Managing imatinib resistance in chronic myeloid leukaemia

Current Opinion in Hematology

Volumn 17, Issue 2, 2010, Pages 97-103

  Osborn, Michael ^a   Hughes, Timothy ^a,b  

^a Rundle Mall ^*  (Australia)

^b CENTRE FOR CANCER BIOLOGY   (Australia)

Author keywords

Chronic myeloid leukaemia; Dasatinib; Imatinib; Kinase domain mutations; Nilotinib; Tyrosine kinase inhibitor

Indexed keywords

BCR ABL PROTEIN; BOSUTINIB; DASATINIB; IMATINIB; NILOTINIB; TRIACYLGLYCEROL LIPASE;

ALLOGENEIC HEMATOPOIETIC STEM CELL TRANSPLANTATION; ANEMIA; ASTHENIA; BONE MARROW BIOPSY; CANCER RESISTANCE; CANCER SURVIVAL; CHRONIC MYELOID LEUKEMIA; CLINICAL ASSESSMENT; CLINICAL TRIAL; DIARRHEA; DRUG CHOICE; DRUG DOSE ESCALATION; DYSPNEA; FATIGUE; FEVER; GENE MUTATION; HEADACHE; HUMAN; HYPERBILIRUBINEMIA; HYPERGLYCEMIA; HYPOPHOSPHATEMIA; NEUTROPENIA; OVERALL SURVIVAL; PLEURA EFFUSION; PRIORITY JOURNAL; RASH; REVIEW; SIDE EFFECT; THROMBOCYTOPENIA; TREATMENT PLANNING; TRIACYLGLYCEROL LIPASE BLOOD LEVEL;

ANTINEOPLASTIC AGENTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG ADMINISTRATION SCHEDULE; DRUG RESISTANCE, NEOPLASM; HUMANS; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; PIPERAZINES; PYRIMIDINES;

EID: 76749090087     PISSN: 10656251     EISSN: 15317048     Source Type: Journal    
DOI: 10.1097/MOH.0b013e3283366bcb     Document Type: Review

References (62)

