Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase.
Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase.
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DOI：
10.1586/14737140.3.3.269
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发表时间：
2003-06-01
影响因子：
3.3
通讯作者：
Perez-Soler, Roman
中科院分区：
文献类型：
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作者：
Bulgaru, Anca M;Mani, Sridhar;Perez-Soler, Roman
表皮生长因子受体（EGFR）的过度表达与几种人类恶性肿瘤的不良预后相关。此外，过表达EGFR的癌症对化疗和放疗的反应都很差。因此，EGFR是癌症治疗的可行靶点。这篇综述将讨论EGFR阻断如何调节信号转导，导致细胞周期进程的改变，并继发性抑制癌细胞的增殖和分化。作为一个典型的例子，厄洛替尼（特罗凯），一个可逆的EGFR酪氨酸激酶抑制剂将进行讨论。该药物已在几种实体瘤的II期试验中显示出有希望的抗肿瘤活性，并且证明临床获益的确定性III期研究已完成累积。
Overexpression of the epidermal growth factor receptor (EGFR) is correlated with a poor prognosis in several human malignancies. In addition, cancers overexpressing EGFR respond poorly to both chemotherapy and radiation therapy. Therefore, EGFR is a viable target for cancer therapy. This review will address how EGFR blockade modulates signal transduction, leading to alterations in the cell cycle progression with secondary inhibition of proliferation and differentiation of cancer cells. As a prototypical example, erlotinib (Tarceva), a reversible EGFR tyrosine kinase inhibitor will be discussed. This drug has demonstrated promising antitumor activity in Phase II trials in several solid tumors and definitive Phase III studies to demonstrate clinical benefit have completed accrual.