Successful treatment of non-small cell lung cancer with gefitinib after severe erlotinib-related hepatotoxicity

Intern Med. 2012;51(4):431-4. doi: 10.2169/internalmedicine.51.6285. Epub 2012 Feb 15.


Gefitinib and erlotinib are first-generation small molecular inhibitors of EGFR tyrosine kinase activity. To the best of our knowledge, to date, two reports have stated that patients with NSCLC who develop severe hepatotoxicity secondary to gefitinib treatment can be safely switched to erlotinib. However, the reverse situation has not been reported. Here, we present the first case with non-small cell lung cancer harboring EGFR mutation who developed grade 3/4 hepatotoxicity after initiation of erlotinib, which resolved when therapy was changed to gefitinib. As far as we know, this is the first report showing the efficacy of gefitinib for a non-small cell lung cancer patient who developed severe hepatotoxicity while under erlotinib therapy.

Publication types

  • Case Reports

MeSH terms

  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / therapeutic use
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Chemical and Drug Induced Liver Injury / etiology*
  • Erlotinib Hydrochloride
  • Female
  • Gefitinib
  • Humans
  • Middle Aged
  • Protein Kinase Inhibitors / adverse effects*
  • Protein Kinase Inhibitors / therapeutic use
  • Quinazolines / adverse effects*
  • Quinazolines / therapeutic use*
  • Treatment Outcome


  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Quinazolines
  • Erlotinib Hydrochloride
  • Gefitinib