Update on recent preclinical and clinical studies of T790M mutant-specific irreversible epidermal growth factor receptor tyrosine kinase inhibitors

摘要: The first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors (1/2G EGFR-TKIs) gefitinib, erlotinib, afatinib have all been approved as standard first-line treatments for advanced EGFR mutation-positive non-small cell lung cancer. third-generation (3G) EGFR-TKIs developed to overcome the T790M mutation, which is most common mechanism of acquired resistance 1/2G EGFR-TKI treatment. This mutation develops in half patients who respond therapy. structures novel 3G are different from those EGFR-TKIs. Particularly, lower affinity wild-type EGFR, therefore associated with rates skin gastrointestinal toxicities. However, many adverse events (AEs) that observed receiving not Although preclinical studies revealed possible mechanisms these AEs, causes some AEs remain unknown. Many therapy also reported. Here, we reviewed recent clinical developments related EGFR-TKIs, including osimertinib, rociletinib, olmutinib, EGF816, ASP8273.