Erlotinib accumulation in brain metastases from non-small cell lung cancer: visualization by positron emission tomography in a patient harboring a mutation in the epidermal growth factor receptor

J Thorac Oncol. 2011 Jul;6(7):1287-9. doi: 10.1097/JTO.0b013e318219ab87.


Introduction: Drugs directed toward the epidermal growth factor receptor (EGFR), such as erlotinib (Tarceva®) and gefitinib (Iressa®), are used for the treatment of patients with advanced non-small cell lung cancer (NSCLC), including patients with brain metastases. However, whether erlotinib actually enters into brain metastases has not been adequately elucidated. In this study, we investigated the accumulation of [¹¹C]-erlotinib by positron emission tomography (PET) combined with computed tomography (CT) and magnetic resonance imaging (MRI).

Methods: A 32-year-old patient with NSCLC and multiple brain metastases was treated with first-line erlotinib. EGFR mutations were determined by analyzing a fine-needle lung tumor biopsy taken before the treatment. A PET/CT of the brain with [¹¹C]-erlotinib was performed during treatment, and a MRI of the head and a CT of the chest were performed pre- and posttreatment.

Results: The primary lung tumor displayed an erlotinib-sensitizing exon 19 deletion in the EGFR gene, and [¹¹C]-erlotinib PET/CT showed accumulation in the brain metastases. Posttreatment MRI and CT demonstrated regression of both brain metastases and primary lung tumor.

Conclusion: Our data demonstrated that erlotinib accumulated in brain metastases in a NSCLC patient who responded to the treatment.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Brain Neoplasms / diagnostic imaging*
  • Brain Neoplasms / drug therapy
  • Brain Neoplasms / genetics*
  • Brain Neoplasms / secondary
  • Carcinoma, Non-Small-Cell Lung / diagnostic imaging*
  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Carcinoma, Non-Small-Cell Lung / genetics*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Drug Resistance, Neoplasm / genetics*
  • ErbB Receptors / genetics*
  • Erlotinib Hydrochloride
  • Female
  • Humans
  • Lung Neoplasms / diagnostic imaging
  • Lung Neoplasms / drug therapy
  • Lung Neoplasms / genetics
  • Lung Neoplasms / pathology
  • Mutation / genetics*
  • Neoplasm Staging
  • Positron-Emission Tomography
  • Prognosis
  • Protein Kinase Inhibitors / pharmacology
  • Quinazolines / pharmacology*
  • Survival Rate
  • Tomography, X-Ray Computed


  • Protein Kinase Inhibitors
  • Quinazolines
  • Erlotinib Hydrochloride
  • EGFR protein, human
  • ErbB Receptors