Nazartinib in EGFR Thr790Met-mutant non-small-cell lung cancer

Abstract

Mutations in the epidermal growth factor receptor (EGFR) gene are the most common actionable alterations in non-small-cell lung cancer (NSCLC). These abnormalities occur almost exclusively in lung adenocarcinoma, with the prevalence ranging from 10–20% among white patients to 40–55% among patients from the Asia-Pacific region. The development of EGFR tyrosine kinase inhibitors (EGFR TKIs), small molecules that specifically inhibit the downstream EGFR signalling pathway, have launched a new era of personalised therapy for lung cancer, with EGFR TKIs largely replacing chemotherapy for first-line and second-line treatment of EGFR-mutant advanced NSCLC. Subsequently, the family of EGFR TKIs has been supplemented by TKIs blocking other molecular targets, such as ALK, ROS1, RET, and BRAF, with a large potential for further developments. Safety and efficacy of nazartinib (EGF816) in adults with EGFR-mutant non-small-cell lung carcinoma: a multicentre, open-label, phase 1 studyNazartinib has a favourable safety profile, with low-grade skin toxicity characterised by a predominantly maculopapular rash that required minimal dose reductions. Full-Text PDF