with resistance or intolerance to imatinib. Leukemia 2008, 22:1200-1206.
72. Kantarjian H., Pasquini R., Hamerschlak N., Rousselot P., Holowiecki J., Jootar S., et al. Dasatinib or high-dose imatinib for chronic-phase chronic myeloid leukemia after failure of first-line imatinib: a randomized phase 2 trial. Blood 2007, 109:5143-5150.
73. Kantarjian H., Pasquini R., Levy V., Jootar S., Holowiecki J., Hamerschlak N., et al. Dasatinib or high-dose imatinib for chronic-phase chronic myeloid leukemia resistant to imatinib at a dose of 400 to 600 milligrams daily: two-year follow-up of a randomized phase 2 study (START-R). Cancer 2009, 115:4136-4147.
74. Guilhot F., Apperley J., Kim D.W., Bullorsky E.O., Baccarani M., Roboz G.J., et al. Dasatinib induces significant hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in accelerated phase. Blood 2007, 109:4143-4150.
75. Apperley J.F., Cortes J.E., Kim D.W., Roy L., Roboz G.J., Rosti G., et al. Dasatinib in the treatment of chronic myeloid leukemia in accelerated phase after imatinib failure: the START a trial. J Clin Oncol 2009, 27:3472-3479.
76. Cortes J., Rousselot P., Kim D.W., Ritchie E., Hamerschlak N., Coutre S., et al. Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis. Blood 2007, 109:3207-3213.
77. Cortes J., Kim D.W., Raffoux E., Martinelli G., Ritchie E., Roy L., et al. Efficacy and safety of dasatinib in imatinib-resistant or -intolerant patients with chronic myeloid leukemia in blast phase. Leukemia 2008, 22:2176-2183.
78. Shah N.P., Kantarjian H.M., Kim D.W., Rea D., Dorlhiac-Llacer P.E., Milone J.H., et al. Intermittent target inhibition with dasatinib 100mg once daily preserves efficacy and improves tolerability in imatinib-resistant and -intolerant chronic-phase chronic myeloid leukemia. J Clin Oncol 2008, 26:3204-3212.
79. Stone R.M., Kim D.W., Kantarjian H.M., Rousselot Aea P. Dasatinib dose-optimization study in chronic phase chronic myeloid leukemia (CML-CP): three-year follow-up with dasatinib 100mg once daily and landmark analysis of cytogenetic response and progression-free survival (PFS). J Clin Oncol 2009, 27:7007. (Meeting Abstracts).
80. Kantarjian H., Cortes J., Kim D.W., Dorlhiac-Llacer P., Pasquini R., DiPersio J., et al. Phase 3 study of dasatinib 140mg once daily versus 70mg twice daily in patients with chronic myeloid leukemia in accelerated phase resistant or intolerant to imatinib: 15-month median follow-up. Blood 2009, 113:6322-6329.
81. Borthakur G., Kantarjian H.M. SMOBe, efficacy of dasatinib in patients (pts) with previously untreated chronic myelogenous leukemia (CML) in early chronic phase (CML-CP). J Clin Oncol 2008, 26:7013. [abstracts].
82. Kantarjian H., Giles F., Wunderle L., Bhalla K., O'Brien S., Wassmann B., et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N Engl J Med 2006, 354:2542-2551.
83. Kantarjian H.M., Giles F., Gattermann N., Bhalla K., Alimena G., Palandri F., et al. 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. Blood 2007, 110:3540-3546.
84. Kantarjian H., Giles F., Bhalla K. Nilotinib in chronic myeloid leukemia patients in chronic phase (CML-CP) with imatinib (IM) resistance or intolerance: longer follow-up results of a phase II study. J Clin Oncol 2009, 27:7029. [meeting abstract].
85. Le Coutre P.D., Giles F., Hochhaus A., et al. Nilotinib in chronic myeloid leukemia patients in accelerated phase (CML-AP) with imatinib (IM) resistance or intolerance: longer follow-up results of a phase II study. J Clin Oncol 2009, 27:7057. [meeting abstracts].
