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Updated: Feb 7, 2026
Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure
Published on: August 11, 2017
Gefitinib
Justyna Rawluk1, Cornelius F Waller2
1Department of Haematology, Oncology and Stem Cell Transplantation, University Medical Centre Freiburg, Faculty of Medicine, University of Freiburg, Hugstetter Str. 55, 79106, Freiburg, Germany.
Abstract:
Gefitinib is an orally active selective inhibitor epidermal growth factor receptor (EGFR). The large randomised phase III IPASS study (gefitinib 250 mg, daily vs carboplatin and paclitaxel) showed a beneficial effect on progression-free survival (PFS) and quality of life in selected patient populations under the treatment with gefitinib (HR for TKI 0.74; 95% CI: 0.65-0.85). In the subgroup of patients with EGFR mutation the effect of gefitinib on PFS was notably, PFS HR 0.48; 95% CI: 0.36-0.64, p < 0.001) and the objective response rate (RR) was 71.2% with gefitinib versus 47.3% with chemotherapy. However no significant difference of overall survival was found. Based on this study gefitinib was approved for the first-line treatment of the patients with non-small cell lung cancer (NSCLC) with sensitising EGFR mutations (exon 19 deletion or L858R point mutation). Gefitinib is metabolized in the liver. Most of the adverse effects of gefitinib, such as rash, dry skin and diarrhoe, are mild to moderate in severity and are reversible.
