Targeting the epidermal growth factor receptor.
Targeting the epidermal growth factor receptor.
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DOI：
10.1038/sj.bjc.6601921
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发表时间：
2004-08-02
影响因子：
8.8
通讯作者：
中科院分区：
文献类型：
--
作者：
表皮生长因子受体（EGFR）是酪氨酸激酶受体（RTK）的erbB家族的成员。EGFR参与细胞增殖、转移和血管生成，并且在大部分上皮肿瘤中表达。临床试验中的两类主要EGFR抑制剂是RTK抑制剂和单克隆抗体。EGFR抑制剂的临床开发为I、II和III期试验的设计带来了新的挑战。这两类药物都可以安全地以足以抑制EGFR系统的剂量给药。受体酪氨酸激酶抑制剂已在非小细胞肺癌中得到广泛评价。在这种情况下，吉非替尼已被证明在初始化疗失败的患者中具有活性。单克隆抗体已被开发与细胞毒性化疗在几种肿瘤类型，最显着的结肠直肠癌和头颈部癌的组合。初步结果表明，在两种疾病模型中，西妥昔单抗和化疗联合治疗的缓解率和进展时间均增加。EGFR抑制剂开发中的未来问题包括识别反应的生物学预测因子，与其他靶向药物的组合，以及它们在早期恶性肿瘤中的应用。
The epidermal growth factor receptor (EGFR) is a member of the erbB family of tyrosine kinase receptors (RTK). The EGFR is involved in cell proliferation, metastasis and angiogenesis, and is expressed in a large proportion of epithelial tumours. The two main classes of EGFR inhibitors in clinical trials are the RTK inhibitors and the monoclonal antibodies. The clinical development of EGFR inhibitors has introduced new challenges to the design of phase I, II, and III trials. Both classes of agents can be safely administered at doses sufficient to inhibit the EGFR system. Receptor tyrosine kinase inhibitors have been extensively evaluated in non-small-cell lung cancer. In this setting, gefitinib has demonstrated activity in patients who fail initial chemotherapy. Monoclonal antibodies have been developed in combination with cytotoxic chemotherapy in several tumour types, most notably colorectal and head and neck cancer. The preliminary results suggest an increase in response rate and time to progression with the combination of cetuximab and chemotherapy in both disease models. Future issues in the development of EGFR inhibitors include the identification of biologic predictors of response, combination with other targeted agents, and their utilisation in earlier stage malignancies.
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影响因子：
45.3
作者：
Albanell, J;Rojo, F;Baselga, J
通讯作者：
Baselga, J
影响因子：
45.3
作者：
Baselga, J;Rischin, D;Albanell, J
通讯作者：
Albanell, J
影响因子：
6.4
作者：
Ciardiello, F;Caputo, R;Tortora, G
通讯作者：
Tortora, G
影响因子：
5.8
作者：
Curnow, RT
通讯作者：
Curnow, RT
影响因子：
45.3
作者：
Hirsch, FR;Varella-Garcia, M;Franklin, WA
通讯作者：
Franklin, WA