Development of F-18-labeled fluoroerythronitroimidazole as a PET agent for imaging tumor hypoxia

Radiology. 1995 Mar;194(3):795-800. doi: 10.1148/radiology.194.3.7862981.

Abstract

Purpose: To develop a hydrophilic ligand to image tumor hypoxia at positron emission tomography (PET).

Materials and methods: Biodistribution of fluorine-18-labeled fluoroerythronitroimidazole (FETNIM) and F-18-labeled fluoromisonidazole (FMISO) was determined at PET and autoradiography in three mammary-tumor-bearing rats. The partition coefficient of FETNIM, FMISO, and misonidazole was determined.

Results: Biodistribution of F-18-labeled FETNIM at 1, 2, and 4 hours showed tumor-to-blood ratios of 2.29 +/- 0.599, 2.41 +/- 0.567 and 8.02 +/- 2.420, respectively, and tumor-to-muscle ratios of 0.66 +/- 0.267, 2.11 +/- 0.347, and 5.92 +/- 2.240, respectively. The tumor-to-blood count density ratio with F-18-labeled FETNIM at 4 hours after injection was significantly higher than with F-18-labeled FMISO. Autoradiographs indicated that both agents could help differentiate hypoxic versus necrotic region in the tumor.

Conclusion: F-18-labeled FETNIM can help detect tumor hypoxia and is easier to prepare, less costly, and more hydrophilic than F-18-labeled FMISO.

Publication types

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

MeSH terms

  • Animals
  • Autoradiography
  • Cell Hypoxia
  • Contrast Media
  • Female
  • Fluorine Radioisotopes*
  • Male
  • Mammary Neoplasms, Experimental / diagnostic imaging*
  • Misonidazole / analogs & derivatives
  • Neoplasm Transplantation
  • Neoplasms, Experimental / diagnostic imaging*
  • Nitroimidazoles* / chemical synthesis
  • Rabbits
  • Rats
  • Rats, Inbred F344
  • Tissue Distribution
  • Tomography, Emission-Computed*

Substances

  • Contrast Media
  • Fluorine Radioisotopes
  • Nitroimidazoles
  • fluoroerythronitroimidazole
  • fluoromisonidazole
  • Misonidazole