Combating drug resistance in acute myeloid leukaemia by drug rotations: the effects of quizartinib and pexidartinib

J Yang, HJG Lindström, R Friedman - Cancer Cell International, 2021 - Springer
Background Acute myeloid leukaemia (AML) is an aggressive blood cancer. In
approximately 30% of the cases, driver mutations in the FLT3 gene are identified. FLT3 …

Combination strategies to overcome drug resistance in FLT+ acute myeloid leukaemia

J Yang, R Friedman - Cancer Cell International, 2023 - Springer
Background Acute myeloid leukaemia (AML) remains difficult to treat despite the
development of novel formulations and targeted therapies. Activating mutations in the FLT3 …

FLT3 inhibitor quizartinib (AC220)

K Naqvi, F Ravandi - Leukemia & Lymphoma, 2019 - Taylor & Francis
Acute myeloid leukemia (AML) is a heterogeneous disease and remains a therapeutic
challenge. Cytogenetics is a well-established prognostic factor. Recent discovery of …

Secondary mutations as mediators of resistance to targeted therapy in leukemia

N Daver, J Cortes, F Ravandi, KP Patel… - Blood, The Journal …, 2015 - ashpublications.org
The advent of small molecule-based targeted therapy has improved the treatment of both
acute and chronic leukemias. Resistance to small molecule inhibitors has emerged as a …

Recurrent mutations in cyclin D3 confer clinical resistance to FLT3 inhibitors in acute myeloid leukemia

CC Smith, AD Viny, E Massi, C Kandoth, ND Socci… - Clinical Cancer …, 2021 - AACR
Purpose: Biomarkers of response and resistance to FLT3 tyrosine kinase inhibitors (TKI) are
still emerging, and optimal clinical combinations remain unclear. The purpose of this study is …

Heterogeneous resistance to quizartinib in acute myeloid leukemia revealed by single-cell analysis

CC Smith, A Paguirigan, GR Jeschke… - Blood, The Journal …, 2017 - ashpublications.org
Genomic studies have revealed significant branching heterogeneity in cancer. Studies of
resistance to tyrosine kinase inhibitor therapy have not fully reflected this heterogeneity …

The evolving role of FLT3 inhibitors in acute myeloid leukemia: quizartinib and beyond

SA Wander, MJ Levis, AT Fathi - Therapeutic advances in …, 2014 - journals.sagepub.com
Acute myeloid leukemia remains associated with poor outcomes despite advances in our
understanding of the complicated molecular events driving leukemogenesis and malignant …

Clinical resistance to crenolanib in acute myeloid leukemia due to diverse molecular mechanisms

H Zhang, S Savage, AR Schultz, D Bottomly… - Nature …, 2019 - nature.com
FLT3 mutations are prevalent in AML patients and confer poor prognosis. Crenolanib, a
potent type I pan-FLT3 inhibitor, is effective against both internal tandem duplications and …

Deciphering the molecular mechanism of FLT3 resistance mutations

PS Georgoulia, S Bjelic, R Friedman - The FEBS Journal, 2020 - Wiley Online Library
FMS‐like tyrosine kinase 3 (FLT3) has been found to be mutated in~ 30% of acute myeloid
leukaemia patients. Small‐molecule inhibitors targeting FLT3 that are currently approved or …

Mechanisms underlying resistance to FLT3 inhibitors in acute myeloid leukemia

M Eguchi, Y Minami, A Kuzume, SG Chi - Biomedicines, 2020 - mdpi.com
FLT3-ITD and FLT3-TKD mutations were observed in approximately 20 and 10% of acute
myeloid leukemia (AML) cases, respectively. FLT3 inhibitors such as midostaurin, gilteritinib …