86. Giles F.J., Larson R.A., Kantarjian H.M. Nilotinib in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in blast crisis (CML-BC) who are resistant or intolerant to imatinib. J Clin Oncol 2008, 7017. (ASCO Meeting Abstracts).
87. Martinelli G., Castagnetti F., Poerio A., et al. Molecular responses with nilotinib 800mg daily as first-line treatment of chronic myeloid leukemia in chronic phase: results of a phase II trial of the GIMEMA CML WP. J Clin Oncol 2009, 27:7074. [meeting abstracts].
88. Litzow M.R. Imatinib resistance: obstacles and opportunities. Arch Pathol Lab Med 2006, 130:669-679.
89. Shah N.P. Medical management of CML. Hematol Am Soc Hematol Educ Prog 2007, 371-375.
90. Lowenberg B. Minimal residual disease in chronic myeloid leukemia. N Engl J Med 2003, 349:1399-1401.
91. Azam M., Latek R.R., Daley G.Q. Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL. Cell 2003, 112:831-843.
92. Hochhaus A., La Rosee P. Imatinib therapy in chronic myelogenous leukemia: strategies to avoid and overcome resistance. Leukemia 2004, 18:1321-1331.
93. Shah N.P., Nicoll J.M., Nagar B., Gorre M.E., Paquette R.L., Kuriyan J., 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, 2:117-125.
94. Branford S., Rudzki Z., Walsh S., Parkinson I., Grigg A., Szer J., et al. Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis. Blood 2003, 102:276-283.
95. Cortes J., Jabbour E., Kantarjian H., Yin C.C., Shan J., O'Brien S., et al. Dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors. Blood 2007, 110:4005-4011.
96. Hochhaus A., Kreil S., Corbin A.S., La Rosee P., Muller M.C., Lahaye T., et al. Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia 2002, 16:2190-2196.
97. Jabbour E., Kantarjian H., Jones D., Talpaz M., Bekele N., O'Brien S., et al. Frequency and clinical significance of BCR-ABL mutations in patients with chronic myeloid leukemia treated with imatinib mesylate. Leukemia 2006, 20:1767-1773.
98. Soverini S., Colarossi S., Gnani A., Rosti G., Castagnetti F., Poerio A., et al. Contribution of ABL kinase domain mutations to imatinib resistance in different subsets of Philadelphia-positive patients: by the GIMEMA Working Party on Chronic Myeloid Leukemia. Clin Cancer Res 2006, 12:7374-7379.
99. Soverini S., Martinelli G., Rosti G., Bassi S., Amabile M., Poerio A., et al. ABL mutations in late chronic phase chronic myeloid leukemia patients with up-front 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, 23:4100-4109.
100. le Coutre P., Kreuzer K.A., Pursche S., Bonin M., Leopold T., Baskaynak G., et al. Pharmacokinetics and cellular uptake of imatinib and its main metabolite CGP74588. Cancer Chemother Pharmacol 2004, 53:313-323.
101. Peng B., Hayes M., Resta D., Racine-Poon A., Druker B.J., Talpaz M., et al. Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients. J Clin Oncol 2004, 22:935-942.
102. Picard S., Titier K., Etienne G., Teilhet E., Ducint D., Bernard M.A., et al. Trough imatinib plasma levels are associated with both cytogenetic and molecular responses to standard-dose imatinib in chronic myeloid leukemia. Blood 2007, 109:3496-3499.
103. Larson R.A., Druker B.J., Guilhot F., O'Brien S.G., Riviere G.J., Krahnke T., et al. Imatinib pharmacokinetics and its correlation with response and safety in chronic-phase chronic myeloid leukemia: a subanalysis of the IRIS study. Blood 2008, 111:4022-4028.
