Imatinib mesylate - A new oral targeted therapy

New England Journal of Medicine

Volumn 346, Issue 9, 2002, Pages 683-693

  Savage, David G ^a   Antman, Karen H ^a  

^a Columbia Univ Coll of Phys/Surg ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALPHA INTERFERON; BCR ABL PROTEIN; CYTARABINE; HYDROXYUREA; IMATINIB; PROTEIN TYROSINE KINASE INHIBITOR;

ARTHRALGIA; BLOOD TOXICITY; BONE MARROW SUPPRESSION; CANCER SURVIVAL; CHRONIC MYELOID LEUKEMIA; CLINICAL FEATURE; CLINICAL TRIAL; CYTOGENETICS; DIARRHEA; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG COST; DRUG INDICATION; DRUG POTENCY; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; EDEMA; ENZYME INHIBITION; FATIGUE; GASTROINTESTINAL TUMOR; HEADACHE; HUMAN; LEUKOCYTE COUNT; MUSCLE CRAMP; NAUSEA; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PHILADELPHIA 1 CHROMOSOME; PRIORITY JOURNAL; RASH; REVIEW; SOLID TUMOR; STEM CELL TRANSPLANTATION; THROMBOCYTE COUNT; TREATMENT OUTCOME; VOMITING;

ADMINISTRATION, ORAL; ANTINEOPLASTIC AGENTS; CLINICAL TRIALS; DRUG RESISTANCE; GASTROINTESTINAL NEOPLASMS; HUMANS; HYDROXYUREA; INTERFERON-ALPHA; LEUKEMIA, LYMPHOCYTIC, ACUTE, L1; LEUKEMIA, MYELOID, CHRONIC; LEUKEMIA, MYELOID, PHILADELPHIA-POSITIVE; PIPERAZINES; PYRIMIDINES; RECEPTORS, PLATELET-DERIVED GROWTH FACTOR; SARCOMA;

EID: 0037186924     PISSN: 00284793     EISSN: None     Source Type: Journal    
DOI: 10.1056/NEJMra013339     Document Type: Review

References (118)

