Afatinib – drug profile

05/2017

MUDr. Leona Koubková

Pneumologická klinika 2. LF UK a FN v Motole, Praha

SUMMARY

The epidermal growth factor receptor (EGFR) plays an important role in the development and progression of human epithelial carcinomas, including non-small cell lung cancer (NSCLC). Activation of the EGFR pathway promotes tumor growth and progression, stimulates tumor cell proliferation, angiogenic factors, invasion and metastasis, and suppresses apoptosis. Several studies have confirmed the predictive role of activation mutations in EGFR exons 19 and 21 for NSCLC. Their presence is clearly associated with higher efficacy of EGFR tyrosine kinase inhibitors (EGFR TKI). We have reversible EGFR TKI of the 1^st generation erlotinib and gefitinib, the irreversible EGFR TKI 2^nd generation afatinib, and also the already irreversible EGFR TKI 3^rd generation osimertinib, the indication of which is above all the proven T790M mutation.

KEY WORDS

non-small cell lung cancer, mutation of the epidermal growth factor receptor gene, afatinib