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European Journal of Nuclear Medicine and Molecular Imaging

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01-07-2008 | Original Article

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

Authors: P. Mahy, X. Geets, M. Lonneux, P. Levêque, N. Christian, M. De Bast, J. Gillart, D. Labar, J. Lee, V. Grégoire

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 7/2008

Abstract

Purpose

The aim of this study was to assess the pharmacokinetics, biodistribution and metabolism of [¹⁸F]EF3, a labelled 2-nitroimidazole hypoxia marker, in ten patients with head and neck cancer.

Methods

[¹⁸F]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. [¹⁸F]EF3 concentration in blood exhibited a bi-exponential decline. [¹⁸F]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 [¹⁸F]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, [¹⁸F]EF3 remained very stable after injection, with percentage of native tracer above 87% in the serum and 84% in the urine.

Conclusion

Administration of [¹⁸F]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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Title: Determination of tumour hypoxia with [18F]EF3 in patients with head and neck tumours: a phase I study to assess the tracer pharmacokinetics, biodistribution and metabolism
Authors: P. Mahy
X. Geets
M. Lonneux
P. Levêque
N. Christian
M. De Bast
J. Gillart
D. Labar
J. Lee
V. Grégoire
Publication date: 01-07-2008
Publisher: Springer-Verlag
Published in: European Journal of Nuclear Medicine and Molecular Imaging / Issue 7/2008
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-008-0742-0

Keynote webinar | Spotlight on medication adherence

Springer Medicine

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

Abstract

Purpose

Methods

Results

Conclusion

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Purpose

Methods

Results

Conclusion

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