Wednesday 4 April 2012
The T790M mutation was shown to confer resistance to gefitinib after it was introduced into the sequence of the wild-type EGFR and L858R mutant EGFR in vitro.
The T790M mutation results in steric hindrance of binding of gefitinib to the ATP-kinase–binding pocket.
third-generation epidermal growth factor receptor (EGFR ) tyrosine kinase inhibitor (TKIs )
Sequist LV, Goldman JW, Wakelee HA, et al. Efficacy of rociletinib (CO-1686) in plasma-genotyped T790M-positive non-small cell lung cancer (NSCLC) patients (pts). J Clin Oncol. 2015;33 (suppl; abstr 8001).
Detection of EGFR T790M mutation in plasma DNA from patients refractory to EGFR tyrosine kinase inhibitor. Sakai K, Horiike A, Irwin DL, Kudo K, Fujita Y, Tanimoto A, Sakatani T, Saito R, Kaburaki K, Yanagitani N, Ohyanagi F, Nishio M, Nishio K. Cancer Sci. 2013 May 31. doi : 10.1111/cas.12211 PMID: 23721103
Challenges of detecting EGFR T790M in gefitinib/erlotinib-resistant tumours. Jänne PA. Lung Cancer. 2008 Jun;60 Suppl 2:S3-9. PMID: 18513582
Screening for germline EGFR T790M mutations through lung cancer genotyping. Oxnard GR, Miller VA, Robson ME, Azzoli CG, Pao W, Ladanyi M, Arcila ME. J Thorac Oncol. 2012 Jun;7(6):1049-52. doi : 10.1097/JTO.0b013e318250ed9d PMID: 22588155