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首页> 外文期刊>Onkologie >Afatinib, Erlotinib and Gefitinib in the first-line therapy of EGFR mutation-positive lung adenocarcinoma: A review
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Afatinib, Erlotinib and Gefitinib in the first-line therapy of EGFR mutation-positive lung adenocarcinoma: A review

机译：阿法替尼，厄洛替尼和吉非替尼用于EGFR突变阳性肺腺癌的一线治疗：综述

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摘要

Non-small cell lung cancer (NSCLC) consists of several histomorphologically defined phenotypes that display an enormous genetic variability. In recent years, epidermal growth factor receptor (EGFR) mutation-positive lung adenocarcinoma has emerged as a unique subset of NSCLC in terms of etiopathogenesis and tumor biology. Since the introduction of the reversible EGFR tyrosine kinase inhibitors (TKIs) erlotinib and gefitinib, patients with metastatic EGFR mutation-positive lung cancer can be offered a therapeutic alternative that has proven its superiority over standard platinum-based chemotherapy. However, primary or acquired resistance limits the therapeutic success of these targeted agents. Irreversible inhibitors targeting all ErbB family receptor tyrosine kinases, such as afatinib and dacomitinib, have been developed to confer sustained disease control in ErbB-dependent cancers. The large LUX-Lung 3 phase III trial recently reported afatinib to be clearly superior over the most effective platinum doublet in patients with EGFR mutation-positive lung cancer. To fully exploit the clinical activity of afatinib, proactive management of its gastrointestinal and dermatologic toxicities is advised.
机译：非小细胞肺癌（NSCLC）由表现出巨大遗传变异性的几种组织形态学定义的表型组成。近年来，就病因和肿瘤生物学而言，表皮生长因子受体（EGFR）突变阳性的肺腺癌已成为NSCLC的独特子集。自从引入可逆性EGFR酪氨酸激酶抑制剂（TKIs）厄洛替尼和吉非替尼以来，可向患有转移性EGFR突变阳性的肺癌患者提供治疗替代方法，已证明其优于标准的铂类化学疗法。但是，原发性或获得性耐药限制了这些靶向药物的治疗成功。已经开发了靶向所有ErbB家族受体酪氨酸激酶的不可逆抑制剂，例如afatinib和dacomitinib，以赋予ErbB依赖性癌症以持续的疾病控制权。最近，一项大型的LUX-Lung 3期III期试验报告称，在EGFR突变阳性的肺癌患者中，afatinib明显优于最有效的铂类双重药物。为了充分利用阿法替尼的临床活性，建议积极管理其胃肠道和皮肤毒性。

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