Determination of tumour hypoxia with [(18)F]EF3 in patients with head and neck tumours : a phase I study to assess the tracer pharmacokinetics, biodistribution and metabolism

Mahy, Pierre;Geets, Xavier;Lonneux, Max;Levêque, Philippe;Grégoire, Vincent;et.al.
(2008) European Journal of Nuclear Medicine and Molecular Imaging — Vol. 35, n° 7, p. 1282-1289 (2008)

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Authors
  • Mahy, PierreUCLouvain
    Author
  • Geets, XavierUCLouvain
    Author
  • Lonneux, MaxUCLouvain
    Author
  • Levêque, PhilippeUCLouvain
    Author
  • Christian, NicolasUCLouvain
    Author
  • De Bast, MarcUCLouvain
    Author
  • Gillart, JacquesUCLouvain
    Author
  • Labar, DanielUCLouvain
    Author
  • Lee, Johnorcid-logoUCLouvain
    Author
  • Grégoire, VincentUCLouvain
    Author
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Abstract
PURPOSE: The aim of this study was to assess the pharmacokinetics, biodistribution and metabolism of [(18)F]EF3, a labelled 2-nitroimidazole hypoxia marker, in ten patients with head and neck cancer. METHODS: [(18)F]EF3 was administered intravenously (group 1, n = 5, mean dose +/- SD: 324 +/- 108 MBq; group 2, n = 5, mean dose +/- SD: 1,134 +/- 138 MBq) to patients (nine male, one female). Blood and urine samples and whole-body PET scans were obtained from 20 s to 4-6 h. Radioactivity was determined in several regions of interest. RESULTS: No serious adverse event was reported. [(18)F]EF3 concentration in blood exhibited a bi-exponential decline. [(18)F]EF3 was mainly eliminated in the urine. By 7 h 40 min after injection, 53 +/- 14% of the injected dose was collected in the urine. There was no significant difference between the low- and high-dose groups. A progressive accumulation occurred also in the colon, indicating a hepatobiliary excretion. Except in organs involved in the elimination of [(18)F]EF3, the tumour-to-organ ratio remained close to or below unity in muscle, lungs, heart and brain at various times after injection. In one patient, tumour hypoxia was observed with a tumour-to-blood ratio ranging from 1.4 to 1.9. Last, [(18)F]EF3 remained very stable after injection, with percentage of native tracer above 87% in the serum and 84% in the urine. CONCLUSION: Administration of [(18)F]EF3 in head and neck cancer patients is feasible and safe. Uptake and retention in tumour was observed, indicating the presence of hypoxia.
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Mahy, P., Geets, X., Lonneux, M., Levêque, P., Christian, N., De Bast, M., Gillart, J., Labar, D., Lee, J., & Grégoire, V. (2008). Determination of tumour hypoxia with [(18)F]EF3 in patients with head and neck tumours : a phase I study to assess the tracer pharmacokinetics, biodistribution and metabolism. European Journal of Nuclear Medicine and Molecular Imaging, 35(7), 1282-1289. https://doi.org/10.1007/s00259-008-0742-0 (Original work published 2008)