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Lapatinib

拉帕替尼

Mechanism of action:

Lapatinib 是一種小分子酪胺酸激酶抑制劑（tyrosine kinase inhibitor），屬於雙重 HER2/EGFR 抑制劑（dual HER2/EGFR inhibitor）。Lapatinib 會與表皮生長因子受體（epidermal growth factor receptor，EGFR）與人類表皮生長因子受體 2（human epidermal growth factor receptor 2 ，HER2）的 ATP 結合位點結合，阻止 ATP 進入激酶結構域，使受體無法自我磷酸化（autophosphorylation）。這導致下游的多條關鍵腫瘤生長與存活路徑（如 PI3K / AKT / mTOR、MAPK / ERK）被抑制，降低腫瘤細胞的增殖與存活訊號，並可誘發凋亡相關反應。

​Reference(s):

1. Nelson MH et al. (2006). Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Ann Pharmacother. 


2. Burris HA et al. (2004). Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist. 


3. Burris HA et al. (2005). Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. J Clin Oncol.

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