Afatinib in the treatment of head and neck squamous cell carcinoma

Expert Opin Investig Drugs. 2014 Jan;23(1):135-43. doi: 10.1517/13543784.2014.858696. Epub 2013 Nov 25.


Introduction: Head and neck squamous cell carcinoma (HNSCC) is the sixth most common cause of cancer death in the United States. Treatment of locally advanced disease is associated with significant acute side effects and can lead to chronic disabilities, while the prognosis of recurrent or metastatic disease is very poor. This highlights the need for better therapeutic options. Epidermal growth factor receptor is overexpressed in 90% of HNSCC patients and is an attractive therapeutic target in this patient population. Afatinib is a potent, irreversible pan-ErbB inhibitor. Preliminary studies in HNSCC show promising activity.

Areas covered: This article reviews the current data evaluating small molecules inhibitors of the ErbB family in the treatment of HNSCC with a specific emphasis on afatinib, a second-generation, irreversible, pan-ErbB inhibitor. It also provides a description of afatinib's drug characteristics, pharmacokinetics and toxicity profile as well as details of the published and ongoing clinical trials evaluating its efficacy in HNSCC patients.

Expert opinion: Phase II trials in HNSCC show that daily oral treatment with afatinib is tolerable. Most common toxicities are skin rash and diarrhea. Afatinib has clinical activity as a single agent in a subset of refractory and/or metastatic HNSCC patients. It is thought that ongoing Phase III trials should better clarify the role of this compound in the treatment of HNSCC.

Publication types

  • Review

MeSH terms

  • Afatinib
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Carcinoma, Squamous Cell / drug therapy*
  • ErbB Receptors / antagonists & inhibitors
  • Head and Neck Neoplasms / drug therapy*
  • Humans
  • Protein Kinase Inhibitors / adverse effects
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • Quinazolines / adverse effects
  • Quinazolines / pharmacology
  • Quinazolines / therapeutic use*
  • Squamous Cell Carcinoma of Head and Neck
  • Treatment Outcome


  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Quinazolines
  • Afatinib
  • ErbB Receptors