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Gefitinib

吉非替尼

Mechanism of action:

Gefitinib 是一種表皮生長因子受體酪胺酸激酶抑制劑（epidermal growth factor receptor tyrosine kinase inhibitor）。Gefitinib 會競爭性結合於表皮生長因子受體的酪胺酸激酶區域的 ATP 結合位點，阻止表皮生長因子受體自我磷酸化（autophosphorylation）。這能防止下游 PI3K/AKT、RAS/RAF/MEK/ERK、JAK/STAT 路徑的活化，能降低細胞存活與增殖相關訊號並提高凋亡路徑的啟動傾向。

​Reference(s):

1. Pao W et al. (2004). EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A. 


2. Sordella R et al. (2004). Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science.

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