Small Molecules in Oncology

Gefitinib

Small Molecules in Oncology

Recent results in cancer research Fortschritte der Krebsforschung Progrès dans les recherches sur le cancer, January 2018

30069771

978-3-31-991441-1, 978-3-31-991442-8

Justyna Rawluk, Cornelius F. Waller, Rawluk, Justyna, Waller, Cornelius F.

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.