104. Forrest D.L., Trainor S., Brinkman R.R., Barnett M.J., Hogge D.E., Nevill T.J., et al. Cytogenetic and molecular responses to standard-dose imatinib in chronic myeloid leukemia are correlated with Sokal risk scores and duration of therapy but not trough imatinib plasma levels. Leuk Res 2009, 33:271-275.
105. Darkow T., Henk H.J., Thomas S.K., Feng W., Baladi J.F., Goldberg G.A., et al. Treatment interruptions and non-adherence with imatinib and associated healthcare costs: a retrospective analysis among managed care patients with chronic myelogenous leukaemia. Pharmacoeconomics 2007, 25:481-496.
106. Halpern R., Barghout V., Mody-Patel N., Williams D. Relationship between compliance, costs, hospitalizations for CML and GIST patients using imatinib mesylate [abstract]. J Clin Oncol 2008, 26:5S. [abstract 6598].
107. Noens L., van Lierde M.A., De Bock R., Verhoef G., Zachee P., Berneman Z., et al. Prevalence, determinants, and outcomes of nonadherence to imatinib therapy in patients with chronic myeloid leukemia: the ADAGIO study. Blood 2009, 113:5401-5411.
108. van Erp N.P., Gelderblom H., Karlsson M.O., Li J., Zhao M., Ouwerkerk J., et al. Influence of CYP3A4 inhibition on the steady-state pharmacokinetics of imatinib. Clin Cancer Res 2007, 13:7394-7400.
109. Gréen H., Skoglund K., Rommel F., Mirghani R.A., Lotfi K. CYP3A activity influences imatinib response in patients with chronic myeloid leukemia: a pilot study on in vivo CYP3A activity. Eur J Clin Pharmacol 2010, 66:383-386.
110. Wilkinson G.R. Cytochrome P4503A (CYP3A) metabolism: prediction of in vivo activity in humans. J Pharmacokinet Biopharm 1996, 24:475-490.
111. eng B., Lloyd P., Schran H. Clinical pharmacokinetics of imatinib. Clin Pharmacokinet 2005, 44:879-894.
112. Gambacorti-Passerini C., Zucchetti M., Russo D., Frapolli R., Verga M., Bungaro S., et al. Alpha1 acid glycoprotein binds to imatinib (STI571) and substantially alters its pharmacokinetics in chronic myeloid leukemia patients. Clin Cancer Res 2003, 9:625-632.
113. Jørgensen H.G., Elliott M.A., Allen E.K., Carr C.E., Holyoake T.L., Smith K.D. Alpha1-acid glycoprotein expressed in the plasma of chronic myeloid leukemia patients does not mediate significant in vitro resistance to STI571. Blood 2002, 5:713-715.
114. Gottesman M.M. Mechanisms of cancer drug resistance. Annu Rev Med 2002, 53:615-627.
115. Mahon F.X., Belloc F., Lagarde V., Chollet C., Moreau-Gaudry F., Reiffers J., et al. MDR1 gene overexpression confers resistance to imatinib mesylate in leukemia cell line models. Blood 2003, 101:2368-2373.
116. Ferrao P.T., Frost M.J., Siah S.P., Ashman L.K. Overexpression of P-glycoprotein in K562 cells does not confer resistance to the growth inhibitory effects of imatinib (STI571) in vitro. Blood 2003, 102:4499-4503.
117. Assef Y., Rubio F., Colo G., del Monaco S., Costas M.A., Kotsias B.A. Imatinib resistance in multidrug-resistant K562 human leukemic cells. Leuk Res 2009, 33:710-716.
118. Galimberti S., Cervetti G., Guerrini F., Testi R., Pacini S., Fazzi R., et al. Quantitative molecular monitoring of BCR-ABL and MDR1 transcripts in patients with chronic myeloid leukemia during Imatinib treatment. Cancer Genet Cytogenet 2005, 162:57-62.
