阿法替尼和厄洛替尼治疗鳞状细胞肺癌。

Afatinib and Erlotinib in the treatment of squamous-cell lung cancer.

机构信息

a Lung Cancer Unit , Ospedale Policlinico San Martino , Genoa , Italy.

b Department of Internal Medicine and Medical Specialties (DIMI) , University of Genoa , Genoa , Italy.

出版信息

Expert Opin Pharmacother. 2018 Dec;19(18):2055-2062. doi: 10.1080/14656566.2018.1540591. Epub 2018 Nov 3.

Abstract

INTRODUCTION

Squamous-cell carcinoma (SCC) of the lung represents around 20% of non-small cell lung cancers. Although activating mutations of EGFR are rare in this subtype, its overexpression occurs in more than half the cases. Consequently, many epidermal growth factor receptor (EGFR)-targeted agents have been investigated in patients with SCC.

AREAS COVERED

This review summarizes the potential roles of erlotinib and afatinib in SCC of the lung. The authors explore the rationale of targeting EGFR in SCC and the pharmacological properties of erlotinib and afatinib. Subsequently, they describe the most relevant clinical data involving each agent with regard to their safety profile and antineoplastic activity. Particular focus is given to the LUX-Lung 8 trial, which compared erlotinib and afatinib as a second-line treatment in a population of patients affected by advanced SCC of the lung.

EXPERT OPINION

Despite being overcome by new therapeutic strategies - in particular immune checkpoint inhibitors - afatinib and erlotinib still represent potential treatment options down the line in lung SCC because they have a more manageable toxicity profile compared to chemotherapy.

摘要

简介

肺鳞状细胞癌(SCC)约占非小细胞肺癌的 20%。虽然该亚型中 EGFR 的激活突变较为罕见,但超过一半的病例存在 EGFR 过表达。因此,已有许多表皮生长因子受体(EGFR)靶向药物在 SCC 患者中进行了研究。

涵盖领域

本文综述了厄洛替尼和阿法替尼在肺 SCC 中的潜在作用。作者探讨了针对 SCC 中 EGFR 的作用机制,以及厄洛替尼和阿法替尼的药理学特性。随后,作者描述了每个药物的最相关临床数据,包括安全性概况和抗肿瘤活性。特别关注 LUX-Lung 8 试验,该试验比较了厄洛替尼和阿法替尼作为二线治疗在晚期肺 SCC 患者中的疗效。

专家意见

尽管新的治疗策略(特别是免疫检查点抑制剂)已经取得进展,但阿法替尼和厄洛替尼仍可能成为肺 SCC 的后续治疗选择,因为与化疗相比,它们具有更易于管理的毒性特征。

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