依鲁替尼:一种新型布鲁顿酪氨酸激酶抑制剂  

Ibrutinib: a novel Bruton's tyrosine kinase inhibitor

作　　者：郑小娟[1] 王婧斯 龚莉 王春龙 

机构地区：[1]天津中医药大学,天津300193 [2]天津泛博生物科技有限公司,天津300384

出　　处：《药物评价研究》2014年第4期381-384,共4页Drug Evaluation Research

摘　　要：依鲁替尼是布鲁顿酪氨酸激酶（BTK）抑制剂,用于治疗慢性淋巴细胞白血病（CLL）和套细胞淋巴瘤（MCL）。MCL和CLL均属于B细胞非霍奇金淋巴瘤,具有难治愈性和易复发性,常用的化学免疫疗法不具备靶向性,常发生3或4级不良反应。依鲁替尼可与B淋巴细胞形成、分化、信息传递和生存所必需的BTK靶向性结合,不可逆地抑制BTK的活性,有效抑制肿瘤细胞的增殖和存活;且口服后吸收迅速,1~2 h达最大血药浓度,不良反应属于1或2级,将成为治疗CLL和MCL的新选择。Ibrutinib, as a Bruton＇s tyrosine kinase （BTK） inhibitor, is indicated for the treatment of the patients with mantle cell lyrnphoma （MCL） and chronic lymphocytic leukaemia （CLL）. MCL and CLL are difficult to cure and easy to recurrent, which belong to the group of B-cell non-Hodgkin lymphomas （NHL）. Chemoimmunotherapy, which commonly applied in clinical, could not realize the targeted therapy, accompanied by adverse reaction of Grade 3 or 4. Ibrutinib could bind to BTK needed by the formation, differenciation, inform translation and survival by lymphocyte B and irreversibly inhibit BTK activity, thereby preventing both B-cell activation and B-cell-mediated signaling. This leads to an inhibition of the proliferation and survival of tumor cells. Ibrutinib is absorbed after oral administration with a median Tmax of 1 to 2 h and the most commonly occurring adverse reactions are Grade 1 or 2. Therefore, Ibrutinib has a potential as a novel drug for treating CLL and MCL.

关 键 词：依鲁替尼 慢性淋巴细胞白血病 套细胞淋巴瘤 布鲁顿酪氨酸激酶 

分 类 号：R979.1[医药卫生—药品]