Pharmacokinetic drug evaluation of osimertinib for the treatment of non-small cell lung cancer

Antonio Rossi, Lucia Anna Muscarella, Concetta Di Micco, Cristiano Carbonelli, Vito D’alessandro, Stefano Notarangelo, Giuseppe Palomba, Gerardo Sanpaolo, Marco Taurchini, Paolo Graziano, Evaristo Maiello

Research output: Contribution to journalArticlepeer-review


Introduction: First- and second-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib, erlotinib, icotinib, and afatinib are the standard-of-care for first-line therapy of non-small-cell lung cancer (NSCLC) harboring activating EGFR mutations. Unfortunately, after initial activity of an average 9–13 months, disease progression has been reported in the majority of patients. In about 50% of cases the progression is due to the onset of the T790M mutation in exon 20 of the EGFR gene. Third-generation EGFR-TKIs targeting this mutation were investigated, with osimertinib the only reaching clinical practice. Areas covered: A structured search of bibliographic databases for peer-reviewed research literature and of main meetings using a focused review question addressing osimertinib, was undertaken. Expert opinion: Osimertinib is the standard-of-care for EGFR-mutated patients progressing to first-line EGFR-TKIs due to the acquired EGFR T790M mutation. Results from the head-to-head first-line trial comparing osimertinib versus gefitinib or erlotinib in activating EGFR mutations might change the front-line approach. Osimertinib in combination regimens, such as immunotherapy, and in adjuvant setting are ongoing. Thus, the strategic approach for the management of EGFR-mutated NSCLC patients will change further in the next few years.

Original languageEnglish
Pages (from-to)1281-1288
Number of pages8
JournalExpert Opinion on Drug Metabolism and Toxicology
Issue number12
Publication statusPublished - Dec 2 2017


  • Afatinib
  • EGFR
  • erlotinib
  • gefitinib
  • icotinib
  • osimertinib
  • rociletinib
  • T790M
  • ulmutinib

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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