The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib

被引:50
作者
Albers, C. [1 ]
Leischner, H. [1 ]
Verbeek, M. [1 ]
Yu, C. [1 ]
Illert, A. L. [2 ]
Peschel, C. [1 ]
von Bubnoff, N. [2 ]
Duyster, J. [2 ]
机构
[1] Tech Univ Munich, Klinikum Rechts Isar, Dept Internal Med 3, D-80290 Munich, Germany
[2] Univ Med Ctr Freiburg, Dept Hematol Oncol, Freiburg, Germany
关键词
ACUTE MYELOID-LEUKEMIA; CLINICAL RESISTANCE; INHIBITORS; SORAFENIB;
D O I
10.1038/leu.2013.14
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
引用
收藏
页码:1416 / 1418
页数:4
相关论文
共 8 条
[1]   Prediction of resistance to small molecule FLT3 inhibitors: Implications for molecularly targeted therapy of acute leukemia [J].
Cools, J ;
Mentens, N ;
Furet, P ;
Fabbro, D ;
Clark, JJ ;
Griffin, JD ;
Marynen, P ;
Gilliland, DG .
CANCER RESEARCH, 2004, 64 (18) :6385-6389
[2]   Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain [J].
Heidel, F ;
Solem, FK ;
Breitenbuecher, F ;
Lipka, DB ;
Kasper, S ;
Thiede, MH ;
Brandts, C ;
Serve, H ;
Roesel, J ;
Giles, F ;
Feldman, E ;
Ehninger, G ;
Schiller, GJ ;
Nimer, S ;
Stone, RM ;
Wang, YF ;
Kindler, T ;
Cohen, PS ;
Huber, C ;
Fischer, T .
BLOOD, 2006, 107 (01) :293-300
[3]   Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations [J].
Kancha, Rama Krishna ;
Grundler, Rebekka ;
Peschel, Christian ;
Duyster, Justus .
EXPERIMENTAL HEMATOLOGY, 2007, 35 (10) :1522-1526
[4]   Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns [J].
Moore, A. S. ;
Faisal, A. ;
de Castro, D. Gonzalez ;
Bavetsias, V. ;
Sun, C. ;
Atrash, B. ;
Valenti, M. ;
Brandon, A. de Haven ;
Avery, S. ;
Mair, D. ;
Mirabella, F. ;
Swansbury, J. ;
Pearson, A. D. J. ;
Workman, P. ;
Blagg, J. ;
Raynaud, F. I. ;
Eccles, S. A. ;
Linardopoulos, S. .
LEUKEMIA, 2012, 26 (07) :1462-1470
[5]   Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia [J].
Smith, Catherine C. ;
Wang, Qi ;
Chin, Chen-Shan ;
Salerno, Sara ;
Damon, Lauren E. ;
Levis, Mark J. ;
Perl, Alexander E. ;
Travers, Kevin J. ;
Wang, Susana ;
Hunt, Jeremy P. ;
Zarrinkar, Patrick P. ;
Schadt, Eric E. ;
Kasarskis, Andrew ;
Kuriyan, John ;
Shah, Neil P. .
NATURE, 2012, 485 (7397) :260-U153
[6]   Identification of a secondary FLT3/A848P mutation in a patient with FLT3-ITD-positive blast phase CMML and response to sunitinib and sorafenib [J].
von Bubnoff, N. ;
Rummelt, C. ;
Menzel, H. ;
Sigl, M. ;
Peschel, C. ;
Duyster, J. .
LEUKEMIA, 2010, 24 (08) :1523-1525
[7]   FMS-Like Tyrosine Kinase 3-Internal Tandem Duplication Tyrosine Kinase Inhibitors Display a Nonoverlapping Profile of Resistance Mutations In vitro [J].
von Bubnoff, Nikolas ;
Engh, Richard A. ;
Aberg, Espen ;
Sanger, Jana ;
Peschel, Christian ;
Duyster, Justus .
CANCER RESEARCH, 2009, 69 (07) :3032-3041
[8]   AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML) [J].
Zarrinkar, Patrick P. ;
Gunawardane, Ruwanthi N. ;
Cramer, Merryl D. ;
Gardner, Michael F. ;
Brigham, Daniel ;
Belli, Barbara ;
Karaman, Mazen W. ;
Pratz, Keith W. ;
Pallares, Gabriel ;
Chao, Qi ;
Sprankle, Kelly G. ;
Patel, Hitesh K. ;
Levis, Mark ;
Armstrong, Robert C. ;
James, Joyce ;
Bhagwat, Shripad S. .
BLOOD, 2009, 114 (14) :2984-2992