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Target Oncol. 2016 Dec;11(6):825-835. doi: 10.1007/s11523-016-0465-2.
Afatinib (Giotrif, Gilotrif) is an orally administered, irreversible inhibitor of the ErbB family of tyrosine kinases. In the first-line treatment of patients with advanced lung adenocarcinoma with activating epidermal growth factor receptor (EGFR) mutations, afatinib significantly prolonged progression-free survival (PFS) and time to treatment failure (TTF), but not overall survival (OS), compared with gefitinib (LUX-Lung 7 trial). In the overall population of patients receiving first-line treatment for advanced lung adenocarcinoma with activating EGFR mutations, afatinib significantly prolonged PFS, but not OS, compared with pemetrexed plus cisplatin (LUX-Lung 3 trial) or gemcitabine plus cisplatin (LUX-Lung 6 trial). However, in both LUX-Lung 3 and LUX-Lung 6, OS was significantly prolonged in the subgroup of patients with deletions in exon 19 receiving afatinib versus chemotherapy. In the second-line treatment of advanced squamous non-small cell lung cancer (NSCLC), afatinib significantly prolonged PFS and OS, compared with erlotinib, regardless of EGFR mutation status (LUX-Lung 8 trial). Afatinib had a predictable and manageable tolerability profile in patients with advanced NSCLC. In conclusion, afatinib is an important option for the first-line treatment of patients with advanced NSCLC and activating EGFR mutations, and provides an additional option for the treatment of patients with squamous NSCLC that has progressed following first-line platinum-based chemotherapy.
阿法替尼（Giotrif，Gilotrif）是一种口服的、不可逆的表皮生长因子受体（EGFR）家族酪氨酸激酶抑制剂。在伴有激活型表皮生长因子受体（EGFR）突变的晚期肺腺癌患者的一线治疗中，与吉非替尼（LUX-Lung 7 试验）相比，阿法替尼显著延长了无进展生存期（PFS）和治疗失败时间（TTF），但未延长总生存期（OS）。在接受一线治疗的伴有激活型 EGFR 突变的晚期肺腺癌患者的总体人群中，与培美曲塞加顺铂（LUX-Lung 3 试验）或吉西他滨加顺铂（LUX-Lung 6 试验）相比，阿法替尼显著延长了 PFS，但未延长 OS。然而，在 LUX-Lung 3 和 LUX-Lung 6 试验中，与化疗相比，接受阿法替尼治疗的 19 号外显子缺失患者亚组的 OS 显著延长。在晚期鳞状非小细胞肺癌（NSCLC）的二线治疗中，与厄洛替尼相比，阿法替尼显著延长了 PFS 和 OS，无论 EGFR 突变状态如何（LUX-Lung 8 试验）。阿法替尼在晚期 NSCLC 患者中具有可预测和可控的耐受性。总之，阿法替尼是治疗伴有激活型 EGFR 突变的晚期 NSCLC 患者的一线治疗的重要选择，为一线铂类化疗后进展的鳞状 NSCLC 患者的治疗提供了另一种选择。