119. Hatziieremia S., Jordanides N.E., Holyoake T.L., Mountford J.C., Jorgensen H.G. Inhibition of MDR1 does not sensitize primitive chronic myeloid leukemia CD34+ cells to imatinib. Exp Hematol 2009, 37:692-700.
120. Mao Q., Unadkat J.D. Role of the breast cancer resistance protein (ABCG2) in drug transport. AAPS J 2005, 7:E118-E133.
121. Brendel C., Scharenberg C., Dohse M., Robey R.W., Bates S.E., Shukla S., et al. Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells. Leukemia 2007, 21:1267-1275.
122. Burger H., van Tol H., Boersma A.W., Brok M., Wiemer E.A., Stoter G., et al. Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood 2004, 104:2940-2942.
123. Shukla S., Sauna Z.E., Ambudkar S.V. Evidence for the interaction of imatinib at the transport-substrate site(s) of the multidrug-resistance-linked ABC drug transporters ABCB1 (P-glycoprotein) and ABCG2. Leukemia 2008, 22:445-447.
124. Mahon F.X., Hayette S., Lagarde V., Belloc F., Turcq B., Nicolini F., et al. Evidence that resistance to nilotinib may be due to BCR-ABL, Pgp, or Src kinase overexpression. Cancer Res 2008, 68:9809-9816.
125. Tiwari A.K., Sodani K., Wang S.R., Kuang Y.H., Ashby C.R., Chen X., et al. Nilotinib (AMN107, Tasigna) reverses multidrug resistance by inhibiting the activity of the ABCB1/Pgp and ABCG2/BCRP/MXR transporters. Biochem Pharmacol 2009, 78:153-161.
126. Chen Y., Agarwal S., Shaik N.M., Chen C., Yang Z., Elmquist W.F. P-glycoprotein and breast cancer resistance protein influence brain distribution of dasatinib. J Pharmacol Exp Ther 2009, 330:956-963.
127. Hiwase D.K., Saunders V., Hewett D., Frede A., Zrim S., Dang P., et al. Dasatinib cellular uptake and efflux in chronic myeloid leukemia cells: therapeutic implications. Clin Cancer Res 2008, 14:3881-3888.
128. Kamath A.V., Wang J., Lee F.Y., Marathe P.H. Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL. Cancer Chemother Pharmacol 2008, 61:365-376.
129. Shen T., Kuang Y.H., Ashby C.R., Lei Y., Chen A., Zhou Y., et al. Imatinib and nilotinib reverse multidrug resistance in cancer cells by inhibiting the efflux activity of the MRP7 (ABCC10). PLoS One 2009, 4:e7520.
130. Thomas J., Wang L., Clark R.E., Pirmohamed M. Active transport of imatinib into and out of cells: implications for drug resistance. Blood 2004, 104:3739-3745.
131. White D.L., Saunders V.A., Dang P., Engler J., Venables A., Zrim S., et al. Most CML patients who have a suboptimal response to imatinib have low OCT-1 activity: higher doses of imatinib may overcome the negative impact of low OCT-1 activity. Blood 2007, 110:4064-4072.
132. Niwa T., Asaki T., Kimura S. NS-187 (INNO-406), a Bcr-Abl/Lyn dual tyrosine kinase inhibitor. Anal Chem Insights 2007, 2:93-106.
133. Meyn M.A., Wilson M.B., Abdi F.A., Fahey N., Schiavone A.P., Wu J., et al. Src family kinases phosphorylate the Bcr-Abl SH3-SH2 region and modulate Bcr-Abl transforming activity. J Biol Chem 2006, 281:30907-30916.
134. Donato N.J., Wu J.Y., Stapley J., Gallick G., Lin H., Arlinghaus R., et al. BCR-ABL independence and LYN kinase overexpression in chronic myelogenous leukemia cells selected for resistance to STI571. Blood 2003, 101:690-698.
