Crystal structure of the FLT3 kinase domain bound to the inhibitor Quizartinib (AC220)

JA Zorn, Q Wang, E Fujimura, T Barros, J Kuriyan - PloS one, 2015 - journals.plos.org
More than 30% of acute myeloid leukemia (AML) patients possess activating mutations in
the receptor tyrosine kinase FMS-like tyrosine kinase 3 or FLT3. A small-molecule inhibitor …

A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells with FLT3 mutations

T Yamaura, T Nakatani, K Uda, H Ogura… - Blood, The Journal …, 2018 - ashpublications.org
An activating mutation of Fms-like tyrosine kinase 3 (FLT3) is the most frequent genetic
alteration associated with poor prognosis in acute myeloid leukemia (AML). Although many …

Quizartinib for the treatment of FLT3/ITD acute myeloid leukemia

M Levis - Future oncology, 2014 - Taylor & Francis
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 …

Quizartinib elicits differential responses that correlate with karyotype and genotype of the leukemic clone

GE Nybakken, J Canaani, D Roy, JD Morrissette… - Leukemia, 2016 - nature.com
Fms-like tyrosine kinase 3 (FLT3) is one of the most commonly mutated genes in acute
myeloid leukemia (AML) and as such has been a highly studied therapeutic target in the …

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

PP Zarrinkar, RN Gunawardane… - Blood, The Journal …, 2009 - ashpublications.org
Activating mutations in the receptor tyrosine kinase FLT3 are present in up to approximately
30% of acute myeloid leukemia (AML) patients, implicating FLT3 as a driver of the disease …

Profile of quizartinib for the treatment of adult patients with relapsed/refractory FLT3-ITD-positive acute myeloid leukemia: evidence to date

L Fletcher, SK Joshi, E Traer - Cancer Management and Research, 2020 - Taylor & Francis
Acute myeloid leukemia (AML) is a clonal hematologic neoplasm characterized by rapid,
uncontrolled cell growth of immature myeloid cells (blasts). There are numerous genetic …

FLT3 inhibitors in AML: are we there yet?

A Sudhindra, CC Smith - Current hematologic malignancy reports, 2014 - Springer
FMS-like tyrosine kinase 3 (FLT3) is the most frequently mutated gene in AML. Thirty percent
of patients with acute myeloid leukemia (AML) harbor activating mutations in FLT3, either …

Transient exposure to quizartinib mediates sustained inhibition of FLT3 signaling while specifically inducing apoptosis in FLT3-activated leukemia cells

RN Gunawardane, RR Nepomuceno, AM Rooks… - Molecular cancer …, 2013 - AACR
Fms-like tyrosine kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid
leukemia (AML). FLT3-activating internal tandem duplication (ITD) mutations are found in …

Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants

A Galanis, H Ma, T Rajkhowa… - Blood, The Journal …, 2014 - ashpublications.org
Mutations of the type III receptor tyrosine kinase FLT3 occur in approximately 30% of acute
myeloid leukemia patients and lead to constitutive activation. This has made FLT3-activating …

The role of quizartinib in the treatment of acute myeloid leukemia

F Ostronoff, E Estey - Expert opinion on investigational drugs, 2013 - Taylor & Francis
Introduction: Approximately one-third of the patients with acute myeloid leukemia (AML)
harbor internal tandem duplication (ITD) in the gene encoding FMS-like tyrosine kinase 3 …