[關(guān)鍵詞]
[摘要]
磷脂酰肌醇-3激酶(PI3K)是一種胞內(nèi)磷脂酰肌醇激酶,吉利德正在開發(fā)的血癌新藥idelalisib是首個(gè)選擇性口服PI3K抑制劑,與α、β、γ亞基相比,其可高度選擇性地作用于δ亞基。idelalisib可阻滯PI3Kδ-Akt信號(hào)通路并促進(jìn)細(xì)胞凋亡,從而有效治療難治性惰性非霍奇金淋巴瘤(iNHL)。研究表明idelalisib能夠顯著增加B細(xì)胞急性淋巴細(xì)胞白血?。˙-ALL)和慢性淋巴細(xì)胞白血?。–LL)細(xì)胞系的凋亡,同時(shí)沒(méi)有顯著增加正常T細(xì)胞的凋亡。在一系列臨床研究中顯示出良好的治療前景,且安全性及耐受性均較好。
[Key word]
[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.
[中圖分類號(hào)]
[基金項(xiàng)目]