Gefitinib (Iressa) - Genomics: pt has an Exon 19 deletion - effective but resistant mutations can develop. (around 9 months). Mets to: local rib, mediastinum, liver Trials in NZ: https://clinicaltrials.gov/ct2/results?term=lung cancer New Zealand&recr=Open EGFR Exon 19 Deletion in Non-Small Cell Lung Cancer http://www.mycancergenome.org/content/disease/lung-cancer/egfr/21/ EGFR exon 19 deletions are in-frame deletions occurring within exon 19, which encodes part of the kinase domain. This mutation occurs with a frequency of approximately 48% in EGFR mutant lung tumors (Mitsudomi and Yatabe 2010). - Multiple EGFR tyrosine kinase inhibitors (TKIs) have been developed or are in development: First-generation: Gefitinib (Iressa) and erlotinib (Tarceva). Icotinib is another reversible inhibitor like gefitinib and erlotinib that was recently developed and is available only in China. Second-generation: Afatinib (Gilotrif), dacomitinib, neratinib. These are irreversible inhibitors with activity against both EGFR and other ERBB family members. Third-generation: CO-1686, AZD9291. These are mutant-selective as they were designed to target mutant EGFR better than wild type EGFR, while the agents above were originally designed to target wild type EGFR.
