Gilotrif is a tyrosine kinase inhibitor that blocks proteins that promote the development of cancerous cells. It is intended for patients whose tumors express the EGFR exon 19 deletions or exon 21 L858R substitution gene mutations. Gilotrif is being approved concurrently with the screen EGFR RGQ PCR Kit, a companion diagnostic that helps determine if a patient’s lung cancer cells express the EGFR mutations. This drug also targets other receptors, such as HER2 (ErbB2). National Cancer Comprehensive Network (NCCN) also recommends the use of Gilotrif in patients with NSCLC that have activity against HER2 mutations or a known sensitizing EGFR mutation
Yang, JC; Wu, YL; Schuler, M; Sebastian, M; Popat, S; Yamamoto, N; Zhou, C; Hu, CP; O’Byrne, K; Feng, J; Lu, S; Huang, Y; Geater, SL; Lee, KY; Tsai, CM; Gorbunova, V; Hirsh, V; Bennouna, J; Orlov, S; Mok, T; Boyer, M; Su, WC; Lee, KH; Kato, T; Massey, D; Shahidi, M; Zazulina, V; Sequist, LV (February 2015). “Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials.”. The Lancet. Oncology. 16 (2): 141–51.
Afatinib, prescribing information 2017
NCCN Lung Cancer 2016