布鲁顿酪氨酸激酶第二代抑制剂
Second-generation inhibitors of Bruton tyrosine kinase.
作者信息
Wu Jingjing, Liu Christina, Tsui Stella T, Liu Delong
机构信息
Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China.
Weinberg College of Arts and Sciences, Northwestern University, Evanston, IL, 60208, USA.
出版信息
J Hematol Oncol. 2016 Sep 2;9(1):80. doi: 10.1186/s13045-016-0313-y.
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.
布鲁顿酪氨酸激酶（BTK）是B细胞发育的关键效应分子，在淋巴瘤发生中起主要作用。伊布替尼是第一代BTK抑制剂。伊布替尼对表皮生长因子受体（EGFR）、白细胞介素-2诱导的T细胞激酶（ITK）和Tec家族激酶有脱靶效应，这解释了伊布替尼的不良反应。也有关于伊布替尼耐药的报道。据报道，BTK激酶结构域中的C481S突变是对伊布替尼耐药主要机制。本综述总结了新型BTK抑制剂ACP-196（阿卡替尼）、ONO/GS-4059和BGB-3111的临床进展。
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