Mechanisms Underlying Resistance to FLT3 Inhibitors in Acute Myeloid Leukemia.
FMS-like tyrosine kinase 3 (FLT3)
acute myeloid leukemia (AML)
gilteritinib
quizartinib
Journal
Biomedicines
ISSN: 2227-9059
Titre abrégé: Biomedicines
Pays: Switzerland
ID NLM: 101691304
Informations de publication
Date de publication:
24 Jul 2020
24 Jul 2020
Historique:
received:
11
06
2020
revised:
10
07
2020
accepted:
16
07
2020
entrez:
30
7
2020
pubmed:
30
7
2020
medline:
30
7
2020
Statut:
epublish
Résumé
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 and quizartinib show excellent response rates in patients with FLT3-mutated AML, but its duration of response may not be sufficient yet. The majority of cases gain secondary resistance either by on-target and off-target abnormalities. On-target mutations (i.e., FLT3-TKD) such as D835Y keep the TK domain in its active form, abrogating pharmacodynamics of type II FLT3 inhibitors (e.g., midostaurin and quizartinib). Second generation type I inhibitors such as gilteritinib are consistently active against FLT3-TKD as well as FLT3-ITD. However, a "gatekeeper" mutation F691L shows universal resistance to all currently available FLT3 inhibitors. Off-target abnormalities are consisted with a variety of somatic mutations such as
Identifiants
pubmed: 32722298
pii: biomedicines8080245
doi: 10.3390/biomedicines8080245
pmc: PMC7459983
pii:
doi:
Types de publication
Journal Article
Review
Langues
eng
Déclaration de conflit d'intérêts
Y.M. received research funding from Ono and honoraria from Bristol-Myers Squibb, Novartis, and Pfizer. The other authors declare no conflicts of interest.
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