2017 Volume 57 Issue 2 Pages 69-74
Lung cancers with epidermal growth factor receptor (EGFR) gene mutations are a common malignancy in East-Asians, including Japanese. Although there have been recent dramatic developments in cancer immunotherapy, EGFR-mutant lung cancers are reported to be relatively refractory to these immunotherapies. Thus, EGFR tyrosine kinase inhibitors (EGFR-TKIs) are still the sole key drug for those patients. After the discovery that an EGFR T790M secondary mutation is the most frequent mechanism of acquired resistance, several agents that simultaneously target this mutation are being developed, and osimertinib has already been approved in Japan. In addition, basic and translational research has revealed many mechanisms underlying resistance to EGFR-TKI. In this review, we will summarize the history of EGFR-TKIs and the detailed data for recently developed EGFR-TKIs. In addition, we discuss the possibility of combined therapies using EGFR-TKIs, based on the basic, translational, and clinical findings.
