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[摘要]
依魯替尼是布魯頓酪氨酸激酶(BTK)抑制劑,用于治療慢性淋巴細胞白血病(CLL)和套細胞淋巴瘤(MCL)。MCL和CLL均屬于B細胞非霍奇金淋巴瘤,具有難治愈性和易復發(fā)性,常用的化學免疫療法不具備靶向性,常發(fā)生3或4級不良反應。依魯替尼可與B淋巴細胞形成、分化、信息傳遞和生存所必需的BTK靶向性結合,不可逆地抑制BTK的活性,有效抑制腫瘤細胞的增殖和存活;且口服后吸收迅速,1~2 h達最大血藥濃度,不良反應屬于1或2級,將成為治療CLL和MCL的新選擇。
[Key word]
[Abstract]
Ibrutinib, as a Bruton's tyrosine kinase (BTK) inhibitor, is indicated for the treatment of the patients with mantle cell lymphoma (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.
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