18F-EF5: a new PET tracer for imaging hypoxia in head and neck cancer

J Nucl Med. 2008 Dec;49(12):1944-51. doi: 10.2967/jnumed.108.053785. Epub 2008 Nov 7.

Abstract

The aim of this study was to evaluate 2-(2-nitro-(1)H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl)-acetamide (EF5) labeled with (18)F-fluorine to image hypoxia in patients with squamous cell carcinoma of the head and neck (HNSCC).

Methods: Fifteen patients with HNSCC were studied. Measurement of tumor blood flow was followed by an (18)F-EF5 PET/CT scan. On a separate day, (18)F-FDG PET/CT was performed to determine the metabolically active tumor volume. In 6 patients, dynamic (18)F-EF5 images of the head and neck area were acquired, followed by static images acquired at 1, 2, and 3 h after injection. In the remaining 9 patients, only static images were obtained. (18)F-EF5 uptake in tumors was compared with that in neck muscle, and the (18)F-EF5 findings were correlated with the (18)F-FDG PET/CT studies.

Results: A total of 13 primary tumors and 5 lymph node metastases were evaluated for their uptake of (18)F-EF5. The median tumor-to-muscle (18)F-EF5 uptake ratio (T/M) increased over time and was 1.38 (range, 1.1-3.2) 3 h after tracer injection. The median blood flow in tumors was 36.7 mL/100 g/min (range, 23.3-78.6 mL/100 g/min). Voxel-by-voxel analysis of coregistered blood flow and (18)F-EF5 images revealed a distinct pattern, resulting in a T/M of 1.5 at 3 h to be chosen as a cutoff for clinically significant hypoxia. Fourteen of 18 tumors (78%) had subvolumes within the metabolically active tumor volumes with T/M greater than or equal to 1.5.

Conclusion: On the basis of these data, the potential of (18)F-EF5 to detect hypoxia in HNSCC is encouraging. Further development of (18)F-EF5 for eventual targeting of antihypoxia therapies is warranted.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Carcinoma, Small Cell / diagnostic imaging*
  • Carcinoma, Small Cell / metabolism*
  • Cell Hypoxia
  • Etanidazole / analogs & derivatives*
  • Etanidazole / pharmacokinetics
  • Female
  • Fluorine Radioisotopes / pharmacokinetics
  • Head and Neck Neoplasms / diagnostic imaging*
  • Head and Neck Neoplasms / metabolism*
  • Humans
  • Hydrocarbons, Fluorinated / pharmacokinetics*
  • Male
  • Middle Aged
  • Oxygen / metabolism*
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / pharmacokinetics
  • Sensitivity and Specificity
  • Young Adult

Substances

  • Fluorine Radioisotopes
  • Hydrocarbons, Fluorinated
  • Radiopharmaceuticals
  • Etanidazole
  • 2-(2-nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl)acetamide
  • Oxygen