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[摘要]
磷脂酰肌醇-3激酶(PI3K)是一种胞内磷脂酰肌醇激酶,吉利德正在开发的血癌新药idelalisib是首个选择性口服PI3K抑制剂,与α、β、γ亚基相比,其可高度选择性地作用于δ亚基。idelalisib可阻滞PI3Kδ-Akt信号通路并促进细胞凋亡,从而有效治疗难治性惰性非霍奇金淋巴瘤(iNHL)。研究表明idelalisib能够显著增加B细胞急性淋巴细胞白血病(B-ALL)和慢性淋巴细胞白血病(CLL)细胞系的凋亡,同时没有显著增加正常T细胞的凋亡。在一系列临床研究中显示出良好的治疗前景,且安全性及耐受性均较好。
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[Abstract]
Phosphatidyl inositol 3 kinase (PI3K) is an intracellular phosphatidyl inositol kinase, and the leukaemia drug idelalisib which is developped by Gilead is the first oral PI3K selective inhibitor. Compared with α, β, and γ subunits, it plays a highly selective role in the δ subunit. idelalisib can block PI3Kδ - Akt signaling pathways and promote cell death. Therefore idelalisib can cure indolent non-hodgkin lymphoma (iNHL) effectively. Studies have shown that idelalisib can significantly increase the cell apoptosis of B cell acute lymphoblastic leukemia (B-ALL) and chronic lymphocytic leukemia (CLL), and it has no significant increase in the normal T cell apoptosis. And it shows a good prospect in a series of clinical studies with good safety and tolerability.
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