Abstract:
:Ibrutinib, an inhibitor of Bruton tyrosine kinase (BTK), has shown promising pharmacologic effects in acute myeloid leukemia (AML). In this study, we report that abivertinib or AC0010, a novel BTK inhibitor, inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations. Abivertinib was also found to be more sensitive than ibrutinib in treating AML. We demonstrate that in addition to targeting the phosphorylation of BTK, abivertinib also targeted the crucial PI3K survival pathway. Furthermore, abivertinib suppressed the expression of p-FLT3 and the downstream target p-STAT5 in AML cells harboring FLT3-ITD mutations. Moreover, in vitro and in vivo data revealed synergistic activity between abivertinib and homoharringtonine (HHT), a natural plant alkaloid commonly used in China, in treating AML cells with or without FLT3-ITD mutations. Collectively, these preclinical data suggest that abivertinib may be a promising novel agent for AML, with potential for combination treatment with HHT. Clinical studies on abivertinib-involved therapy are planned.
journal_name
Cancer Lettjournal_title
Cancer lettersauthors
Huang S,Pan J,Jin J,Li C,Li X,Huang J,Huang X,Yan X,Li F,Yu M,Hu C,Jin J,Xu Y,Ling Q,Ye W,Wang Y,Jin Jdoi
10.1016/j.canlet.2019.07.008subject
Has Abstractpub_date
2019-10-01 00:00:00pages
132-143eissn
0304-3835issn
1872-7980pii
S0304-3835(19)30404-5journal_volume
461pub_type
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