AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

@article{Cross2014AZD9291AI,
  title={AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.},
  author={Darren A. E. Cross and Susan Elizabeth Ashton and Serban Ghiorghiu and Cath A Eberlein and Caroline A. Nebhan and Paula J. Spitzler and Jonathon P Orme and M Raymond V Finlay and Richard A. Ward and Martine J. Mellor and Gareth Hughes and Amar Rahi and Vivien N. Jacobs and Monica Red Brewer and Eiki Ichihara and Jing Sun and Hailing Jin and Peter Ballard and Katherine J Al-Kadhimi and Rachel A. Rowlinson and Teresa C M Klinowska and Graham H. P. Richmond and Mireille Cantarini and Dong-Wan Kim and Malcolm Richard Ranson and William Pao},
  journal={Cancer discovery},
  year={2014},
  volume={4 9},
  pages={1046-61}
}
UNLABELLED First-generation EGFR tyrosine kinase inhibitors (EGFR TKI) provide significant clinical benefit in patients with advanced EGFR-mutant (EGFRm(+)) non-small cell lung cancer (NSCLC). Patients ultimately develop disease progression, often driven by acquisition of a second T790M EGFR TKI resistance mutation. AZD9291 is a novel oral, potent, and selective third-generation irreversible inhibitor of both EGFRm(+) sensitizing and T790M resistance mutants that spares wild-type EGFR. This… CONTINUE READING
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