Irreversible tyrosine kinase inhibition of epidermal growth factor receptor with afatinib in EGFR activating mutation–positive advanced non-small-cell lung cancer

Current oncology

S. Morin-Ben Abdallah¹ 

[1] McGill University Health Centre

关键词: Non-small-cell lung cancer;    nsclc;    epidermal growth factor receptor;    egfr;    tyrosine kinase inhibitors;    tkis;    afatinib;   

DOI  :  10.3747/co.25.3732

学科分类：肿瘤学

来源: Multimed, Inc.

【 摘 要 】

Despite recent advances in the systemic therapy of non-small-cell lung cancer (nsclc), the prognosis for stage iv disease remains poor. The discovery of targetable mutations has led to new treatment options. The most common mutations, theEGFRactivating mutations, are present in about 50% of Asian patients and up to 15% of white patients. First-generation reversible epidermal growth factor receptor (egfr) tyrosine kinase inhibitors (tkis) have led to improved survival in patients positive forEGFRactivating mutations, but resistance eventually leads to disease progression. The irreversible egfr tki afatinib was developed to counter such resistance. The clinical efficacy of afatinib has been shown in first-line studies comparing it with both cytotoxic chemotherapy and first-generation egfr tkis. Afatinib has also shown continued benefit beyond progression while a patient is taking an egfr inhibitor. Furthermore, its toxicity profile is both predictable and manageable. The results of the principal clinical trials assessing afatinib are reviewed here.

【 授权许可】

Unknown