Dacomitinib (PF-00299804), a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor, demonstrates remarkable activity against HER2-amplified uterine serous endometrial cancer in vitro

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• 作者：Liancheng Zhu ; Salvatore Lopez ; Stefania Bellone ; Jonathan Black…
• 关键词：Dacomitinib ; Endometrial cancer ; USC ; HER2/neu amplification ; PF ; 00299804
• 刊名：Tumor Biology
• 出版年：2015
• 出版时间：July 2015
• 年：2015
• 卷：36
• 期：7
• 页码：5505-5513
• 全文大小：806 KB
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• 作者单位：Liancheng Zhu (1) (2) r> Salvatore Lopez (1) (3) r> Stefania Bellone (1) r> Jonathan Black (1) r> Emiliano Cocco (1) r> Tiffany Zigras (1) r> Federica Predolini (1) r> Elena Bonazzoli (1) r> Beatrice Bussi (1) r> Zachary Stuhmer (1) r> Carlton L. Schwab (1) r> Diana P. English (1) r> Elena Ratner (1) r> Dan-Arin Silasi (1) r> Masoud Azodi (1) r> Peter E. Schwartz (1) r> Thomas J. Rutherford (1) r> Alessandro D. Santin (1) r>r>1. Department of Obstetrics, Gynecology and Reproductive Sciences, Yale University School of Medicine, Rm. 305 LSOG, 333 Cedar Street, PO Box 208063, New Haven, CT, 06520-8063, USA r> 2. Department of Obstetrics and Gynecology, Shengjing Hospital affiliated to China Medical University, Shenyang, Liaoning, 110004, China r> 3. Division of Gynecologic Oncology, University Campus Bio-Medico of Roma, 00128, Rome, Italy r>
• 刊物主题：Cancer Research;
• 出版者：Springer Netherlands
• ISSN：1423-0380

文摘

Uterine serous carcinoma (USC) is an aggressive subtype of endometrial cancer that carries an extremely poor prognosis. Up to 35?% of USC may overexpress the epidermal growth factor receptor-2 (HER2/neu) at strong (i.e., 3+) level by immunohistochemistry (IHC) or harbor HER2/neu gene amplification by fluorescence in situ hybridization (FISH). In this study, we assessed the sensitivity of a panel of USC cell lines with and without HER2/neu gene amplification to dacomitinib (PF-00299804), an irreversible pan-human epidermal growth factor receptor tyrosine kinase inhibitor. Eight primary cell lines (i.e., four harboring HER2/neu gene amplification by FISH and four FISH?cell lines), all demonstrating similar in vitro growth rates, were evaluated in viability/proliferation assays. The effect of dacomitinib on cell growth, cell cycle distribution, and signaling was determined using flow cytometry-based assays. Dacomitinib caused a significantly stronger growth inhibition in HER2/neu FISH+ USC cell lines when compared to FISH?USC (dacomitinib half maximal inhibitory concentration (IC50) mean?±?SEM--.02803?±-.003355?μM in FISH+ versus 1.498?±-.2209?μM in FISH?tumors, P-lt;-.0001). Dacomitinib growth inhibition was associated with a significant and dose-dependent decline in phosphorylated HER2/neu and S6 transcription factor and a dose-dependent and time-dependent cell cycle arrest in G0/G1 in FISH+ USC. Dacomitinib is remarkably effective against chemotherapy-resistant HER2/neu gene-amplified USC. Clinical studies with dacomitinib in HER2/neu FISH+ USC patients resistant to standard salvage chemotherapy are warranted.