New era of epidermal growth factor receptor-tyrosine kinase inhibitors for lung cancer |
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Authors: | Joana Espiga Macedo |
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Affiliation: | Joana Espiga Macedo, Department of Medical Oncology, Centro Hospitalar de Entre Douro e Vouga, 4520-211 Santa Maria Da Feira, Portugal |
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Abstract: | Lung cancer is the leading cause of death globally, besides recent advances in its management; it maintains a low 5-year survival rate of 15%. The discovery of epidermal growth factor receptor (EGFR) activating mutations and the introduction of its tyrosine kinase inhibitors (TKIs) have expanded the treatment options for patients with non-small cell lung cancer. Nowadays, EGFR mutation testing is now a common routine for newly diagnosed lung cancer. First generation TKIs developed, erlotinib and gefitinib, were reversible ones. After a median of 14 mo, eventually all EGFR mutated patients develop resistance to reversible TKIs. Afatinib, dacomitinib and neratinib, second generation inhibitors, are selective and irreversible TKIs. Finally, third generation phase I clinical trials were performed, with lower toxicity profiles, and targeting with more precision the driving clone of this heterogeneous disease. |
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Keywords: | Epidermal growth factor receptor-tyrosine kinase inhibitors Clonal evolution Non-small cell lung cancer Acquired resistance |
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