Quizartinib for the treatment of FLT3/ITD acute myeloid leukemia

被引:2
作者
Levis, Mark [1 ]
机构
[1] Johns Hopkins Univ, Sidney Kimmel Comprehens Canc Ctr, Dept Oncol, Baltimore, MD 21287 USA
关键词
c-KIT; FLT3; kinase; leukemia; quizartinib; INTERNAL TANDEM DUPLICATION; TYROSINE KINASE INHIBITOR; RISK MYELODYSPLASTIC SYNDROME; PHASE-I; THERAPEUTIC TARGET; ANTITUMOR-ACTIVITY; MUTANT FLT3; SORAFENIB; AML; ACTIVATION;
D O I
10.2217/FON.14.105
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
FLT3/ITD acute myeloid leukemia is a poor prognosis disease driven by a constitutively activated receptor tyrosine kinase, making it an obvious target for drug development. The development of clinically effective FLT3 inhibitors has been slow, in part because many are multi-targeted inhibitors that are not selective or specific for FLT3. Quizartinib is the first small molecule FLT3 tyrosine kinase inhibitor expressly developed as a FLT3 inhibitor. It is potent, selective and has ideal pharmacokinetics in comparison to other compounds previously tested. This article summarizes its advantages and limitations, and details the insights into the biology of the disease that have been uncovered through the laboratory and clinical use of quizartinib.
引用
收藏
页码:1571 / 1579
页数:9
相关论文
共 64 条
  • [1] Antitumor activity of sorafenib in FLT3-driven leukemic cells
    Auclair, D.
    Miller, D.
    Yatsula, V.
    Pickett, W.
    Carter, C.
    Chang, Y.
    Zhang, X.
    Wilkie, D.
    Burd, A.
    Shi, H.
    Rocks, S.
    Gedrich, R.
    Abriola, L.
    Vasavada, H.
    Lynch, M.
    Dumas, J.
    Trail, P. A.
    Wilhelm, S. M.
    [J]. LEUKEMIA, 2007, 21 (03) : 439 - 445
  • [2] A novel molecular mechanism of primary resistance to FLT3-kinase inhibitors in AML
    Breitenbuecher, Frank
    Markova, Boyka
    Kasper, Stefan
    Carius, Birgit
    Stauder, Torsten
    Boehmer, Frank D.
    Masson, Kristina
    Ronnstrand, Lars
    Huber, Christoph
    Kindler, Thomas
    Fischer, Thomas
    [J]. BLOOD, 2009, 113 (17) : 4063 - 4073
  • [3] Hematopoietic transplantation for acute myeloid leukemia with internal tandem duplication of FLT3 gene (FLT3/ITD)
    Brunet, Salut
    Martino, Rodrigo
    Sierra, Jorge
    [J]. CURRENT OPINION IN ONCOLOGY, 2013, 25 (02) : 195 - 204
  • [4] Therapeutic Advances in Acute Myeloid Leukemia
    Burnett, Alan
    Wetzler, Meir
    Loewenberg, Bob
    [J]. JOURNAL OF CLINICAL ONCOLOGY, 2011, 29 (05) : 487 - 494
  • [5] Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor
    Chao, Qi
    Sprankle, Kelly G.
    Grotzfeld, Robert M.
    Lai, Andiliy G.
    Carter, Todd A.
    Velasco, Anne Marie
    Gunawardane, Ruwanthi N.
    Cramer, Merryl D.
    Gardner, Michael F.
    James, Joyce
    Zarrinkar, Patrick P.
    Patel, Hitesh K.
    Bhagwat, Shripad S.
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2009, 52 (23) : 7808 - 7816
  • [6] Revised recommendations of the international working group for diagnosis, standardization of response criteria, treatment outcomes, and reporting standards for therapeutic trials in acute myeloid leukemia
    Cheson, BD
    Bennett, JM
    Kopecky, KJ
    Büchner, T
    Willman, CL
    Estey, EH
    Schiffer, CA
    Döhner, H
    Tallman, MS
    Lister, TA
    LoCocco, F
    Willemze, R
    Biondi, A
    Hiddemann, W
    Larson, RA
    Löwenberg, B
    Sanz, MA
    Head, DR
    Ohno, R
    Bloomfield, CD
    [J]. JOURNAL OF CLINICAL ONCOLOGY, 2003, 21 (24) : 4642 - 4649
  • [7] AML-associated Flt3 kinase domain mutations show signal transduction differences compared with Flt3 ITD mutations
    Choudhary, C
    Schwäble, J
    Brandts, C
    Tickenbrock, L
    Sargin, B
    Kindler, T
    Fischer, T
    Berdel, WE
    Müller-Tidow, C
    Serve, H
    [J]. BLOOD, 2005, 106 (01) : 265 - 273
  • [8] Mislocalized Activation of Oncogenic RTKs Switches Downstream Signaling Outcomes
    Choudhary, Chunaram
    Olsen, Jesper V.
    Brandts, Christian
    Cox, Jurgen
    Reddy, Pavankurnar N. G.
    Boehmer, Frank D.
    Gerke, Volker
    Schmidt-Arras, Dirk-E.
    Berdel, Wolfgang E.
    Mueller-Tidow, Carsten
    Mann, Matthias
    Serve, Hubert
    [J]. MOLECULAR CELL, 2009, 36 (02) : 326 - 339
  • [9] Cortes J, 2011, 16 C EUR HEM ASS LON
  • [10] Cortes J, 2012, ASH ANN M, V120, p48a