1. Targeting the BCR-ABL tyrosine kinase in chronic myeloid leukemia
2. Protein tyrosine kinase and cancer
3. Lessons learned from the development of an abl tyrosine kinase inhibitor for chronic myelogenous leukemia
4. The biology of chronic myeloid leukemia
5. Chronic myeloid leukemia
6. Tyrosine kinase inhibitors in chronic myeloid leukemia
7. The molecular biology of chronic myeloid leukemia
8. Tyrosine-kinase inhibition in treatment of chronic myeloid leukemia
9. Recent advances in the molecular and cellular biology of chronic myeloid leukaemia: Lessons to be learned from the laboratory
10. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia
11. Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome
12. Effect of the tyrosine kinase inhibitor STI571 in a patient with a metastatic gastrointestinal stromal tumor
13. Evaluation of the safety and efficacy of oral molecularly-targeted therapy, STI571, in patients (Pts) with unresectable or metastatic gastrointestinal stromal tumors (GISTs) expressing c kit (CD117)
14. Safety and efficacy of imatinib (STI571) in metastatic gastrointestinal stromal tumours: A phase I study
15. Clinical features at diagnosis in 430 patients with chronic myeloid leukaemia seen at a referral centre over a 16-year period
16. Chronic myelogenous leukemia
17. Novel therapies for chronic myelogenous leukemia
18. Chronic myelogenous leukaemia
19. A minute chromosome in human chronic granulocytic leukemia
20. A new consistent chromosomal abnormality in chronic myelogenous leukaemia identified by quinacrine fluorescence and Giemsa staining
21. Translocation of c-abl oncogene correlates with the presence of a Philadelphia chromosome in chronic myelocytic leukaemia
22. Localization of the c-abl oncogene adjacent to a translocation break point in chronic myelocytic leukaemia
23. Philadelphia chromosomal breakpoints are clustered within a limited region, bcr, on chromosome 22
24. Fused transcript of abl and bcr genes in chronic myelogenous leukaemia
25. Tyrosine kinase activity and transformation potency of bcr-abl oncogene products
26. Induction of chronic myelogenous leukemia in mice by the P210bcr/abl gene of the philadelphia chromosome
27. Blast crisis in a murine model of chronic myelogenous leukemia
28. Clinical significance of the BCR-ABL fusion gene in adult acute lymphoblastic leukemia: A Cancer and Leukemia Group B study (8762)
29. The biology and treatment of acute lymphoblastic leukemia in adults
30. Outcome of treatment in children with Philadelphia chromosome-positive acute lymphoblastic leukemia
31. BCR/ABL P210 and P190 cause distinct leukemia in transgenic mice
32. BCR-ABL tyrosine kinase activity regulates the expression of multiple genes implicated in the pathogenesis of chronic myeloid leukemia
33. BCR-ABL-induced oncogenesis is mediated by direct interaction with the SH2 domain of the GRB-2 adaptor protein
34. Role of p21 RAS in p210 bcr-abl transformation of murine myeloid cells
35. Bcr-Abl oncoproteins bind directly to activators of the Ras signalling pathway
36. p62(Dok): A constitutively tyrosine-phosphorylated, GAP-associated protein in chronic myelogenous leukemia progenitor cells
37. Identification of the Abl- and rasGAP-associated 62 kDa protein as a docking protein, Dok
38. Altered adhesive interactions with marrow stroma of haematopoietic progenitor cells in chronic myeloid leukaemia
39. Interferon-alpha overrides the deficient adhesion of chronic myeloid leukemia primitive progenitor cells to bone marrow stromal cells
40. Signal transduction by wild-type and leukemogenic Abl proteins
41. Inhibition of BCR-ABL expression with antisense oligodeoxynucleotides restores beta1 integrin-mediated adhesion and proliferation inhibition in chronic myelogenous leukemia hematopoietic progenitors
42. Discordant maturation as the primary biological defect in chronic myelogenous leukemia
43. Factor independence of human myeloid leukemia cell lines is associated with increased phosphorylation of the proto-oncogene Raf-1
44. Inhibition of apoptosis by BCR-ABL in chronic myeloid leukemia
45. Structural and signaling requirements for BCR-ABL-mediated transformation and inhibition of apoptosis
46. Induction of apoptosis in chronic myelogenous leukemia cells through nuclear entrapment of BCR-ABL tyrosine kinase
47. Clonal evolution in a myeloid cell line transformed to interleukin-3 independent growth by retroviral transduction and expression of p210bcr/abl
48. Blocking of EGF-dependent cell proliferation by EGF receptor kinase inhibitors
49. Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors
50. Inbibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor
51. Intracranial inhibition of platelet-derived growth factor-mediated glioblastoma cell growth by an orally active kinase inhibitor of the 2-phenylaminopyrintidine class
52. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells
53. 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)
54. CGP 57148, a tyrosine kinase inhibitor, inhibits the growth of cells expressing BCR-ABL, TEL-ABL, and TEL-PDGFR fusion proteins
55. The tyrosine kinase inhibitor CGP57148B selectively inhibits the growth of BCR-ABL-positive cells
56. Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative
57. In vivo eradication of human BCR/ABL-positive leukemia cells with an ABL kinase inhibitor
58. Interferon-alpha before allogeneic bone marrow transplantation in chronic myelogenous leukemia does not affect outcome adversely, provided it is discontinued at least 90 days before the procedure
59. Busulfan versus hydroxyurea in long-term therapy of chronic myelogenous leukemia
60. Randomized comparison of busulfan and hydroxyurea in chronic myelogenous leukemia: Prolongation of survival by hydroxyurea
61. Leukocyte interferon-induced myeloid cytoreduction in chronic myelogenous leukemia
62. A in chronic myelogenous leukemia
63. Prolonged survival in chronic myelogenous leukemia after cytogenetic response to interferon alpha therapy
64. Impact of Interferon alpha-induced cytogenetic improvement on survival in chronic myelogenous leukaemia
65. A randomized trial comparing interferon-alpha with busulfan for newly diagnosed chronic myelogenous leukemia in chronic phase
66. Prolonged subcutaneous administration of recombinant alpha 2b interferon in patients with previously untreated Philadelphia chromosome-positive chronic-phase chronic myelogenous leukemia: Effect on remission duration and survival: Cancer and Leukemia Group B study 8583
