Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

By E. Weisberg, P. Manley, W. Breitenstein, J. Brüggen, S. Cowan-Jacob, A. Ray, B. Huntly, D. Fabbro, G. Fendrich, Elizabeth Hall-Meyers and 11 more. Cancer Cell, 2005

1,536 citations recorded by the source corpus.

Subfields: Genetics, Hematology, Public Health, Environmental and Occupational Health

View Paper: https://www.semanticscholar.org/paper/be3326b8a09fea4696d0827e5f4a1e2ad8afec8a

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In Genetics

1. Brian J. Druker
2. Zhesheng Chen
3. C. Ashby
4. J. Cortes
5. Andreas Hochhaus
6. H. Kantarjian
7. M. Baccarani

In Hematology

1. Brian J. Druker
2. J. Cortes
3. J. Goldman
4. C. Ashby
5. Zhesheng Chen
6. J. Apperley
7. Andreas Hochhaus
8. H. Kantarjian

Citations in the corpus

• AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. (2009, background): “…by minimizing BCR-ABL kinase domain mutation-based drug resistance. ancer Cell 16, 401–412, November 3, 2009 ª2009 Elsevier Inc. 401 imatinib family member nilotinib (Tasigna; AMN107) and the multitargeted kinase inhibitor dasatinib (Sprycel; BMS-354825) (Shah et al., 2004; Weisberg et al., 2005).”
• Chronic myeloid leukemia: an update of concepts and management recommendations of European LeukemiaNet. (2009, background): “The data are taken from 10 reports.(16,17,67-74)It is relevant to remember the plasma concentration of the drugs as follows: imatinib 400 mg once daily minimum plasma concentration mean and standard deviation, 978 530 ng/mL(75) and maximum plasma concentration range, 2,000 to 2,500 ng/mL(76,77); ima”
• 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. (2007, background): “Median duration of disease, mo (range) 57 (5-275)”
• BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review. (2010, background): “In addition, nilotinib s effective against 32 out of 33 imatinib-resistant point mutants, ut had no significant activity against T315I mutants [23,43].”
• Dasatinib induces notable hematologic and cytogenetic responses in chronic-phase chronic myeloid leukemia after failure of imatinib therapy. (2007, neutral): “Median age, y (range) 59 (24-79) 59 (24-79) 59 (24-79)”
• Human chronic myeloid leukemia stem cells are insensitive to imatinib despite inhibition of BCR-ABL activity. (2011, background): “Introduction Chronic myeloid leukemia (CML) originates in a HSC with the reciprocal translocation t(9;22) (1).”
• Kinase-targeted cancer therapies: progress, challenges and future directions (2018, background): “A first approach is to develop inhibitors that can tolerate diverse amino acids at the gatekeeper position [289, 290].”