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Association details:
Evidence:
Evidence Level:
Resistant: C3 – Early Trials
New
Source:
Title:

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

Excerpt:
...evolution of AC220-resistant substitutions at two of these amino acid positions was observed in eight of eight FLT3-ITD-positive AML patients with acquired resistance to AC220….The activation loop mutation D835Y was detected in three cases, D835V in two, and the gatekeeper mutation F691L was identified in three....
DOI:
https://dx.doi.org/10.1038%2Fnature11016
Trial ID:
Evidence Level:
Resistant: D – Preclinical
New
Title:

Characterizing and Overriding the Structural Mechanism of the Quizartinib-resistant FLT3 “Gatekeeper” F691L Mutation with PLX3397

Excerpt:
We performed proliferation studies of PLX3397 and quizartinib for Ba/F3 cells expressing FLT3-ITD and FLT3-ITD/F691L and confirmed that PLX3397, in contrast to quizartinib, has the ability to inhibit the proliferation of both isoforms...
DOI:
https://dx.doi.org/10.1158%2F2159-8290.CD-15-0060