135. Donato N.J., Wu J.Y., Stapley J., Lin H., Arlinghaus R., Aggarwal B.B., et al. Imatinib mesylate resistance through BCR-ABL independence in chronic myelogenous leukemia. Cancer Res 2004, 64:672-677.
136. Dai Y., Rahmani M., Corey S.J., Dent P., Grant S. A Bcr/Abl-independent, Lyn-dependent form of imatinib mesylate (STI-571) resistance is associated with altered expression of Bcl-2. J Biol Chem 2004, 279:34227-34239.
137. Wu J., Meng F., Kong L.Y., Peng Z., Ying Y., Bornmann W.G., et al. Association between imatinib-resistant BCR-ABL mutation-negative leukemia and persistent activation of LYN kinase. J Natl Cancer Inst 2008, 100:926-939.
138. Redaelli S., Piazza R., Rostagno R., Magistroni V., Perini P., Marega M., et al. Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants. J Clin Oncol 2009, 27:469-471.
139. Puttini M., Coluccia A.M., Boschelli F., Cleris L., Marchesi E., Donella-Deana A., 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, 66:11314-11322.
140. Graham S.M., Jorgensen H.G., Allan E., Pearson C., Alcorn M.J., Richmond L., et al. Primitive, quiescent, Philadelphia-positive stem cells from patients with chronic myeloid leukemia are insensitive to STI571 in vitro. Blood 2002, 99:319-325.
141. Burgering B.M. A brief introduction to FOXOlogy. Oncogene 2008, 27(April (16)):2258-2262.
142. Komatsu N., Watanabe T., Uchida M., Mori M., Kirito K., Kikuchi S., et al. A member of Forkhead transcription factor FKHRL1 is a downstream effector of STI571-induced cell cycle arrest in BCR-ABL-expressing cells. J Biol Chem 2003, 278(February (8)):6411-6419.
143. Marin D., Goldman J.M., Olavarria E., Apperley J.F. Transient benefit only from increasing the imatinib dose in CML patients who do not achieve complete cytogenetic remissions on conventional doses. Blood 2003, 102:2702-2703. [author reply 2703-4].
144. Kantarjian H.M., Larson R.A., Guilhot F., O'Brien S.G., Mone M., Rudoltz M., et al. Efficacy of imatinib dose escalation in patients with chronic myeloid leukemia in chronic phase. Cancer 2009, 115:551-560.
145. Le Coutre P., Ottmann O.G., Giles F., Kim D.W., Cortes J., Gattermann N., et al. 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 2008, 111:1834-1839.
146. Weisser M., Schleuning M., Haferlach C., Schwerdtfeger R., Kolb H.J. Allogeneic stem-cell transplantation provides excellent results in advanced stage chronic myeloid leukemia with major cytogenetic response to pre-transplant imatinib therapy. Leuk Lymphoma 2007, 48:295-301.
147. Kreuzer K.A., Kluhs C., Baskaynak G., Movassaghi K., Dorken B., le Coutre P. Filgrastim-induced stem cell mobilization in chronic myeloid leukaemia patients during imatinib therapy: safety, feasibility and evidence for an efficient in vivo purging. Br J Haematol 2004, 124(January (2)):195-199.
148. Rea D., Raffoux E., Cayuela J.M., Maarek O., Dombret H. Sustained major molecular response in the absence of any antileukaemic therapy after dasatinib treatment and autologous peripheral blood stem cell transplantation in a patient with imatinib-resistant myeloblastic-phase chronic myeloid leukaemia. Leukemia 2009, 23(June (6)):1158-1159.
149. Mughal T.I., Goldman J.M. Emerging strategies for the treatment of mutant Bcr-Abl T315I myeloid leukemia. Clin Lymphoma Myeloma 2007, 7(Suppl. 2):S81-S84.
150. Zhang J., Adrian F.J., Jahnke W., Cowan-Jacob S.W., Li A.G., Iacob R.E., et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature 2010, 463(January (7280)):501-506.