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Radiation dosimetry of (18)F-AzaFol: A first in-human use of a folate receptor PET tracer

BACKGROUND: The folate receptor alpha (FRα) is an interesting target for imaging and therapy of different cancers. We present the first in-human radiation dosimetry and radiation safety results acquired within a prospective, multicentric trial (NCT03242993) evaluating the (18)F-AzaFol (3′-aza-2′-[(1...

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Autores principales: Gnesin, Silvano, Müller, Joachim, Burger, Irene A., Meisel, Alexander, Siano, Marco, Früh, Martin, Choschzick, Matthias, Müller, Cristina, Schibli, Roger, Ametamey, Simon M., Kaufmann, Philipp A., Treyer, Valerie, Prior, John O., Schaefer, Niklaus
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer Berlin Heidelberg 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7142191/
https://www.ncbi.nlm.nih.gov/pubmed/32270313
http://dx.doi.org/10.1186/s13550-020-00624-2
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author Gnesin, Silvano
Müller, Joachim
Burger, Irene A.
Meisel, Alexander
Siano, Marco
Früh, Martin
Choschzick, Matthias
Müller, Cristina
Schibli, Roger
Ametamey, Simon M.
Kaufmann, Philipp A.
Treyer, Valerie
Prior, John O.
Schaefer, Niklaus
author_facet Gnesin, Silvano
Müller, Joachim
Burger, Irene A.
Meisel, Alexander
Siano, Marco
Früh, Martin
Choschzick, Matthias
Müller, Cristina
Schibli, Roger
Ametamey, Simon M.
Kaufmann, Philipp A.
Treyer, Valerie
Prior, John O.
Schaefer, Niklaus
author_sort Gnesin, Silvano
collection PubMed
description BACKGROUND: The folate receptor alpha (FRα) is an interesting target for imaging and therapy of different cancers. We present the first in-human radiation dosimetry and radiation safety results acquired within a prospective, multicentric trial (NCT03242993) evaluating the (18)F-AzaFol (3′-aza-2′-[(18)F]fluorofolic acid) as the first clinically assessed PET tracer targeting the FRα. MATERIAL AND METHODS: Six eligible patients presented a histologically confirmed adenocarcinoma of the lung with measurable lesions (≥ 10 mm according to RECIST 1.1). TOF-PET images were acquired at 3, 11, 18, 30, 40, 50, and 60 min after the intravenous injection of 327 MBq (range 299–399 MBq) of (18)F-AzaFol to establish dosimetry. Organ absorbed doses (AD), tumor AD, and patient effective doses (E) were assessed using the OLINDA/EXM v.2.0 software and compared with pre-clinical results. RESULTS: No serious related adverse events were observed. The highest AD were in the liver, the kidneys, the urinary bladder, and the spleen (51.9, 45.8, 39.1, and 35.4 μGy/MBq, respectively). Estimated patient and gender-averaged E were 18.0 ± 2.6 and 19.7 ± 1.4 μSv/MBq, respectively. E in-human exceeded the value of 14.0 μSv/MBq extrapolated from pre-clinical data. Average tumor AD was 34.8 μGy/MBq (range 13.6–60.5 μGy/MBq). CONCLUSIONS: (18)F-Azafol is a PET agent with favorable dosimetric properties and a reasonable radiation dose burden for patients which merits further evaluation to assess its performance. TRIAL REGISTRATION: ClinicalTrial.gov, NCT03242993, posted on August 8, 2017
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spelling pubmed-71421912020-04-15 Radiation dosimetry of (18)F-AzaFol: A first in-human use of a folate receptor PET tracer Gnesin, Silvano Müller, Joachim Burger, Irene A. Meisel, Alexander Siano, Marco Früh, Martin Choschzick, Matthias Müller, Cristina Schibli, Roger Ametamey, Simon M. Kaufmann, Philipp A. Treyer, Valerie Prior, John O. Schaefer, Niklaus EJNMMI Res Original Research BACKGROUND: The folate receptor alpha (FRα) is an interesting target for imaging and therapy of different cancers. We present the first in-human radiation dosimetry and radiation safety results acquired within a prospective, multicentric trial (NCT03242993) evaluating the (18)F-AzaFol (3′-aza-2′-[(18)F]fluorofolic acid) as the first clinically assessed PET tracer targeting the FRα. MATERIAL AND METHODS: Six eligible patients presented a histologically confirmed adenocarcinoma of the lung with measurable lesions (≥ 10 mm according to RECIST 1.1). TOF-PET images were acquired at 3, 11, 18, 30, 40, 50, and 60 min after the intravenous injection of 327 MBq (range 299–399 MBq) of (18)F-AzaFol to establish dosimetry. Organ absorbed doses (AD), tumor AD, and patient effective doses (E) were assessed using the OLINDA/EXM v.2.0 software and compared with pre-clinical results. RESULTS: No serious related adverse events were observed. The highest AD were in the liver, the kidneys, the urinary bladder, and the spleen (51.9, 45.8, 39.1, and 35.4 μGy/MBq, respectively). Estimated patient and gender-averaged E were 18.0 ± 2.6 and 19.7 ± 1.4 μSv/MBq, respectively. E in-human exceeded the value of 14.0 μSv/MBq extrapolated from pre-clinical data. Average tumor AD was 34.8 μGy/MBq (range 13.6–60.5 μGy/MBq). CONCLUSIONS: (18)F-Azafol is a PET agent with favorable dosimetric properties and a reasonable radiation dose burden for patients which merits further evaluation to assess its performance. TRIAL REGISTRATION: ClinicalTrial.gov, NCT03242993, posted on August 8, 2017 Springer Berlin Heidelberg 2020-04-08 /pmc/articles/PMC7142191/ /pubmed/32270313 http://dx.doi.org/10.1186/s13550-020-00624-2 Text en © The Author(s) 2020 Open AccessThis article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.
spellingShingle Original Research
Gnesin, Silvano
Müller, Joachim
Burger, Irene A.
Meisel, Alexander
Siano, Marco
Früh, Martin
Choschzick, Matthias
Müller, Cristina
Schibli, Roger
Ametamey, Simon M.
Kaufmann, Philipp A.
Treyer, Valerie
Prior, John O.
Schaefer, Niklaus
Radiation dosimetry of (18)F-AzaFol: A first in-human use of a folate receptor PET tracer
title Radiation dosimetry of (18)F-AzaFol: A first in-human use of a folate receptor PET tracer
title_full Radiation dosimetry of (18)F-AzaFol: A first in-human use of a folate receptor PET tracer
title_fullStr Radiation dosimetry of (18)F-AzaFol: A first in-human use of a folate receptor PET tracer
title_full_unstemmed Radiation dosimetry of (18)F-AzaFol: A first in-human use of a folate receptor PET tracer
title_short Radiation dosimetry of (18)F-AzaFol: A first in-human use of a folate receptor PET tracer
title_sort radiation dosimetry of (18)f-azafol: a first in-human use of a folate receptor pet tracer
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7142191/
https://www.ncbi.nlm.nih.gov/pubmed/32270313
http://dx.doi.org/10.1186/s13550-020-00624-2
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