title: Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.
abstract: The tyrosine kinase inhibitors (TKI) against epidermal growth factor receptor (EGFR) are widely used in patients with non-small cell lung cancer (NSCLC). However, EGFR T790M mutation leads to resistance to most clinically available EGFR TKIs. Third-generation EGFR TKIs against the T790M mutation have been in active clinical development. These agents include osimertinib, rociletinib, HM61713, ASP8273, EGF816, and PF-06747775. Osimertinib and rociletinib have shown clinical efficacy in phase I/II trials in patients who had acquired resistance to first- or second-generation TKIs. Osimertinib (AZD9291, TAGRISSO) was recently approved by FDA for metastatic EGFR T790M mutation-positive NSCLC. HM61713, ASP8237, EGF816, and PF-06747775 are still in early clinical development. This article reviews the emerging data regarding third-generation agents against EGFR T790M mutation in the treatment of patients with advanced NSCLC.
authors.affiliation: The Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Peking University Cancer Hospital, Beijing, China.
authors.forename: Shuhang
authors.initials: S
authors.lastname: Wang
authors.affiliation: Department of Oncology, People's Hospital of Henan Province, Zhengzhou University, Zhengzhou, China.
authors.forename: Shundong
authors.initials: S
authors.lastname: Cang
authors.affiliation: Department of Oncology, Henan Cancer Hospital, Zhengzhou University, Zhengzhou, China. delong_liu@nymc.edu.|Henan Cancer Hospital, Zhengzhou University, Zhengzhou, China. delong_liu@nymc.edu.
authors.forename: Delong
authors.initials: D
authors.lastname: Liu
mesh_terms: D000178:Acrylamides / Q000627:therapeutic use; D000814:Aniline Compounds; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D002986:Clinical Trials as Topic; D019008:Drug Resistance, Neoplasm / Q000187:drug effects / Q000235:genetics; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000235:genetics; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D020125:Mutation, Missense; D010879:Piperazines / Q000627:therapeutic use; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011743:Pyrimidines / Q000627:therapeutic use; D007211:Indoles
chemical_list: D000178:Acrylamides; D000814:Aniline Compounds; D066246:ErbB Receptors; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; C000596361:osimertinib; D007211:Indoles; C000589977:rociletinib