Resistance to epidermal growth factor receptor (EGFR) inhibitors in patients with non-small-cell lung cancer (NSCLC) is often caused by acquisition of the T790M mutation in EGFR (EGFR-T790M). Walter et al. have developed a kinase inhibitor, CO-1686, that effectively inhibits EGFR-T790M without affecting wild-type EGFR. CO-1686 reduced tumour growth in several preclinical models of NSCLC, including transgenic mice expressing mutant EGFR and xenograft models. CO-1686 is being tested in Phase I/II clinical trials for EGFR-mutant NSCLC.
References
Walter, A. O. et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. http://dx.doi.org/10.1158/2159-8290.CD-13-0314 (2013)
Rights and permissions
About this article
Cite this article
Seton-Rogers, S. Blocking a mutant. Nat Rev Cancer 13, 757 (2013). https://doi.org/10.1038/nrc3624
Published:
Issue Date:
DOI: https://doi.org/10.1038/nrc3624