67. UK Medical Research Council randomised, multicentre trial of interferon-alpha n1 for chronic myeloid leukaemia: Improved survival irrespective of cytogenetic response leukemia: Improved survival irrespective of cytogenetic response
68. Interferon alfa-2a as compared with conventional chemotherapy for the treatment of chronic myeloid leukemia
69. Interferon alfa versus chemotherapy for chronic myeloid leukemia: A meta-analysis of seven-randomized trials
70. Chronic myeloid leukemia: Current treatment options
71. Interferon-alfa based treatment of chronic myeloid leukemia and implications of signal transduction inhibition
72. Interferon alfa-2b combined with cytarabine versus interferon alone in chronic myelogenous leu kemia
73. Relation of "lymphoid" phenotype and response to chemotherapy incorporating vincristine-prednisolone in the acute phase of Ph1 positive leukemia
74. Therapy of lymphoid and undifferentiated chronic myelogenous leukemia in blast crisis with continuous vincristine and adriamycin infusions plus high-dose decadron
75. Intensive chemotherapy induction followed by interferon-alpha maintenance in patients with Philadelphia chromosome-positive chronic myelogenous leukemia
76. Chronic myelogenous leukemia in nonlymphoid blastic phase: Analysis of the results of first salvage therapy with three different treatment approaches for 162 patients
77. Treatment of chronic granulocytic leukaemia in chronic phase by allogeneic marrow transplantation
78. Marrow transplantation for patients in the chronic phase of chronic granulocytic leukaemia
79. Allografting for chronic myeloid leukaemia
80. Allogeneic bone marrow transplantation for CML: A report from the international Bone Marrow Transplant Registry
81. Long-term results after allogeneic bone marrow transplantation for chronic myelogenous leukemia in chronic phase: A report from the Chronic Leukemia Working Party of the European Group for Blood and Marrow Transplantation
82. Choice of pretransplant treatment and timing of transplants for chronic myelogenous leukemia in chronic phase
83. Risk assessment for patients with chronic myeloid leukaemia before allogeneic blood or marrow transplantation
84. Results of allogeneic bone marrow transplants for leukemia using donors other than HLA-identical siblings
85. Bone marrow transplants from unrelated donors for patients with chronic myeloid leukemia
86. Hematologic and cyrogenetic responses to imatinib mesylate in chronic myelogenous leukemia
87. Gleevec (formerly STI571): An active drug in patients with Ph+ chronic myeloid leukemia in accelerated phase - Updated results of a phase II study
88. Gleevec/Glivec (imatinib mesylate, STI-571) in patients with chronic myeloid leukemia (CML) in myeloid blast crisis: Updated results of a phase II study
89. Acute generalized exanthematous pustulosis associated with STI571 in a patient with chronic myeloid leukemia
90. Adverse events after imatinib mesylate therapy
91. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification
92. Induction of resistance to the Abelson inhibitor STI571 in human leukemic cells through gene amplification
93. Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: Diverse mechanisms of resistance
94. Mechanism of resistance to the ABL tyrosine kinase inhibitor STI571 in BCR/ABL-transformed hematopoietic cell lines
95. Role of alpha1 acid glycoprotein in the in vivo resistance of human BCR-ABL(+) leukemic cells to the abl inhibitor STI571
96. Sensitivity to the abl inhibitor STI571 in flesh leukaemic cells obtained from chronic myelongenous leukaemia patients in different stages of disease
97. Molecular studies in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors
98. Efficacy of STI571, an abl tyrosine kinase inhibitor, in conjunction with other antileukemic agents against bcr-abl-positive cells
99. CGPS7148B (STI-571) induces differentiation and apoptosis and sensitizes Bcr-Abl-positive human leukemia cells to apoptosis due to antileukemic drugs
100. Prolonged administration of interferon-alpha in patients with chronic-phase Philadelphia chromosome-positive chronic myelogenous leukemia before allogeneic bone marrow transplantation may adversely affect transplant outcome
101. Association between pretransplant interferon-alpha and outcome after unrelated donor marrow transplantation for chronic myelogenous leukemia in chronic phase
102. Treatment of Bcr/Abl-positive acute lymphoblastic leukemia in P190 transgenic mice with the farnesyl transferase inhibitor SCH66336
103. Results of imatinib mesylate (STI571) therapy in patients (pts) with chronic myelogenous leukemia (CML) in relapse after allogeneic stem cell transplantation (allo SCT)
104. Gastrointestinal stromal tumors/smooth muscle tumors (GISTs) primary in the omentum and mesentery: Clinicopathologic and immunohistochemical study of 26 cases
105. Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors
106. Gastrointestinal stromal tumors: Recent advances in understanding of their biology
107. Prognosis of gastrointestinal smooth-muscle (stromal) tumors: Dependence on anatomic site
108. The selective tyrosine kinase inhibitor STI571 inhibits small cell lung cancer growth
109. Expression of stem cell factor and c-kit in human neuroblastoma
110. Paraffin section deletion of the c-kit gene product (CD117) in human tissues: Value in the diagnosis of mast cell disorders
111. Lack of expression of c-KIT in ovarian cancers is associated with poor prognosis
112. Growth inhibition and modulation of kinase pathways of small cell lung cancer cell lines by the novel tyrosine kinase inhibitor STI 571
113. Expression of platelet-derived growth factor (PDGF)-A, PDFG-B and the PDGF-alpha receptor, but not the PDGF-beta receptor, in human malignant melanoma in vivo
114. Growth-inhibitory effect of STI571 on cells transformed by the COL1A1/PDGFB rearrangement
115. Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class
116. Blockade of PDGF-R signaling by STI571 inhibits angiogenesis and growth of human prostate cancer cells in the bone of nude mice
117. Inhibition of platelet-derived growth factor receptors reduces interstitial hypertension and increases transcapillary transport in tumors
118. Chronic myeloproliferative diseases with t(5;12) and a PDGFRB fusion gene: Complete cytogenetic remissions on STI571