- 作者: Bin-Chi Liao, Chia-Chi Lin, Jih-Hsiang Lee and James Chih-Hsin Yang
- 作者服務機構: 1. Department of Oncology, National Taiwan University Hospital, 7, Chung-Shan South Road, Taipei 100, Taiwan 2. National Taiwan University Cancer Center, College of Medicine, National Taiwan University, Taipei, Taiwan 3. Graduate Institute of Clinical Medicine, College of Medicine, National Taiwan University, Taipei, Taiwan
- 中文摘要: --
- 英文摘要:
The first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors (1/2G EGFR-TKIs) gefitinib, erlotinib, and afatinib have all been approved as standard first-line treatments for advanced EGFR mutation-positive non-small cell lung cancer. The third-generation (3G) EGFR-TKIs have been developed to overcome the EGFR T790M mutation, which is the most common mechanism of acquired resistance to 1/2G EGFR-TKI treatment. This resistance mutation develops in half of the patients who respond to 1/2G EGFR-TKI therapy. The structures of the novel 3G EGFR-TKIs are different from those of 1/2G EGFR-TKIs. Particularly, 3G EGFR-TKIs have lower affinity to wild-type EGFR, and are therefore associated with lower rates of skin and gastrointestinal toxicities. However, many of the adverse events (AEs) that are observed in patients receiving 3G EGFR-TKIs have not been observed in patients receiving 1/2G EGFR-TKIs. Although preclinical studies have revealed many possible mechanisms for these AEs, the causes of some AEs remain unknown. Many mechanisms of resistance to 3G EGFR-TKI therapy have also been reported. Here, we have reviewed the recent clinical and preclinical developments related to novel 3G EGFR-TKIs, including osimertinib, rociletinib, olmutinib, EGF816, and ASP8273. - 中文關鍵字: --
- 英文關鍵字: Non-small cell lung cancer, Epidermal growth factor receptor, Tyrosine kinase inhibitor, T790M mutation, Osimertinib, Rociletinib, Olmutinib, EGF816, ASP8273