Mutations of the epidermal growth factor receptor in non-small cell lung cancer – Search and destroy

The targeting of the ATP binding pocket of the epidermal growth factor receptor (EGFR) tyrosine kinase, by the small molecule drugs gefitinib and erlotinib, represents a promising new therapeutic strategy in non-small cell lung cancer. However, it is now apparent that only a subset of patients respo...

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Bibliographic Details
Published in:European journal of cancer (1990) 2006, Vol.42 (1), p.17-23
Main Authors: Chan, S.K., Gullick, W.J., Hill, M.E.
Format: Article
Language:English
Subjects:
Biological and medical sciences
Carcinoma, Non-Small-Cell Lung - genetics
Carcinoma, Non-Small-Cell Lung - therapy
EGFR
Erlotinib
Erlotinib Hydrochloride
Female
Gefitinib
Genes, erbB-1 - genetics
Genetic Therapy - methods
Humans
Lung Neoplasms - genetics
Male
Medical sciences
Mutation
Mutation - genetics
NSCLC
Pharmacology. Drug treatments
Protein Kinase Inhibitors - therapeutic use
Protein-Tyrosine Kinases - antagonists & inhibitors
Quinazolines - therapeutic use
Targeted therapy
Tumors
Tyrosine kinase
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Summary:The targeting of the ATP binding pocket of the epidermal growth factor receptor (EGFR) tyrosine kinase, by the small molecule drugs gefitinib and erlotinib, represents a promising new therapeutic strategy in non-small cell lung cancer. However, it is now apparent that only a subset of patients responds to such treatment. Two publications in early 2004 reported the presence of activating mutations in the EGFR tyrosine kinase gene conferring exquisite sensitivity to these drugs. Several publications have since reported prospective data consistent with this finding. This brief review summarises the mutation data from 15 such studies in terms of mutation frequency by clinicopathological features and correlation with response to tyrosine kinase inhibition. A new paradigm for the routine detection of such mutations is needed to facilitate patient selection for treatment and further studies.
ISSN:0959-8049
1879-0852
DOI:10.1016/j.ejca.2005.07.031