Afatinib in advanced NSCLC: a profile of its use.

Afatinib in advanced NSCLC: a profile of its use.
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DOI:
10.1007/s40267-018-0482-6
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发表时间:
2018
期刊:
Drugs & therapy perspectives : for rational drug selection and use
影响因子:
--
通讯作者:
Keating GM
Keating GM
中科院分区:
其他
文献类型:
--
作者:
Deeks ED;Keating GM

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阿法替尼 [Giotrif®(欧盟); Gilotrif®(美国)]是一种口服、不可逆的酪氨酸激酶 ErbB 家族抑制剂,为具有激活表皮生长因子受体(EGFR)突变(即 EGFRactMUT+)的晚期非小细胞肺癌(NSCLC)提供重要的一线治疗选择,并为一线铂类化疗后进展的鳞状 NSCLC 提供额外的治疗选择。相对于一线治疗 EGFRactMUT+ 晚期肺腺癌的吉非替尼,阿法替尼延长了无进展生存期 (PFS) 和治疗失败时间 (TTF),但没有延长总生存期 (OS)。在此情况下,与基于顺铂的化疗相比,阿法替尼还延长了 PFS,但没有延长 OS;然而,在外显子 19 缺失的患者亚组中,阿法替尼与化疗相比改善了 OS。作为晚期鳞状 NSCLC 的二线治疗,与厄洛替尼相比,阿法替尼延长了 PFS 和 OS,无论 EGFR 突变状态如何。阿法替尼具有可预测且可管理的耐受性。
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. EGFRactMUT+), 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 EGFRactMUT+ 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.