STI571: An inhibitor of the BCR-ABL tyrosine kinase for the treatment of chronic myelogenous leukaemia

Lancet Oncology

Volumn 1, Issue 4, 2000, Pages 207-211

  O'Dwyer, Michael E ^a   Druker, Brian J ^a  

^a OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; BCR ABL PROTEIN; BCR ABL TYROSINE KINASE; BCR-ABL TYROSINE KINASE; ENZYME INHIBITOR; IMATINIB; PIPERAZINE DERIVATIVE; PROTEIN TYROSINE KINASE; PYRIMIDINE DERIVATIVE;

ANIMAL; CHRONIC MYELOID LEUKEMIA; DISEASE MODEL; DRUG ANTAGONISM; DRUG EFFECT; HUMAN; METABOLISM; PHASE 1 CLINICAL TRIAL; REVIEW; SENSITIVITY AND SPECIFICITY;

ANIMALS; ANTINEOPLASTIC AGENTS; CLINICAL TRIALS, PHASE I; DISEASE MODELS, ANIMAL; ENZYME INHIBITORS; FUSION PROTEINS, BCR-ABL; HUMANS; LEUKEMIA, MYELOID, CHRONIC; PIPERAZINES; PROTEIN-TYROSINE KINASES; PYRIMIDINES; SENSITIVITY AND SPECIFICITY;

EID: 0034584880     PISSN: 14702045     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1470-2045(00)00149-2     Document Type: Review

References (34)

