Afatinib efficacy against squamous cell carcinoma of the head and neck cell lines in vitro and in vivo

Target Oncol. 2015 Dec;10(4):501-8. doi: 10.1007/s11523-014-0353-6. Epub 2015 Jan 6.


Epidermal growth factor receptor (EGFR) inhibitors have demonstrated efficacy in squamous cell carcinoma of the head and neck (SCCHN). In addition to EGFR, other ErbB family members are expressed and activated in SCCHN. Afatinib is an ErbB family blocker that has been approved for treating patients with EGFR-mutated nonsmall cell lung cancer. We sought to determine the efficacy of afatinib in preclinical models and compare this to other EGFR-targeted agents. Afatinib efficacy was characterized in a panel of ten SCCHN cell lines and found to be most effective against cell lines amplified for EGFR. Afatinib had lower IC(50) values than did gefitinib against the same panel. Two EGFR-amplified cell lines that are resistant to gefitinib are sensitive to afatinib. Cetuximab was not found to have a synergistic effect with afatinib either in vitro or in vivo. Both afatinib and cetuximab were effective in tumor xenograft model. Afatinib is an effective agent in SCCHN especially in models with EGFR amplification.

Keywords: Afatinib; Cetuximab; Epidermal growth factor receptor; Gefitinib; Squamous cell carcinoma of the head and neck.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Afatinib
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Carcinoma, Squamous Cell / drug therapy*
  • Cell Line, Tumor
  • Cetuximab / administration & dosage
  • Female
  • Head and Neck Neoplasms / drug therapy*
  • Humans
  • Mice
  • Mice, Nude
  • Quinazolines / administration & dosage
  • Quinazolines / pharmacology*
  • Squamous Cell Carcinoma of Head and Neck
  • Xenograft Model Antitumor Assays


  • Quinazolines
  • Afatinib
  • Cetuximab