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FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML.

Pratz KW, Sato T, Murphy KM, Stine A, Rajkhowa T, Levis M.

Blood. 2010 Feb 18;115(7):1425-32. doi: 10.1182/blood-2009-09-242859. Epub 2009 Dec 10.


Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations.

Kancha RK, Grundler R, Peschel C, Duyster J.

Exp Hematol. 2007 Oct;35(10):1522-6.


Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns.

Moore AS, Faisal A, Gonzalez de Castro D, Bavetsias V, Sun C, Atrash B, Valenti M, de Haven Brandon A, Avery S, Mair D, Mirabella F, Swansbury J, Pearson AD, Workman P, Blagg J, Raynaud FI, Eccles SA, Linardopoulos S.

Leukemia. 2012 Jul;26(7):1462-70. doi: 10.1038/leu.2012.52. Epub 2012 Feb 22.


FLT3 inhibition as therapy in acute myeloid leukemia: a record of trials and tribulations.

Fathi AT, Chabner BA.

Oncologist. 2011;16(8):1162-74. doi: 10.1634/theoncologist.2011-0084. Epub 2011 Jul 17.


AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q, Sprankle KG, Patel HK, Levis M, Armstrong RC, James J, Bhagwat SS.

Blood. 2009 Oct 1;114(14):2984-92. doi: 10.1182/blood-2009-05-222034. Epub 2009 Aug 4.


FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo.

Sato T, Yang X, Knapper S, White P, Smith BD, Galkin S, Small D, Burnett A, Levis M.

Blood. 2011 Mar 24;117(12):3286-93. doi: 10.1182/blood-2010-01-266742. Epub 2011 Jan 24.


Reversal of acquired drug resistance in FLT3-mutated acute myeloid leukemia cells via distinct drug combination strategies.

Zhang W, Gao C, Konopleva M, Chen Y, Jacamo RO, Borthakur G, Cortes JE, Ravandi F, Ramachandran A, Andreeff M.

Clin Cancer Res. 2014 May 1;20(9):2363-74. doi: 10.1158/1078-0432.CCR-13-2052. Epub 2014 Mar 11.


Emergence of polyclonal FLT3 tyrosine kinase domain mutations during sequential therapy with sorafenib and sunitinib in FLT3-ITD-positive acute myeloid leukemia.

Baker SD, Zimmerman EI, Wang YD, Orwick S, Zatechka DS, Buaboonnam J, Neale GA, Olsen SR, Enemark EJ, Shurtleff S, Rubnitz JE, Mullighan CG, Inaba H.

Clin Cancer Res. 2013 Oct 15;19(20):5758-68. doi: 10.1158/1078-0432.CCR-13-1323. Epub 2013 Aug 22.


Mutant FLT3: a direct target of sorafenib in acute myelogenous leukemia.

Zhang W, Konopleva M, Shi YX, McQueen T, Harris D, Ling X, Estrov Z, Quintás-Cardama A, Small D, Cortes J, Andreeff M.

J Natl Cancer Inst. 2008 Feb 6;100(3):184-98. doi: 10.1093/jnci/djm328. Epub 2008 Jan 29.


Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD.

Smith CC, Lasater EA, Zhu X, Lin KC, Stewart WK, Damon LE, Salerno S, Shah NP.

Blood. 2013 Apr 18;121(16):3165-71. doi: 10.1182/blood-2012-07-442871. Epub 2013 Feb 21.


FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro.

von Bubnoff N, Engh RA, Aberg E, Sänger J, Peschel C, Duyster J.

Cancer Res. 2009 Apr 1;69(7):3032-41. doi: 10.1158/0008-5472.CAN-08-2923. Epub 2009 Mar 24.


Targeting the FMS-like tyrosine kinase 3 in acute myeloid leukemia.

Swords R, Freeman C, Giles F.

Leukemia. 2012 Oct;26(10):2176-85. doi: 10.1038/leu.2012.114. Epub 2012 Apr 27. Review.


Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation.

Man CH, Fung TK, Ho C, Han HH, Chow HC, Ma AC, Choi WW, Lok S, Cheung AM, Eaves C, Kwong YL, Leung AY.

Blood. 2012 May 31;119(22):5133-43. doi: 10.1182/blood-2011-06-363960. Epub 2012 Feb 24.


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

Albers C, Leischner H, Verbeek M, Yu C, Illert AL, Peschel C, von Bubnoff N, Duyster J.

Leukemia. 2013 Jun;27(6):1416-8. doi: 10.1038/leu.2013.14. Epub 2013 Jan 16. No abstract available.


Treatment with FLT3 inhibitor in patients with FLT3-mutated acute myeloid leukemia is associated with development of secondary FLT3-tyrosine kinase domain mutations.

Alvarado Y, Kantarjian HM, Luthra R, Ravandi F, Borthakur G, Garcia-Manero G, Konopleva M, Estrov Z, Andreeff M, Cortes JE.

Cancer. 2014 Jul 15;120(14):2142-9. doi: 10.1002/cncr.28705. Epub 2014 Apr 15.


Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia.

Zimmerman EI, Turner DC, Buaboonnam J, Hu S, Orwick S, Roberts MS, Janke LJ, Ramachandran A, Stewart CF, Inaba H, Baker SD.

Blood. 2013 Nov 21;122(22):3607-15. doi: 10.1182/blood-2013-07-513044. Epub 2013 Sep 17.


Breakdown of the FLT3-ITD/STAT5 axis and synergistic apoptosis induction by the histone deacetylase inhibitor panobinostat and FLT3-specific inhibitors.

Pietschmann K, Bolck HA, Buchwald M, Spielberg S, Polzer H, Spiekermann K, Bug G, Heinzel T, Böhmer FD, Krämer OH.

Mol Cancer Ther. 2012 Nov;11(11):2373-83. doi: 10.1158/1535-7163.MCT-12-0129. Epub 2012 Aug 31.


FLT3 kinase inhibitor TTT-3002 overcomes both activating and drug resistance mutations in FLT3 in acute myeloid leukemia.

Ma HS, Nguyen B, Duffield AS, Li L, Galanis A, Williams AB, Brown PA, Levis MJ, Leahy DJ, Small D.

Cancer Res. 2014 Sep 15;74(18):5206-17. doi: 10.1158/0008-5472.CAN-14-1028. Epub 2014 Jul 24.


Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia.

Smith CC, Wang Q, Chin CS, Salerno S, Damon LE, Levis MJ, Perl AE, Travers KJ, Wang S, Hunt JP, Zarrinkar PP, Schadt EE, Kasarskis A, Kuriyan J, Shah NP.

Nature. 2012 Apr 15;485(7397):260-3. doi: 10.1038/nature11016.


The role of quizartinib in the treatment of acute myeloid leukemia.

Ostronoff F, Estey E.

Expert Opin Investig Drugs. 2013 Dec;22(12):1659-69. doi: 10.1517/13543784.2013.842973. Epub 2013 Sep 26. Review.


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