Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib by Costa Daniel B, Nguyen Kim-Son H, Cho Byoung C, Sequist Lecia V, Jackman David M, Riely Gregory J, Yeap Beow Y, Halmos Balázs, Kim Joo H, Jänne Pasi A, Huberman Mark S, Pao William, Tenen Daniel G, Kobayashi Susumu in Clinical cancer research : an official journal of the American Association for Cancer Research (2008).

[PMID: 18981003] PubMed


Most lung cancers with activating epidermal growth factor receptor (EGFR) mutations respond to gefitinib; however, resistance to this tyrosine kinase inhibitor (TKI) invariably ensues. The T790M mutation occurs in 50% and MET amplification in 20% of TKI-resistant tumors. Other secondary mutations (D761Y and L747S) are rare. Our goal was to determine the effects of erlotinib 150 mg/d in EGFR mutated patients resistant to gefitinib 250 mg/d, because the EGFR TKI erlotinib is given at a higher biologically active dose than gefitinib.

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