Deeks Emma D, Keating Gillian M
Springer, Private Bag 65901, Mairangi Bay, 0754 Auckland, New Zealand.
Drugs Ther Perspect. 2018;34(3):89-98. doi: 10.1007/s40267-018-0482-6. Epub 2018 Feb 1.
Afatinib [Giotrif (EU); Gilotrif (USA)] is an orally administered, irreversible inhibitor of the ErbB family of tyrosine kinases that provides an important first-line treatment option for advanced non-small cell lung cancer (NSCLC) with activating epidermal growth factor receptor (EGFR) mutations (i.e. EGFR), and an additional treatment option for squamous NSCLC that has progressed following first-line platinum-based chemotherapy. Relative to gefitinib in the first-line treatment of EGFR advanced lung adenocarcinoma, afatinib prolonged progression-free survival (PFS) and time to treatment failure (TTF), but not overall survival (OS). Afatinib also prolonged PFS, but not OS, versus cisplatin-based chemotherapy in this setting; however, afatinib improved OS versus chemotherapy in the subgroup of patients with deletions in exon 19. As a second-line treatment for advanced squamous NSCLC, afatinib prolonged PFS and OS compared with erlotinib, regardless of EGFR mutation status. Afatinib had a predictable and manageable tolerability profile.
阿法替尼[妥复克（欧盟）；吉泰瑞（美国）]是一种口服的不可逆表皮生长因子受体（EGFR）家族酪氨酸激酶抑制剂，为携带激活型EGFR突变的晚期非小细胞肺癌（NSCLC）提供了重要的一线治疗选择，也是一线铂类化疗后进展的鳞状NSCLC的额外治疗选择。相对于吉非替尼用于EGFR阳性晚期肺腺癌的一线治疗，阿法替尼延长了无进展生存期（PFS）和至治疗失败时间（TTF），但未延长总生存期（OS）。在此情况下，与基于顺铂的化疗相比，阿法替尼也延长了PFS，但未延长OS；然而，在第19外显子缺失的患者亚组中，阿法替尼相对于化疗改善了OS。作为晚期鳞状NSCLC的二线治疗，无论EGFR突变状态如何，与厄洛替尼相比，阿法替尼延长了PFS和OS。阿法替尼具有可预测且可控的耐受性。
