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2016 ; 9
(1
): 80
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Second-generation inhibitors of Bruton tyrosine kinase
#MMPMID27590878
Wu J
; Liu C
; Tsui ST
; Liu D
J Hematol Oncol
2016[Sep]; 9
(1
): 80
PMID27590878
show ga
Bruton tyrosine kinase (BTK) is a critical effector molecule for B cell
development and plays a major role in lymphoma genesis. Ibrutinib is the
first-generation BTK inhibitor. Ibrutinib has off-target effects on EGFR, ITK,
and Tec family kinases, which explains the untoward effects of ibrutinib.
Resistance to ibrutinib was also reported. The C481S mutation in the BTK kinase
domain was reported to be a major mechanism of resistance to ibrutinib. This
review summarizes the clinical development of novel BTK inhibitors, ACP-196
(acalabrutinib), ONO/GS-4059, and BGB-3111.