1. Sawyers CL. Chronic myeloid leukemia. N Engl J Med. 340:1999;1330-1340.
2. Chronic Myeloid Leukemia Trialists' Collaborative Group. Interferon alfa versus chemotherapy for chronic myeloid leukemia: a meta-analysis of seven randomized trials. J Natl Cancer Inst 1997; 89: 1616-20.
3. Silver RT, Woolf SH, Hehlmann R, 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. 94:1999;1517-1536.
4. Nowell PC, Hungerford DA. A minute chromosome in human chronic granulocytic leukemia. Science. 132:1960;1497-1501.
5. Rowley JD. A new consistent chromosomal abnormality in chronic myelogenous leukaemia identified by quinacrine fluorescence and Giemsa staining. Nature. 243:1973;290-293.
6. de Klein A, van Kessel AG, Grosveld G, et al. A cellular oncogene is translocated to the Philadelphia chromosome in chronic myelocytic leukaemia. Nature. 300:1982;765-767.
7. Heisterkamp N, Stam K, Groffen J, de Klein A, Grosveld G. Structural organization of the bcr gene and its role in the Ph' translocation. Nature. 315:1985;758-761.
8. Shtivelman E, Lifshitz B, Gale RP, Canaani E. Fused transcript of abl and bcr genes in chronic myelogenous leukaemia. Nature. 315:1985;550-554.
9. Clark SS, McLaughlin J, Timmons M, et al. Expression of a distinctive BCR-ABL oncogene in Ph1-positive acute lymphocytic leukemia (ALL). Science. 239:1988;775-777.
10. Witte ON, Dasgupta A, Baltimore D. Abelson murine leukaemia virus protein is phosphorylated in vitro to form phosphotyrosine. Nature. 283:1980;826-831.
11. Witte ON, Goff S, Rosenberg N, Baltimore D. A transformation-defective mutant of Abelson murine leukemia virus lacks protein kinase activity. Proc Natl Acad Sci USA. 77:1980;4993-4997.
12. Lugo TG, Pendergast AM, Muller AJ, Witte ON. Tyrosine kinase activity and transformation potency of bcr-abl oncogene products. Science. 247:1990;1079-1082.
13. Daley GQ, Van Etten RA, Baltimore D. Induction of chronic myelogenous leukemia in mice by the P210bcr/abl gene of the Philadelphia chromosome. Science. 247:1990;824-830.
14. Heisterkamp N, Jenster G, ten Hoeve J, et al. Acute leukaemia in bcr/abl transgenic mice. Nature. 344:1990;251-253.
15. Faderl S, Talpaz M, Estrov Z, et al. The biology of chronic myeloid leukemia. N Engl J Med. 341:1999;164-172.
16. Sawyers CL, McLaughlin J, Witte ON. Genetic requirement for Ras in the transformation of fibroblasts and hematopoietic cells by the Bcr-Abl oncogene. J Exp Med. 181:1995;307-313.
17. Neshat MS, Raitano AB, Wang HG, Reed JC, Sawyers CL. The survival function of the Bcr-Abl oncogene is mediated by Bad- dependent and-independent pathways: roles for phosphatidylinositol 3-kinase and Raf. Mol Cell Biol. 20:2000;1179-1186.
18. Horita M, Andreu EJ, Benito A, et al. Blockade of the Bcr-Abl kinase activity induces apoptosis of chronic myelogenous leukemia cells by suppressing signal transducer and activator of transcription 5-dependent expression of Bcl-xL. J Exp Med. 191:2000;977-984.
19. Verfaillie CM. Biology of chronic myelogenous leukemia. Hematol Oncol Clin North Am. 12:1998;1-29.
20. Yaish P, Gazit A, Gilon C, Levitzki A. Blocking of EGF-dependent cell proliferation by EGF receptor kinase inhibitors. Science. 242:1988;933-935.
21. Druker BJ, Lydon NB. Lessons learned from the development of an abl tyrosine kinase inhibitor for chronic myelogenous leukemia. J Clin Invest. 105:2000;3-7.
22. Druker BJ, 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. 2:1996;561-566.
23. Deininger MW, Goldman JM, Lydon N, Melo JV. The tyrosine kinase inhibitor CGP57148B selectivelyinhibits the growth of BCR-ABL-positive cells. Blood. 90:1997;3691-3698.
24. Kasper B, Fruehauf S, Schiedlmeier B, Buchdunger E, Ho AD, Zeller WJ. Favorable therapeutic index of a p210(BCR-ABL)-specific tyrosine kinase inhibitor; activity on lineage-committed and primitive chronic myelogenous leukemia progenitors. Cancer Chemother Pharmacol. 44:1999;433-438.
25. Carroll M, Ohno-Jones S, Tamura S, et al. CGP 57148, a tyrosine kinase inhibitor, inhibits the growth of cells expressing BCR-ABL, TEL-ABL, and TEL-PDGFR fusion proteins. Blood. 90:1997;4947-4952.
26. 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. 4:1998;1661-1672.
27. le Coutre P, Mologni L, Cleris L, et al. In vivo eradication of human BCR/ABL-positive leukemia cells with an ABL kinase inhibitor. J Natl Cancer Inst. 91:1999;163-168.
28. Druker BJ, Talpaz M, Resta D, et al. Clinical efficacy and safety of an ABL specific tyrosine kinase inhibitor as targeted therapy for chronic myelogenous leukemia. Blood 1999; 94: 697a (abstr).
29. Talpaz M, Sawyers C L, Kantarjian H, et al. Activity of an Abl specific tyrosine kinase inhibitor in patients with Bcr-Abl positive acute leukemias, including chronic myelogenous leukemia in blast crisis. Proc ASCO 2000; 19: 4a (abstr).
30. Mahon FX, Deininger MW, Schultheis B, et al. Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: diverse mechanisms of resistance. Blood. 96:2000;1070-1079.
31. le Coutre P, Tassi E, Varella-Garcia M, et al. Inductionof resistance to the Abelson inhibitor STI571 in human leukemic cells through gene amplification. Blood. 95:2000;1758-1766.
32. Weisberg E, Griffin JD. Mechanism of resistance to the ABL tyrosine kinase inhibitor STI571 in BCR/ABL-transformed hematopoietic cell lines. Blood. 95:2000;3498-3505.
33. Thiesing JT, Ohno-Jones S, Kolibaba KS, Druker BJ. Efficacy of STI571, an ABL tyrosine kinase inhibitor in conjunction with other anti-leukemic agents against BCR-ABL positive cells. Blood. 96:2000;3195-3199.
34. Fang G, Kim CN, Perkins CL, et al. CGP57148B (STI-571) induces differentiation and apoptosis and sensitizes Bcr-Abl-positive human leukemia cells to apoptosis due to antileukemic drugs. Blood. 96:2000;2246-2253.