Targeting the epidermal growth factor receptor in egfr-mutated lung cancer: Current and emerging therapies

Karam Khaddour*, Sushma Jonna, Alexander Deneka, Jyoti D. Patel, Mohamed E. Abazeed, Erica Golemis, Hossein Borghaei, Yanis Boumber*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

35 Scopus citations


Epidermal growth factor receptor-targeting tyrosine kinase inhibitors (EGFR TKIs) are the standard of care for patients with EGFR-mutated metastatic lung cancer. While EGFR TKIs have initially high response rates, inherent and acquired resistance constitute a major challenge to the longitudinal treatment. Ongoing work is aimed at understanding the molecular basis of these resistance mechanisms, with exciting new studies evaluating novel agents and combination therapies to improve control of tumors with all forms of EGFR mutation. In this review, we first provide a discussion of EGFR-mutated lung cancer and the efficacy of available EGFR TKIs in the clinical setting against both common and rare EGFR mutations. Second, we discuss common resistance mechanisms that lead to therapy failure during treatment with EGFR TKIs. Third, we review novel approaches aimed at improving outcomes and overcoming resistance to EGFR TKIs. Finally, we highlight recent breakthroughs in the use of EGFR TKIs in non-metastatic EGFR-mutated lung cancer.

Original languageEnglish (US)
Article number3164
Issue number13
StatePublished - Jul 1 2021


  • Adenocarcinoma
  • EGFR
  • Lung cancer
  • Overall survival
  • Progression-free survival
  • Tyrosine kinase inhibitors

ASJC Scopus subject areas

  • Oncology
  • Cancer Research


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