新型布鲁顿酪氨酸激酶抑制剂奥布替尼研究进展

Research progress of new Bruton’s tyrosine kinase inhibitor Orelabrutinib

奥布替尼是一种新型布鲁顿酪氨酸激酶(BTK)抑制剂,是我国自主研发的Ⅰ类创新药,为淋巴瘤患者尤其是复发/难治性套细胞淋巴瘤和复发/难治性慢性淋巴细胞白血病/小淋巴细胞淋巴瘤的治疗带来新的手段。BTK是B细胞抗原受体信号通路的关键激酶,对恶性B细胞的增殖和生存至关重要,是治疗B细胞恶性淋巴瘤极具前景的药物靶标。因此,本文回顾了BTK抑制剂的作用机制与已上市BTK抑制剂的基本信息,整理了奥布替尼的药理学性质与临床数据,梳理了迄今为止最新的奥布替尼临床研究进展,提出了奥布替尼是目前具有潜力的BTK抑制剂并且是进行BTK抑制剂联合治疗时的最佳候选药物。

Orelabrutinib,a novel Bruton’s tyrosine kinase(BTK)inhibitor,is a classⅠinnovative drug independently developed in China.Its emergence brings new therapeutic methods for the treatment of lymphoma patients,especially the patients with relapsed/refractory mantle cell lymphoma and relapsed/refractory chronic lymphocytic leukemia/small cell leukemia.BTK is a key kinase in the B-cell antigen receptor signaling pathway and is crucial to the proliferation and survival of malignant B cells,thus it is a promising target for the treatment of B-cell malignant lymphoma.Therefore,this paper reviews the mechanism of action of BTK inhibitor and the basic information of listed BTK inhibitors,summarizes the pharmacological properties and clinical data of Orelabrutinib,and sorts out the latest clinical research progress of Orelabrutinib so far,and proposed that Orelabrutinib is the most potential BTK inhibitor at present and candidate drug for BTK inhibitor combination therapy.