Abstract
Introduction: The translocator protein (TSPO) ligands [{sup 18}F]PBR111 and [{sup 18}F]PBR102 show promise for imaging neuroinflammation. Our aim was to estimate the radiation dose to humans from primate positron emission tomography (PET) studies using these ligands and compare the results with those obtained from studies in rodents. Methods: [{sup 18}F]PBR111 and [{sup 18}F]PBR102 PET-computed tomography studies were carried out in baboons. The cumulated activity in the selected source organs was obtained from the volume of interest time-activity curves drawn on coronal PET slices and adjusted for organ mass relative to humans. Radiation dose estimates were calculated in OLINDA/EXM Version 1.1 from baboon studies and compared with those calculated from Sprague-Dawley rat tissue concentration studies, also adjusted for relative organ mass. Results: In baboons, both ligands cleared rapidly from brain, lung, kidney and spleen and more slowly from liver and heart. For [{sup 18}F]PBR111, the renal excretion fraction was 6.5% and 17% for hepatobiliary excretion; for [{sup 18}F]PBR102, the renal excretion was 3.0% and 15% for hepatobiliary excretion. The estimated effective dose in humans from baboon data was 0.021 mSv/MBq for each ligand, whilst from rat data, the estimates were 0.029 for [{sup 18}F]PBR111 and 0.041 mSv/MBq for [{sup 18}F]PBR102. Conclusion:
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Verschuer, Jordan D., E-mail: jordan@nucmed.rpa.cs.nsw.gov.au;
[1]
Towson, Jocelyn;
[1]
Eberl, Stefan;
[1]
School of Information Technologies, University of Sydney, NSW 2006 (Australia)];
Katsifis, Andrew;
[2]
Henderson, David;
Lam, Peter;
[1]
Wen, Lingfeng;
[1]
School of Information Technologies, University of Sydney, NSW 2006 (Australia)];
Loc'h, Christian;
Mattner, Filomena;
[2]
Thomson, Sally;
[3]
Mohamed, Armin;
[1]
Sydney Medical School, University of Sydney, NSW 2006 (Australia)];
Fulham, Michael J;
[1]
School of Information Technologies, University of Sydney, NSW 2006 (Australia);
Sydney Medical School, University of Sydney, NSW 2006 (Australia)]
- Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown, NSW 2050 (Australia)
- ANSTO LifeSciences, Lucas Heights, NSW 2234 (Australia)
- Department of Renal Medicine, Royal Prince Alfred Hospital, Camperdown, NSW 2050 (Australia)
Citation Formats
Verschuer, Jordan D., E-mail: jordan@nucmed.rpa.cs.nsw.gov.au, Towson, Jocelyn, Eberl, Stefan, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Katsifis, Andrew, Henderson, David, Lam, Peter, Wen, Lingfeng, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Loc'h, Christian, Mattner, Filomena, Thomson, Sally, Mohamed, Armin, Sydney Medical School, University of Sydney, NSW 2006 (Australia)], Fulham, Michael J, School of Information Technologies, University of Sydney, NSW 2006 (Australia), and Sydney Medical School, University of Sydney, NSW 2006 (Australia)].
Radiation dosimetry of the translocator protein ligands [{sup 18}F]PBR111 and [{sup 18}F]PBR102.
United Kingdom: N. p.,
2012.
Web.
doi:10.1016/J.NUCMEDBIO.2011.11.003.
Verschuer, Jordan D., E-mail: jordan@nucmed.rpa.cs.nsw.gov.au, Towson, Jocelyn, Eberl, Stefan, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Katsifis, Andrew, Henderson, David, Lam, Peter, Wen, Lingfeng, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Loc'h, Christian, Mattner, Filomena, Thomson, Sally, Mohamed, Armin, Sydney Medical School, University of Sydney, NSW 2006 (Australia)], Fulham, Michael J, School of Information Technologies, University of Sydney, NSW 2006 (Australia), & Sydney Medical School, University of Sydney, NSW 2006 (Australia)].
Radiation dosimetry of the translocator protein ligands [{sup 18}F]PBR111 and [{sup 18}F]PBR102.
United Kingdom.
https://doi.org/10.1016/J.NUCMEDBIO.2011.11.003
Verschuer, Jordan D., E-mail: jordan@nucmed.rpa.cs.nsw.gov.au, Towson, Jocelyn, Eberl, Stefan, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Katsifis, Andrew, Henderson, David, Lam, Peter, Wen, Lingfeng, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Loc'h, Christian, Mattner, Filomena, Thomson, Sally, Mohamed, Armin, Sydney Medical School, University of Sydney, NSW 2006 (Australia)], Fulham, Michael J, School of Information Technologies, University of Sydney, NSW 2006 (Australia), and Sydney Medical School, University of Sydney, NSW 2006 (Australia)].
2012.
"Radiation dosimetry of the translocator protein ligands [{sup 18}F]PBR111 and [{sup 18}F]PBR102."
United Kingdom.
https://doi.org/10.1016/J.NUCMEDBIO.2011.11.003.
