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Idelalisib

伊德利塞

Mechanism of action:

Idelalisib 是一種磷酸肌醇3-激酶 δ 抑制劑（PI3K-δ inhibitor）。磷酸肌醇3-激酶 δ（PI3K-δ）主要表達在各種血細胞，特別是 B 淋巴球中，並在 B 細胞受體（BCR）訊號傳遞中扮演關鍵功能。Idelalisib 會抑制 PI3K-δ 的活性，阻斷 PIP2 轉換為 PIP3 的反應，使其下游 AKT、mTOR 等訊號路徑活性下降，導致細胞增殖受抑、細胞凋亡增加。

​Reference(s):

1. Jin F et al. (2015). Clinical drug interaction profile of idelalisib in healthy subjects. J Clin Pharmacol. 


2. Fiorcari S et al. (2013). The PI3-kinase delta inhibitor idelalisib (GS-1101) targets integrin-mediated adhesion of chronic lymphocytic leukemia (CLL) cell to endothelial and marrow stromal cells. PLoS One. 


3. Flinn IW et al. (2014). Idelalisib, a selective inhibitor of phosphatidylinositol 3-kinase-delta, as therapy for previously treated indolent non-Hodgkin lymphoma. Blood.

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