AMN107, a novel aminopyrimidine inhibitor of p190 Bcr-Abl activation and of in vitro proliferation of Philadelphia-positive acute lymphoblastic leukemia cells

Cancer

Volumn 104, Issue 6, 2005, Pages 1230-1236

  Verstovsek, Srdan ^a   Golemovic, Mirna ^a   Kantarjian, Hagop ^a   Manshouri, Tashi ^a   Estrov, Zeev ^a   Manley, Paul ^b   Sun, Tong ^a   Arlinghaus, Ralph B ^a   Alland, Leila ^b   Dugan, Margaret ^b   Cortes, Jorge ^a   Giles, Francis ^a   Beran, Miloslav ^a  

^a UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Acute lymphoblastic leukemia; AMN107; Bcr Abl kinase inhibitor; Imatinib; In vitro models

Indexed keywords

AMINOPYRIDINE DERIVATIVE; BENZAMIDE DERIVATIVE; IMATINIB; NILOTINIB; P190 BCR ABL TYROSINE KINASE; PROTEIN INHIBITOR; PROTEIN TYROSINE KINASE; UNCLASSIFIED DRUG;

ACUTE LYMPHOBLASTIC LEUKEMIA; APOPTOSIS; ARTICLE; CANCER CELL CULTURE; CANCER MODEL; CELL PROLIFERATION; CONTROLLED STUDY; DRUG EFFECT; DRUG EFFICACY; DRUG POTENCY; ENZYME PHOSPHORYLATION; GENOTYPE; HUMAN; HUMAN CELL; LEUKEMIA CELL; PHILADELPHIA CHROMOSOME POSITIVE CELL; PRIORITY JOURNAL;

ANTINEOPLASTIC AGENTS; APOPTOSIS; CASPASE 3; CASPASES; CELL CYCLE; CELL LINE, TUMOR; CELL PROLIFERATION; FUSION PROTEINS, BCR-ABL; HUMANS; LEUKEMIA, LYMPHOCYTIC, ACUTE, L2; PHOSPHORYLATION; PIPERAZINES; PYRIMIDINES;

EID: 24644464172     PISSN: 0008543X     EISSN: None     Source Type: Journal    
DOI: 10.1002/cncr.21299     Document Type: Article

References (22)

1. 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. 1996;2:561-566.
2. 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;4:1661-1672.
3. Kantarjian H, Sawyers C, Hochhaus A, et al. International STI571 CML Study Group. Hematological and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia. N Engl J Med. 2002;346:645-652.
4. Kantarjian H, Talpaz M, O'Brien S, et al. High-dose imatinib mesylate therapy in newly diagnosed Philadelphia chromosome-positive chronic phase chronic myeloid leukemia. Blood. 2004;103:2873-2878.
5. Hoelzer D, Gokbuget N, Ottmann OG. Targeted therapies in the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia. Semin Hematol. 2002;39:32-37.
6. Ottman OG, Druker BJ, Sawyers CL, 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.
7. Gorre ME, Mohammed M, Ellwood K, et al. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science. 2001;293:876-880.
8. Corbin AS, La Rosee P, Stoffregen EP, Drucker BJ, Deininger MW. Several Bcr-Abl kinase domain mutants associated with imatinib mesylate resistance remain sensitive to imatinib. Blood. 2003;101:4611-4614.
9. Cowan-Jacob SW, Guez V, Griffin JD, et al. Bcr-Abl kinase mutations and drug resistance to imatinib (STI571) in chronic myelogenous leukemia. Mini Rev Med Chem. 2004;4:285-299.
10. Hochhaus A, Kreil S, Corbin A, et al. Roots of clinical resistance to STI-571 cancer therapy. Science. 2001;293:2163.
11. Ricci C, Scappini B, Divoky V, et al. Mutation in the ATP-binding pocket of the ABL kinase domain in an STI571-resistant BCR/ABL-positive cell line. Cancer Res. 2002;62:5995-5998.
12. 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. 2000;95:1758-1766.
13. Mahon FX, Deininger MB, Schultheis B, Chabrol Reiffers J, Goldman JM, Melo JV. Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: diverse mechanisms of resistance. Blood. 2000;96:1070-1079.
14. Scappini B, Gatto S, Onida F, et al. Changes associated with the development of resistance to imatinib (STI571) in two leukemia cell lines expressing p210 Bcr/Abl protein. Cancer. 2004;100:1459-1471.
15. Weisberg E, Griffin JD. Resistance to imatinib (Glivec): update on clinical mechanisms. Drug Resist Updat. 2003;6:231-238.
16. Nardi V, Azam M, Daley GQ. Mechanisms and implications of imatinib resistance mutations in BCR-ABL. Curr Opin Hematol. 2004;11:35-43.
17. Shah NP, Tran C, Lee FY, Chen P, Norris D, Sawyers DL. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science. 2004;305:399-401.
18. Weisberg E, Manley P, Breitenstein W, et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell. 2005;7:129-141.
19. Golemovic M, Verstovsek S, Giles F, et al. AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia. Clin Cancer Res. 2005;11:4941-4947.
20. 1-positive cell lines (Z-119 and Z-181). J Cell Physiol. 1996;166:618-630.
21. Beran M, Pisa P, O'Brien S, et al. Biological properties and growth in SCID mice of a new myelogenous leukemia cell line (KBM-5) derived from chronic myelogenous leukemia cells in the blastic phase. Cancer Res. 1993;53:3603-3610.
22. Giles F, Kantarjian H, Wassmann B, et al. A phase I/II study of AMN107, a novel aminopyrimidine inhibitor of Bcr/Abl, on a continuous daily dosing schedule in adult patients (pts) with imatinib-resistant advanced phase chronic myeloid leukemia (CML) or relapsed/refractory Philadelphia chromosome (Ph+) acute lymphocytic leukemia (ALL) [abstract]. Blood. 2004;104:10a-11a.