@misc{etde_22048820,
title = {Radiation dosimetry of the translocator protein ligands [{sup 18}F]PBR111 and [{sup 18}F]PBR102}
author = {Verschuer, Jordan D., E-mail: jordan@nucmed.rpa.cs.nsw.gov.au, Towson, Jocelyn, Eberl, Stefan, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Katsifis, Andrew, Henderson, David, Lam, Peter, Wen, Lingfeng, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Loc'h, Christian, Mattner, Filomena, Thomson, Sally, Mohamed, Armin, Sydney Medical School, University of Sydney, NSW 2006 (Australia)], Fulham, Michael J, School of Information Technologies, University of Sydney, NSW 2006 (Australia), and Sydney Medical School, University of Sydney, NSW 2006 (Australia)]}
abstractNote = {Introduction: The translocator protein (TSPO) ligands [{sup 18}F]PBR111 and [{sup 18}F]PBR102 show promise for imaging neuroinflammation. Our aim was to estimate the radiation dose to humans from primate positron emission tomography (PET) studies using these ligands and compare the results with those obtained from studies in rodents. Methods: [{sup 18}F]PBR111 and [{sup 18}F]PBR102 PET-computed tomography studies were carried out in baboons. The cumulated activity in the selected source organs was obtained from the volume of interest time-activity curves drawn on coronal PET slices and adjusted for organ mass relative to humans. Radiation dose estimates were calculated in OLINDA/EXM Version 1.1 from baboon studies and compared with those calculated from Sprague-Dawley rat tissue concentration studies, also adjusted for relative organ mass. Results: In baboons, both ligands cleared rapidly from brain, lung, kidney and spleen and more slowly from liver and heart. For [{sup 18}F]PBR111, the renal excretion fraction was 6.5% and 17% for hepatobiliary excretion; for [{sup 18}F]PBR102, the renal excretion was 3.0% and 15% for hepatobiliary excretion. The estimated effective dose in humans from baboon data was 0.021 mSv/MBq for each ligand, whilst from rat data, the estimates were 0.029 for [{sup 18}F]PBR111 and 0.041 mSv/MBq for [{sup 18}F]PBR102. Conclusion: Biodistribution in a nonhuman primate model is better suited than the rat model for the calculation of dosimetry parameters when translating these ligands from preclinical to human clinical studies. Effective dose calculated from rat data was overestimated compared to nonhuman primate data. The effective dose coefficient for both these TSPO ligands determined from PET studies in baboons is similar to that for [{sup 18}F]FDG.}
doi = {10.1016/J.NUCMEDBIO.2011.11.003}
journal = []
issue = {5}
volume = {39}
journal type = {AC}
place = {United Kingdom}
year = {2012}
month = {Jul}
}
title = {Radiation dosimetry of the translocator protein ligands [{sup 18}F]PBR111 and [{sup 18}F]PBR102}
author = {Verschuer, Jordan D., E-mail: jordan@nucmed.rpa.cs.nsw.gov.au, Towson, Jocelyn, Eberl, Stefan, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Katsifis, Andrew, Henderson, David, Lam, Peter, Wen, Lingfeng, School of Information Technologies, University of Sydney, NSW 2006 (Australia)], Loc'h, Christian, Mattner, Filomena, Thomson, Sally, Mohamed, Armin, Sydney Medical School, University of Sydney, NSW 2006 (Australia)], Fulham, Michael J, School of Information Technologies, University of Sydney, NSW 2006 (Australia), and Sydney Medical School, University of Sydney, NSW 2006 (Australia)]}
abstractNote = {Introduction: The translocator protein (TSPO) ligands [{sup 18}F]PBR111 and [{sup 18}F]PBR102 show promise for imaging neuroinflammation. Our aim was to estimate the radiation dose to humans from primate positron emission tomography (PET) studies using these ligands and compare the results with those obtained from studies in rodents. Methods: [{sup 18}F]PBR111 and [{sup 18}F]PBR102 PET-computed tomography studies were carried out in baboons. The cumulated activity in the selected source organs was obtained from the volume of interest time-activity curves drawn on coronal PET slices and adjusted for organ mass relative to humans. Radiation dose estimates were calculated in OLINDA/EXM Version 1.1 from baboon studies and compared with those calculated from Sprague-Dawley rat tissue concentration studies, also adjusted for relative organ mass. Results: In baboons, both ligands cleared rapidly from brain, lung, kidney and spleen and more slowly from liver and heart. For [{sup 18}F]PBR111, the renal excretion fraction was 6.5% and 17% for hepatobiliary excretion; for [{sup 18}F]PBR102, the renal excretion was 3.0% and 15% for hepatobiliary excretion. The estimated effective dose in humans from baboon data was 0.021 mSv/MBq for each ligand, whilst from rat data, the estimates were 0.029 for [{sup 18}F]PBR111 and 0.041 mSv/MBq for [{sup 18}F]PBR102. Conclusion: Biodistribution in a nonhuman primate model is better suited than the rat model for the calculation of dosimetry parameters when translating these ligands from preclinical to human clinical studies. Effective dose calculated from rat data was overestimated compared to nonhuman primate data. The effective dose coefficient for both these TSPO ligands determined from PET studies in baboons is similar to that for [{sup 18}F]FDG.}
doi = {10.1016/J.NUCMEDBIO.2011.11.003}
journal = []
issue = {5}
volume = {39}
journal type = {AC}
place = {United Kingdom}
year = {2012}
month = {Jul}
}