Lapatinib, a dual inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2, potentiates the antitumor effects of cisplatin on esophageal carcinoma.

摘要: Epidermal growth factor receptor (EGFR) and human epidermal 2 (HER2) overexpression occurs in over 30% of esophageal carcinomas. Combination therapies EGFR- HER2-targeting agents with cytotoxic are considered a potential therapeutic strategy for cancer. The antitumor effects lapatinib, dual tyrosine kinase inhibitor EGFR HER2, cisplatin alone, the combination two drugs on cancer cells were evaluated. inhibition activity cisplatin, lapatinib plus was measured by 3-(4,5)-dimethylthiahiazo(-z-y1)-3,5-di-phenytetrazoliumromide (MTT) assays, index values calculated. Additionally, cell cycle distribution apoptosis treated or alone detected flow cytometry analysis. activation HER2 signaling pathways monitored Western blot These experimental data showed that synergistically inhibited proliferation exhibited an enhanced pro-apoptotic effect cells. underlying mechanisms potentiated combined treatment associated reduced phosphorylation downstream molecules AKT extracellular regulated protein kinases (ERK). Our findings indicated is one promising strategies carcinomas overexpression.