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非小细胞肺癌中的新型表皮生长因子受体抑制剂:阿法替尼的现状

Novel EGFR Inhibitors in Non-small Cell Lung Cancer: Current Status of Afatinib.

作者信息

Liao Bin-Chi, Lin Chia-Chi, Yang James Chih-Hsin

机构信息

Department of Oncology, National Taiwan University Hospital, 7, Chung-Shan South Road, Taipei, Taiwan.

National Taiwan University Cancer Center, College of Medicine, National Taiwan University, Taipei, Taiwan.

出版信息

Curr Oncol Rep. 2017 Jan;19(1):4. doi: 10.1007/s11912-017-0560-2.

DOI:10.1007/s11912-017-0560-2
PMID:28138934
Abstract

Afatinib, a second-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, has been approved worldwide as a first-line treatment for advanced non-small cell lung cancer (NSCLC) that harbors activating EGFR mutations. Here, we have reviewed the recent clinical developments in the treatment of lung cancer using afatinib. Emerging data have revealed the overall survival benefit of first-line afatinib therapy in patients with advanced EGFR -positive NSCLC. Phase III studies of afatinib have shown the effectiveness of afatinib as a second-line treatment for advanced lung squamous cell carcinoma, as well as the benefit of continuing afatinib therapy in combination with cytotoxic chemotherapy for advanced NSCLC after the occurrence of disease progression in patients who are receiving afatinib monotherapy. Therapeutic benefits of afatinib have also been reported in studies of patients with central nervous system metastasis and patients with HER2 mutation. The utility of afatinib-based combination therapies is being investigated in ongoing research.

摘要

阿法替尼是一种第二代表皮生长因子受体(EGFR)酪氨酸激酶抑制剂,已在全球范围内被批准作为一线治疗药物,用于治疗携带激活型EGFR突变的晚期非小细胞肺癌(NSCLC)。在此,我们回顾了使用阿法替尼治疗肺癌的近期临床进展。新出现的数据显示,一线使用阿法替尼治疗对晚期EGFR阳性NSCLC患者具有总生存获益。阿法替尼的III期研究表明,阿法替尼作为晚期肺鳞状细胞癌的二线治疗药物是有效的,并且对于接受阿法替尼单药治疗后疾病进展的晚期NSCLC患者,继续将阿法替尼与细胞毒性化疗联合使用也有益处。在中枢神经系统转移患者和HER2突变患者的研究中也报道了阿法替尼的治疗益处。目前正在进行的研究中,正在探究以阿法替尼为基础的联合疗法的效用。

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本文引用的文献

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Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.剂量调整对阿法替尼治疗表皮生长因子受体突变阳性肺腺癌的安全性和疗效的影响:随机 LUX-Lung 3 和 6 试验的事后分析。
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Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): a phase 2B, open-label, randomised controlled trial.阿法替尼对比吉非替尼用于治疗表皮生长因子受体突变阳性的非小细胞肺癌患者的一线治疗(LUX-Lung 7):一项 2B 期、开放标签、随机对照临床试验。
Lancet Oncol. 2016 May;17(5):577-89. doi: 10.1016/S1470-2045(16)30033-X. Epub 2016 Apr 12.
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成功靶向融合显示肺腺癌对阿法替尼有持久反应:一例报告
Ann Transl Med. 2021 Oct;9(19):1507. doi: 10.21037/atm-21-3923.
4
Real-world effectiveness of second-line Afatinib versus chemotherapy for the treatment of advanced lung squamous cell carcinoma in immunotherapy-naïve patients.二线阿法替尼对比化疗治疗免疫治疗初治的晚期肺鳞癌的真实世界疗效。
BMC Cancer. 2021 Nov 15;21(1):1225. doi: 10.1186/s12885-021-08920-3.
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Crit Rev Oncol Hematol. 2016 Apr;100:107-16. doi: 10.1016/j.critrevonc.2016.01.024. Epub 2016 Jan 25.
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J Thorac Oncol. 2016 Mar;11(3):380-90. doi: 10.1016/j.jtho.2015.11.014. Epub 2016 Jan 25.
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Clin Cancer Res. 2016 May 1;22(9):2139-45. doi: 10.1158/1078-0432.CCR-15-1653. Epub 2015 Dec 14.
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Afatinib beyond progression in patients with non-small-cell lung cancer following chemotherapy, erlotinib/gefitinib and afatinib: phase III randomized LUX-Lung 5 trial.阿法替尼用于经化疗、厄洛替尼/吉非替尼及阿法替尼治疗后病情进展的非小细胞肺癌患者:III期随机LUX-Lung 5试验
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