© 1999 by Oxford University Press
Journal of the National Cancer Institute, Vol. 91, No. 2, 163-168,
January 20, 1999
© 1999 Oxford University Press
REPORTS |
In Vivo Eradication of Human BCR/ABL-Positive Leukemia Cells With an ABL Kinase Inhibitor
Affiliations of authors: P. le Coutre, L. Mologni, L.Cleris, E. Marchesi, F. Formelli (Department of Experimental Oncology), R. Giardini (Department of Pathology), Istituto Nazionale Tumori, Milan, Italy; E. Buchdunger, Oncology Research Department, Novartis International Inc., Basel, Switzerland; C. Gambacorti-Passerini, Department of Experimental Oncology, Istituto Nazionale Tumori, Milan, and Section of Hematology, University of Milan, S. Gerardo Hospital, Monza, Italy.
Correspondence to: Carlo Gambacorti-Passerini, M.D.,Department of Experimental Oncology, Istituto Nazionale Tumori, Via Venezian 1, 20133 Milan, Italy (e-mail: gambacorti{at}istitutotumori.mi.it).
BACKGROUND: The leukemia cells of approximately 95% of patients with chronic myeloid leukemia and 30%-50% of adult patients with acute lymphoblastic leukemia express the Bcr/Abl oncoprotein, which is the product of a fusion gene created by a chromosomal translocation [(9:22) (q34;q11)]. This oncoprotein expresses a constitutive tyrosine kinase activity that is crucial for its cellular transforming activity. In this study, we evaluated the antineoplastic activity of CGP57148B, which is a competitive inhibitor of the Bcr/Abl tyrosine kinase. METHODS: Nude mice were given an injection of the Bcr/Abl-positive human leukemia cell lines KU812 or MC3. Tumor-bearing mice were treated intraperitoneally or orally with CGP57148B according to three different schedules. In vitro drug wash-out experiments and in vivo molecular pharmacokinetic experiments were performed to optimize the in vivo treatment schedule. RESULTS: Treatment schedules administering CGP57148B once or twice per day produced some inhibition of tumor growth, but no tumor-bearing mouse was cured. A single administration of CGP57148B caused substantial (>50%) but short-lived (2-5 hours) inhibition of Bcr/Abl kinase activity. On the basis of the results from in vitro wash-out experiments, 20-21 hours was defined as the duration of continuous exposure needed to block cell proliferation and to induce apoptosis in these two leukemia cell lines. A treatment regimen assuring the continuous block of the Bcr/Abl phosphorylating activity that was administered over an 11-day period cured 87%-100% of treated mice. CONCLUSION: These data indicate that the continuous block of the oncogenic tyrosine kinase of Bcr/Abl protein is needed to produce important biologic effects in vivo.
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|
|
|
 |
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
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|
|
|
|
 |
|
 Y. A. Elsayed and E. A. Sausville Selected Novel Anticancer Treatments Targeting Cell Signaling Proteins Oncologist, December 1, 2001; 6(6): 517 - 537. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
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|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
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|
|
|
|
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|
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|
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|
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|
|
|
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|
 |
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|
 S. Faderl, M. Talpaz, Z. Estrov, and H. M. Kantarjian Chronic Myelogenous Leukemia: Biology and Therapy Ann Intern Med, August 3, 1999; 131(3): 207 - 219. [Abstract] [Full Text] [PDF]
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E. A. Sausville A Bcr/Abl Kinase Antagonist for Chronic Myelogenous Leukemia: a Promising Path for Progress Emerges J Natl Cancer Inst, January 20, 1999; 91(2): 102 - 103. [Full Text] [PDF]
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