1. Chronic Myeloid Leukemia Trialists' Collaborative Group. Interferon alfa versus chemotherapy for chronic myeloid leukaemia: a meta-analysis of seven randomized trials. J Natl Cancer Inst 1997; 89:1616-1620.
2. O'Brien SG, Guilhot F, Goldman JM, et al. International Randomized Study of Interferon Versus STI571 (IRIS) 7-year follow-up: sustained survival, low rate of transformation and increased rate of major molecular response (MMR) in patients (pts) with newly diagnosed chronic myeloid leukemia in chronic phase (CMLCP) treated with imatinib (IM) [abstract #186]. Blood (ASH Annual Meeting abstracts) 2008; 112:76.
3. de Lavallade H, Apperley JF, Khorashad JS, et al. Imatinib for newly diagnosed patients with chronic myeloid leukemia: incidence of sustained responses in an intention-to-treat analysis. J Clin Oncol 2008; 26:3358-3363.
4. Baccarani M, Cortes J, Pane F, et al. Chronic myeloid leukemia: an update of concepts and management recommendations of European LeukemiaNet. J Clin Oncol 2009; 27:6041-6051.
5. Deininger M. Milestones and monitoring in patients with CML treated with imatinib. Haematology 2008; 419-426.
6. Gorre ME, Mohammed M, Ellwood K, et al. Clinical resistance to STI571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science 2001; 293:876-880.
7. Hochhaus A, Kreil S, Corbin AS, et al. Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia 2002; 16:2190-2196.
8. 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; 99:3472-3475.
9. Shah NP, Nicoll JM, 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; 2:117-125.
10. Al-Ali HK, Heinrich MC, Lange T, et al. High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in CML patients with secondary resistance to imatinib. Haematol J 2004; 5:55-60.
11. Soverini S, Colarossi S, Gnani 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.
12. 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; 20:1767-1773. (Pubitemid 44574988)
13. Noens L, van Lierde M, De Bock R, 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.
14. Peng B, Hayes M, Resta D, et al. Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients. J Clin Oncol 2004; 22:935-942.
15. Le Coutre P, Kreuzer KA, Pursche S, et al. Pharmacokinetics and cellular uptake of imatinib and its main metabolite CGP74588. Cancer Chemother Pharmacol 2004; 53:313-323. (Pubitemid 38392356)
16. Cohen MH, Williams G, Johnson JR, et al. Approval summary for imatinib mesylate capsules in the treatment of chronic myelogenous leukemia. Clin Cancer Res 2002; 8:935-942.
17. Picard S, Titier K, Etienne G, 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.
18. Larson RA, Druker BJ, Guilhot FA, 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.
19. Thomas J, Wang L, Clark RE, et al. Active transport of imatinib into and out of cells: implications for drug resistance. Blood 2004; 104:3739-3745.
20. Mahon FX, Belloc F, Lagarde V, et al. MDR1 gene overexpression confers resistance to imatinib mesylate in leukaemia cell line models. Blood 2003; 101:2368-2373.
21. Dulucq S, Bouchet S, Turcq B, et al. Multidrug resistance gene (MDR1) polymorphisms are associated with major molecular responses to standard-dose imatinib in chronic myeloid leukemia. Blood 2008; 112:2024-2027.
22. Nakanishi T, Shiozawa K, Hassel BA, et al. Complex interaction of BCRP/ ABCG2 and imatinib in BCR-ABL expressing cells: BCRP-mediated resistance to imatinib is attenuated by imatinib-induced reduction of BCRP expression. Blood 2006; 108:678-684.
23. White DL, Saunders VA, Dang P, 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.
24. Wang L, Giannoudis A, Lane S, et al. Expression of the uptake drug transporter hOCT1 is an important clinical determinant of the response to imatinib in chronic myeloid leukemia. Clin Pharm Ther 2008; 83:258-264.
25. Crossman LC, Druker BJ, Deininger MWN, et al. hOCT1 and resistance to imatinib. Blood 2005; 106:1133-1134.
26. Marin D, Milojkovic D, Olavarria E, et al. European LeukemiaNet criteria for failure or suboptimal response reliably identify patients with CML in early chronic phase treated with imatinib whose eventual outcome is poor. Blood 2008; 112:4437-4444.
27. Alvarado Y, Kantarjian H, O'Brien S, et al. Significance of suboptimal response to imatinib, as defined by the European LeukemiaNet, in the long-term outcome of patients with early chronic myeloid leukemia in chronic phase. Cancer 2009; 115:3709-3718.
28. Kantarjian H, O'Brien S, Talpaz M, et al. Outcome of patients with Philadelphia chromosome-positive chronic myelogenous leukemia post-imatinib mesylate failure. Cancer 2007; 109:1556-1560.
29. Quintas-Cardama A, Cortes JE, O'Brien S, et al. Dasatinib early intervention after cytogenetic or hematologic resistance to imatinib in patients with chronic myeloid leukemia. Cancer 2009; 115:2912-2921.
30. Ross DM, Branford S, Moore S, et al. Limited clinical value of regular bone marrow cytogenetic analysis in imatinib-treated chronic phase CML patients monitored by RQ-PCR for BCR-ABL. Leukemia 2006; 20:664-670.
31. Hughes T, Deininger M, Hochhaus A, et al. Monitoring CML patients responding to treatment with tyrosine kinase inhibitors: review and recommendations for harmonizing current methodology for detecting BCR-ABL transcripts and kinase domain mutations and for expressing results. Blood 2006; 108:28-37.
32. Branford S, Fletcher L, Cross NCP, et al. Desirable performance characteristics for BCR-ABL measurement on an international reporting scale to allow consistent interpretation of individual patient response and comparison of response rates between clinical trials. Blood 2008; 112:3330-3338.
