Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants

Journal of Clinical Oncology

Volumn 27, Issue 3, 2009, Pages 469-471

  Redaelli, Sara ^a   Piazza, Rocco ^a   Rostagno, Roberta ^a   Magistroni, Vera ^a   Perini, Pietro ^a   Marega, Manuela ^a   Gambacorti Passerini, Carlo ^a   Boschelli, Frank ^b  

^a SAN GERARDO HOSPITAL   (Italy)

^b PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

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

ANTINEOPLASTIC ACTIVITY; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; DRUG BIOAVAILABILITY; DRUG EFFICACY; HUMAN; LETTER; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; PROTEIN EXPRESSION;

ANILINE COMPOUNDS; ANTINEOPLASTIC AGENTS; DRUG RESISTANCE, NEOPLASM; GENES, ABL; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; MUTATION; NITRILES; PHILADELPHIA CHROMOSOME; PIPERAZINES; PRECURSOR CELL LYMPHOBLASTIC LEUKEMIA-LYMPHOMA; PROTEIN KINASE INHIBITORS; PYRIMIDINES; QUINOLINES; THIAZOLES;

EID: 58549088155     PISSN: 0732183X     EISSN: None     Source Type: Journal    
DOI: 10.1200/JCO.2008.19.8853     Document Type: Letter

References (23)

1. Kantarjian H, Sawyers C, Hochhaus A, et al: Hematologic and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia. N Engl J Med 346:645-652, 2002
2. Druker BJ, Guilhot F, O'Brien SG, et al: Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia. N Engl J Med 355:2408-2417, 2006
3. Hochhaus A, Druker B, Sawyers C, et al: Favorable long-term follow-up results over 6 years for response, survival, and safety with imatinib mesylate therapy in chronic-phase chronic myeloid leukemia after failure of interferon-alpha treatment. Blood 111:1039-1043, 2008
4. Schindler T, Bornmann W, Pellicena P, et al: Structural mechanism for STI-571 inhibition of abelson tyrosine kinase. Science 289:1938-1942, 2000
5. Gambacorti-Passerini C, Gunby R, Piazza R, et al: Molecular mechanisms of resistance to imatinib in Philadelphia-chromosome-positive leukaemias. Lancet Oncol 4:75-85, 2003
6. le Coutre P, Tassi E, Varella-Garcia M, et al: Induction of resistance to the Abelson inhibitor STI571 in human leukemic cells through gene amplification. Blood 95:1758-1766, 2000
7. 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 110:4064-4072, 2007
8. Apperley J: Part I: Mechanisms of resistance to imatinib in chronic myeloid leukaemia. Lancet Oncol 8:1018-1029, 2007
9. Weisberg E, Manley P, Breitenstein W, et al: Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell 7:129-141, 2005
10. Shah N, Tran C, Lee F, et al: Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 305:399-401, 2004
11. Tokarski J, Newitt J, Chang C, 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 66:5790-5797, 2006
12. Golas J, Arndt K, Etienne C, et al: SKI-606, a 4-anilino-3- quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiprolif-erative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res 63:375-381, 2003
13. Puttini M, Coluccia A, 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 66:11314-11322, 2006
14. Redaelli S, Boschelli F, Viltadi M, et al: Synergistic activity of the novel Src/Abl inhibitor bosutinib in combination with imatinib. Blood 110:2930, 2007
15. Cortes J, Bruemmendorf T, Kantarjian H, et al: Efficacy and safety of bosutinib (SKI-606) among patients with chronic phase Ph+ chronic myeloge- nous leukemia (CML). Blood 110:733, 2007
16. Gambacorti-Passerini C, Kantarjian H, Bruemmendorf T, et al: Bosutinib (SKI-606) demonstrates clinical activity and is well tolerated among patients with AP and BP CML and Ph+ ALL. Blood 110:473, 2007
17. Bruemmendorf 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. J Clin Oncol 26:372s, 2008 (suppl; abstr 7001)
18. Konig H, Holyoake TL, Bhatia R: Effective and selective inhibition of chronic myeloid leukemia primitive hematopoietic progenitors by the dual Src/Abl kinase inhibitor SKI-606. Blood 111:2329-2338, 2008
19. 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 109:2303-2309, 2007
20. 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 110:3540-3546, 2007
21. Azam M, Latek RR, Daley GQ: Mechanisms of autoinhibition and STI-571/ imatinib resistance revealed by mutagenesis of BCR-ABL. Cell 112:831-843, 2003
22. Quintas-Cardama A, Cortes J: Tailoring tyrosine kinase inhibitor therapy to tackle specific BCR-ABL1 mutant clones. Leuk Res 2008
23. Quintas-Cardama A, Kantarjian H, Jones D, et al: Dasatinib (BMS-354825) is active in Philadelphia chromosome-positive chronic myelogenous leukemia after imatinib and nilotinib (AMN107) therapy failure. Blood 109:497-499, 2007