Anti-FLT3 nanoparticles for acute myeloid leukemia: Preclinical pharmacology and pharmacokinetics

M Park, VP Vaikari, AT Lam, Y Zhang… - Journal of Controlled …, 2020 - Elsevier
… The presence of wild-type FLT3, which is sensitive to FLT3 ligand and relatively resistant
to … to have promising antileukemia activity both in vitro and in FLT3-ITD murine models [39]. …

[HTML][HTML] Effect of Fms-like tyrosine kinase 3 (FLT3) ligand (FL) on antitumor activity of gilteritinib, a FLT3 inhibitor, in mice xenografted with FL-overexpressing cells

T Kawase, T Nakazawa, T Eguchi, H Tsuzuki, Y Ueno… - Oncotarget, 2019 - ncbi.nlm.nih.gov
… One of the critical issues of treatment with FLT3 inhibitors in FLT3-mutated AML is drug
resistance. FLT3 ligand (FL) represents a mechanism of resistance to FLT3 inhibitors, including …

Discovery of orally active indirubin-3′-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia

P Jeong, Y Moon, JH Lee, SD Lee, J Park, J Lee… - European Journal of …, 2020 - Elsevier
leukemia cells and normal hematopoietic stem cells. The activation of FLT3 is initiated by the
binding of the FLT3 ligand … in the AML cell line and in vivo anticancer efficacy in a xenograft …

[HTML][HTML] LT-171-861, a novel FLT3 inhibitor, shows excellent preclinical efficacy for the treatment of FLT3 mutant acute myeloid leukemia

Z Yu, J Du, H Hui, S Kan, T Huo, K Zhao, T Wu… - Theranostics, 2021 - ncbi.nlm.nih.gov
… changes within FLT3 result in constitutive activation without stimulation of the FLT3 ligand
(FL… We report in vitro anti-leukemic activity of LT-171-861 that is as potent as that of AC220 and …

[HTML][HTML] Quizartinib, a selective FLT3 inhibitor, maintains antileukemic activity in preclinical models of RAS-mediated midostaurin-resistant acute myeloid leukemia …

T Aikawa, N Togashi, K Iwanaga, H Okada, Y Nishiya… - Oncotarget, 2020 - ncbi.nlm.nih.gov
Antileukemic activity of quizartinib in xenograft models of midostaurin-… on the antileukemic
activity of FLT3 inhibitors in the mouse xenograft model… signaling, independent of FLT3 ligand. …

FLT3 inhibitors in acute myeloid leukemia: challenges and recent developments in overcoming resistance

Z Wang, J Cai, J Cheng, W Yang, Y Zhu… - Journal of Medicinal …, 2021 - ACS Publications
… (4) When the FLT3 ligand (FL) binds the extracellular domain, FLT3 dimerizes and is …
antileukemic activity in mice xenografted with FLT3-ITD-D835Y cells, extending the OS of mice

A review of FLT3 inhibitors in acute myeloid leukemia

JC Zhao, S Agarwal, H Ahmad, K Amin, JP Bewersdorf… - Blood reviews, 2022 - Elsevier
… and is activated by FLT3 ligand (FL). … mouse models, gilteritinib decreased FLT3
phosphorylation levels along with its downstream targets supporting single-agent anti-leukemic

Characterization of a novel FLT3 BiTE molecule for the treatment of acute myeloid leukemia

B Brauchle, RL Goldstein, CM Karbowski, A Henn… - Molecular Cancer …, 2020 - AACR
antileukemic effect of HSCT is driven by recognition and elimination of allogeneic antigens
on chemoresistant leukemic … with or without 10 ng/mL soluble FLT3 ligand (16) for 48 hours. …

Glucocorticoids enhance the antileukemic activity of FLT3 inhibitors in FLT3-mutant acute myeloid leukemia

MT Gebru, JM Atkinson, MM Young… - Blood, The Journal …, 2020 - ashpublications.org
… Moreover, the enhanced antileukemic activity by quizartinib and dexamethasone … and
xenograft mouse models. Collectively, our study indicates that the combination of FLT3 inhibitors …

Small-molecule fms-like tyrosine kinase 3 inhibitors: an attractive and efficient method for the treatment of acute myeloid leukemia

Y Zhong, RZ Qiu, SL Sun, C Zhao, TY Fan… - Journal of medicinal …, 2020 - ACS Publications
… These first-generation inhibitors lack specificity for FLT3 and perform antileukemia efficacy
… and FLT3 may contribute to the antileukemia therapy, particularly drug resistance after FLT3