阿卡替尼（ACP-196）：一种选择性第二代布鲁顿酪氨酸激酶（BTK）抑制剂。
Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor.
作者信息
Wu Jingjing, Zhang Mingzhi, Liu Delong
机构信息
Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China.
出版信息
J Hematol Oncol. 2016 Mar 9;9:21. doi: 10.1186/s13045-016-0250-9.
Abstract
More and more targeted agents become available for B cell malignancies with increasing precision and potency. The first-in-class Bruton's tyrosine kinase (BTK) inhibitor, ibrutinib, has been in clinical use for the treatment of chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom's macroglobulinemia. More selective BTK inhibitors (ACP-196, ONO/GS-4059, BGB-3111, CC-292) are being explored. Acalabrutinib (ACP-196) is a novel irreversible second-generation BTK inhibitor that was shown to be more potent and selective than ibrutinib. This review summarized the preclinical research and clinical data of acalabrutinib.
摘要
随着精准度和效力的不断提高，越来越多的靶向药物可用于治疗B细胞恶性肿瘤。首个布鲁顿酪氨酸激酶（BTK）抑制剂依鲁替尼已在临床上用于治疗慢性淋巴细胞白血病、套细胞淋巴瘤和华氏巨球蛋白血症。更多选择性BTK抑制剂（ACP-196、ONO/GS-4059、BGB-3111、CC-292）正在进行研究。阿卡替尼（ACP-196）是一种新型不可逆第二代BTK抑制剂，已证明其比依鲁替尼更有效且更具选择性。本综述总结了阿卡替尼的临床前研究和临床数据。
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