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Osimertinib

奧希替尼

Mechanism of action:

Osimertinib 是一種第三代表皮生長因子受體酪胺酸激酶抑制劑（third-generation EGFR tyrosine kinase inhibitor）。Osimertinib 主要作用於突變型表皮生長因子受體（epidermal growth factor receptor，EGFR），會與受體的酪胺酸激酶形成共價鍵，抑制受體的訊號傳遞，使下游的 PI3K-AKT、MAPK-ERK、JAK-STAT 的訊號路徑無法產生，進而抑制細胞增殖、啟動凋亡。

​Reference(s):

1. Xu M et al. (2015). The latest therapeutic strategies after resistance to first generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) in patients with non-small cell lung cancer (NSCLC). Ann Transl Med. 


2. Tan CS et al. (2015). Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer. Lancet Oncol. 


3. Ayeni D et al. (2015). Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer. Clin Cancer Res.

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