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Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
Published on: June 26, 2019
Afatinib-refractory brain metastases from EGFR-mutant non-small-cell lung cancer successfully controlled with
Yoshikane Nonagase1, Kunio Okamoto, Tsutomu Iwasa
1aDepartment of Medical Oncology, Kinki University Faculty of Medicine bDepartment of Medical Oncology, Kishiwada City Hospital, Osaka, Japan.
Abstract:
Both afatinib and erlotinib are tyrosine kinase inhibitors that inhibit aberrant epidermal growth factor receptor (EGFR) signals in non-small-cell lung cancer (NSCLC). Afatinib is an irreversible inhibitor directed against EGFR, ErbB-2, and ErbB-4, whereas erlotinib is a reversible inhibitor directed against EGFR only. Although afatinib has been shown to be effective in the treatment for erlotinib-refractory and/or gefitinib-refractory central nervous system metastases from NSCLC, little is known about the efficacy of erlotinib for afatinib-refractory central nervous system metastases. In the present report we describe a case of EGFR mutation-positive NSCLC in which brain metastases developed during first-line afatinib treatment. Whole-brain radiation therapy and substitution of erlotinib for afatinib led to successful shrinkage of the brain metastases. Our report highlights the potential benefit of erlotinib for the management of brain metastases refractory over afatinib in patients with NSCLC.
Insights
Afatinib and erlotinib treat non-small-cell lung cancer (NSCLC) brain metastases. Erlotinib showed efficacy in a case of afatinib-refractory central nervous system metastases, suggesting its potential benefit.
Area of Science:
- Oncology
- Pharmacology
Background:
- Afatinib and erlotinib are tyrosine kinase inhibitors targeting epidermal growth factor receptor (EGFR) in non-small-cell lung cancer (NSCLC).
- Afatinib irreversibly inhibits EGFR, ErbB-2, and ErbB-4, while erlotinib reversibly inhibits EGFR only.
- Limited data exists on erlotinib's efficacy for afatinib-refractory central nervous system (CNS) metastases in NSCLC.
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