33. Branford S, Rudzki Z, Parkinson I, et al. Real-time quantitative PCR analysis can be used as a primary screen to identify patients with CML treated with imatinib who have BCR-ABL kinase domain mutations. Blood 2004; 104: 2926-2932.
34. Press RG, Willis SG, Laudadio J, et al. Determining the rise in BCR-ABL RNA that optimally predicts a kinase domain mutation in patients with chronic myeloid leukemia on imatinib. Blood 2009; 114:2598-2605.
35. Druker BJ, Talpaz M, Resta DJ, 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.
36. Zonder JA, Pemberton P, Brandt H, et al. The effect of dose increase to imatinib mesylate in patients with chronic or accelerated phase chronic myeloid leukemia with inadequate hematologic or cytogenetic response to initial treatment. Clin Cancer Res 2002; 9:2092-2097.
37. Kantarjian HM, Talpaz M, O'Brien S, et al. Dose escalation of imatinib mesylate can overcome resistance to standard-dose therapy in patients with chronic myelogenous leukemia. Blood 2003; 101:473-475. (Pubitemid 36077567)
38. Marin D, Goldman JM, Olavarria E, et al. Transient benefit only from increasing the imatinib dose in CML patients who do not achieve cytogenetic remissions on conventional doses. Blood 2003; 102:2702-2703.
39. Kantarjian HM, Larson RA, Guilhot FG, et al. Efficacy of imatinib dose escalation in patients with chronic myeloid leukemia in chronic phase. Cancer 2009; 115:551-560.
40. Jabbour E, Kantarjian HM, Jones D, et al. Imatinib mesylate dose escalation is associated with durable response in patients with chronic myeloid leukemia after cytogenetic failure on standard-dose imatinib therapy. Blood 2009; 113:2154-2160.
41. Kantarjian H, Pasquini R, Levy V, 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.
42. Rea D, Etienne G, Corm S, et al. Imatinib dose escalation for chronic phase: chronic myelogenous leukemia patients in primary suboptimal response to imatinib 400 mg daily standard therapy. Leukemia 2009; 23: 1193-1196.
43. Cortes JE, Kantarjian HM, Goldberg SL, et al. High-dose imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: high rates of rapid cytogenetic and molecular responses. J Clin Oncol 2009; 27:4754-4759.
44. Cortes JE, Baccarani M, Guilhot F, et al. A phase III, randomised, open-label study of 400 versus 800 mg 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 [abstract #335]. Blood (ASH Annual Meeting Abstracts) 2008; 112:130-131.
45. Shah NP, Tran C, Lee FY, et al. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 2004; 305:399-401.
46. Hochhaus A, Kantarjian HM, Baccarani M, 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. (Pubitemid 46425867)
47. 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; 22:1200-1206.
48. Hochhaus A, Muller MC, Radich J, et al. Dasatinib-associated major molecular responses in patients with chronic myeloid leukemia in chronic phase following imatinib failure: response dynamics and predictive value. Leukemia 2009; 23:1628-1633.
49. 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.
50. Kantarjian HM, Giles F, Gattermann N, 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.
51. Nicolini FE, Alimena G, Al-Ali HK, et al. Final safety analysis of 1,793 CML patients from ENACT (Expanding nilotinib access in clinical trials) study in adult patients with imatinib-resistant or-intolerant chronic myeloid leukemia [abstract #0630]. Haematologica 2009; 94 (Suppl 2): 255.
52. Kantarjian HM, Giles F, Bhalla KN, et al. Nilotinib in chronic myeloid leukemia patients in chronic phase (CMLCP) with imatinib resistance or intolerance: 2-year follow-up results of a phase 2 study [abstract #3238]. Blood (ASH Annual Meeting Abstracts) 2008; 112.
53. Jabbour E, Jones D, Kantarjian HM, et al. Long-term outcome of patients with chronic myeloid leukemia treated with second-generation tyrosine kinase inhibitors after imatinib failure is predicted by the in vitro sensitivity of BCR-ABL kinase domain mutations. Blood 2009; 114:2037-2043.
54. Hughes T, Saglio G, Branford S, 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.
55. Muller MC, Cortes JE, Kim DW, et al. Dasatinib treatment of chronic phase chronic myeloid leukemia: analysis of responses according to preexisting BCR-ABL mutations. Blood 2009; 114:4944-4953.
56. Garg RJ, Kantarjian H, O'Brien S, et al. The use of nilotinib or dasatinib after failure to two prior tyrosine kinase inhibitors (TKI): long-term follow-up. Blood 2009; 114:4361-4368.
57. Brummendorf TH, Cervantes F, Kim D, et al. Bosutinib is safe and active in patients (pts) with chronic phase (CP) chronic myeloid leukemia (CML) with resistance or intolerance to imatinib and other tyrosine kinase inhibitors [abstract #7001]. J Clin Oncol (ASCO Annual Meeting Abstracts) 2008; 26:372.
58. Neviani P, Santhanam R, Oaks JJ, et al. FTY720, a new alternative for treating blast crisis chronic myelogenous leukemia and Philadelphia chromosome-positive acute lymphocytic leukemia. J Clin Invest 2007; 117:2408-2421.
59. Legros L, Hayette S, Nicolini FE, et al. BCR-ABL (T315I) transcript disappearance in an imatinib-resistant CML patient treated with homoharringto-nine: a new therapeutic challenge? Leukemia 2007; 21:2204-2206.
60. Deininger M, Schleuning M, Greinix H, et al. The effect of prior exposure to imatinib on transplant-related mortality. Haematologica 2006; 91:452-459.
61. Saussele S, Lauseker M, Gratwohl A, et al. Allogeneic hematopoietic stem cell transplantation (alloSCT) for chronic myeloid leukemia in the imatinib era; evaluation of its impact within a subgroup of the randomized German CML Study IV. Blood 2009; Nov 18 [E-pub ahead of print].
62. Oehler VG, Yeung KY, Choi YE, et al. The derivation of diagnostic markers of chronic myeloid leukemia progression from microarray data. Blood 2009; 114:3292-3298.