Abstract In recent years, development of the targeted drugs according to the biological characteristics of tumors have provided more treatment options for tumor patients. It was found that the overactivation or abnormality of B cell receptor (BCR) signal pathway closely related to the occurrence and development of various B cell tumors, such as chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL). As a key kinase in the BCR pathway, BTK inhibitors have obvious anti-tumor effect when its activity is being inhibitered. Currently, BTK inhibitors developed include the first-generation Ibrutinib and the second-generation Acalabrutinib, which can be targeted at the inhibition of BTK and its downstream signaling pathway, and have important therapeutic value for a variety of B-cell tumors, such as CLL and partial non-Hodgkin's lymphoma (NHL). However, its side effects and drug-resistance also gradually emerged, effective drug combination therapy has shown a certain clinical activity. This reviews summarizes briefly the mechanism and status of BTK inhibitors in the treatment of various B-cell tumors.
题目: BTK抑制剂在B细胞肿瘤治疗中的研究进展.
摘要: 近年来，根据肿瘤生物学特性研发的靶向药物已为肿瘤患者提供更多的治疗选择。有研究发现，B细胞受体（BCR）信号通路的过度活化或异常与多种B细胞肿瘤如慢性淋巴细胞白血病（CLL）、套细胞淋巴瘤（MCL）等的发生发展密切相关。BTK（Bruton酪氨酸激酶）作为BCR通路上的关键激酶，抑制其活性可产生明显的抗肿瘤效应。目前已研发的BTK抑制剂包括第一代Ibrutinib、第二代Acalabrutinib等，可靶向抑制BTK及其下游信号通路，对多种B细胞肿瘤如CLL，部分非霍奇金淋巴瘤（NHL）等具有重要治疗价值。然而其毒副作用及耐药问题亦逐渐显现，有效的药物联合治疗方案已显示出一定的临床活性。现就BTK抑制剂治疗多种B细胞肿瘤的机制及现状做一综述.