title: Osimertinib making a breakthrough in lung cancer targeted therapy.
abstract: Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are the evidence-based first-line treatment for advanced non-small-cell lung cancer that harbors sensitizing EGFR mutations (EGFRm(+)) such as exon 19 deletions and L858R substitutions in exon 21. However, acquired resistance to EGFR TKIs is mostly driven by a second-site EGFR T790M mutation, which negates their inhibitory activity. Osimertinib (AZD9291, Tagrisso™), an oral, third-generation EGFR TKI, has been designed to target the EGFR T790M mutation, while sparing wild-type EGFR. In this up-to-date review, focus is not only on the structure, mechanisms, and pharmacokinetics of osimertinib but also on summarizing clinical trials and making recommendations of osimertinib for patients with non-small-cell lung cancer.
authors.affiliation: Department of Oncology, Zhongda Hospital, Medical School, Southeast University, Nanjing, People's Republic of China.
authors.forename: Haijun
authors.initials: H
authors.lastname: Zhang
keywords: T790M mutation; epidermal growth factor receptor; non-small cell lung cancer; osimertinib; tyrosine kinase inhibitors