G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia

HK Lee, HW Kim, IY Lee, J Lee, J Lee… - Blood, The Journal …, 2014 - ashpublications.org
Aberrant activations of Fms-like tyrosine receptor kinase (FLT) 3 are implicated in the
pathogenesis of 20% to 30% of patients with acute myeloid leukemia (AML). G-749 is a …

Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia

BD Smith, M Levis, M Beran, F Giles, H Kantarjian… - Blood, 2004 - ashpublications.org
Activating mutations of FMS-like tyrosine kinase 3 (FLT3) are present in approximately 30%
of patients with de novo acute myeloid leukemia (AML) and are associated with lower cure …

MZH29 is a novel potent inhibitor that overcomes drug resistance FLT3 mutations in acute myeloid leukemia

B Xu, Y Zhao, X Wang, P Gong, W Ge - Leukemia, 2017 - nature.com
More than one-third of patients with acute myeloid leukemia (AML) harbor aberrant
mutations in Fms-like tyrosine kinase 3 (FLT3). Among them, the internal tandem duplication …

A dual inhibitor overcomes drug-resistant FLT3-ITD acute myeloid leukemia

P Wang, X Xiao, Y Zhang, B Zhang, D Li, M Liu… - Journal of Hematology & …, 2021 - Springer
FLT3 mutations are the most frequently identified genetic alterations in acute myeloid
leukemia (AML) and are associated with poor prognosis. Multiple FLT3 inhibitors are in …

Targeting AML-associated FLT3 mutations with a type I kinase inhibitor

LQM Jones, K Melgar, L Bolanos… - The Journal of …, 2020 - Am Soc Clin Investig
Tyrosine kinase domain (TKD) mutations contribute to acquired resistance to FMS-like
tyrosine kinase 3 (FLT3) inhibitors used to treat FLT3-mutant acute myeloid leukemia (AML) …

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

HS Ma, B Nguyen, AS Duffield, L Li, A Galanis… - Cancer research, 2014 - AACR
There have been a number of clinical trials testing the efficacy of FMS-like tyrosine kinase-3
(FLT3) tyrosine kinase inhibitors (TKI) in patients with acute myeloid leukemia (AML) …

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

AS Moore, A Faisal, DG De Castro, V Bavetsias, C Sun… - Leukemia, 2012 - nature.com
Acquired resistance to selective FLT3 inhibitors is an emerging clinical problem in the
treatment of FLT3-ITD+ acute myeloid leukaemia (AML). The paucity of valid pre-clinical …

The irreversible FLT3 inhibitor FF-10101 is active against a diversity of FLT3 inhibitor resistance mechanisms

TT Ferng, D Terada, M Ando, TC Tarver… - Molecular cancer …, 2022 - AACR
Small-molecule FLT3 inhibitors have recently improved clinical outcomes for patients with
FLT3-mutant acute myeloid leukemia (AML) after many years of development, but resistance …

Drug resistance in mutant FLT3-positive AML

E Weisberg, M Sattler, A Ray, JD Griffin - Oncogene, 2010 - nature.com
Abstract Mutant Fms-Like Tyrosine kinase-3 (FLT3), which is expressed in the leukemic cells
of a subpopulation of acute myeloid leukemia (AML) patients, represents an attractive target …

Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and-resistant FLT3-expressing cells

E Weisberg, J Roesel, G Bold, P Furet… - Blood, The Journal …, 2008 - ashpublications.org
An attractive target for therapeutic intervention is constitutively activated, mutant FLT3, which
is expressed in a subpopulation of patients with acute myelocyic leukemia (AML) and is …