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Published in: Molecular Imaging and Biology 6/2016

01-12-2016 | Brief Article

Biodistribution and Radiation Dosimetry of [18F]Mefway in Humans

Authors: Jae Yong Choi, Chul Hyoung Lyoo, Jin Su Kim, Kyeong Min Kim, Minkyung Lee, Young Hoon Ryu

Published in: Molecular Imaging and Biology | Issue 6/2016

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Abstract

Purpose

[18F]Mefway is a positron emission tomography (PET) radioligand for quantification of the brain serotonin 1A (5-HT1A) receptor density. The purpose of this study was to evaluate the radiation safety of [18F]Mefway in humans.

Procedures

Six healthy volunteers (three males and three females) were whole-body PET scanned for 114 min after injection of [18F]Mefway (226 ± 35 MBq). Estimated radiation doses were determined by the OLINDA/EXM software.

Results

[18F]Mefway was safe and well tolerated by all subjects. Residence time ranges from 0 (gallbladder) to 0.822 h (urinary bladder wall). While the estimated radiation doses in the reproductive and blood-forming organs were below 13.35–22.87 μSv/MBq, radiation dose in the urinary bladder wall was 471 μSv/MBq. The mean effective dose was 40.23 ± 6.63 μSv/MBq.

Conclusion

For a typical single injection of 185 MBq (5 mCi), the dose will result in 87.1 mSv for the urinary bladder wall. To reduce radiation burden, the bladder voiding can be used before [18F]Mefway PET scan.
Literature
1.
go back to reference Lai MK, Tsang SW, Francis PT et al (2003) Reduced serotonin 5-HT1A receptor binding in the temporal cortex correlates with aggressive behavior in Alzheimer disease. Brain Res 974:82–87CrossRefPubMed Lai MK, Tsang SW, Francis PT et al (2003) Reduced serotonin 5-HT1A receptor binding in the temporal cortex correlates with aggressive behavior in Alzheimer disease. Brain Res 974:82–87CrossRefPubMed
2.
go back to reference Drevets WC, Frank E, Price JC et al (1999) PET imaging of serotonin 1A receptor binding in depression. Biol Psychiatry 46:1375–1387CrossRefPubMed Drevets WC, Frank E, Price JC et al (1999) PET imaging of serotonin 1A receptor binding in depression. Biol Psychiatry 46:1375–1387CrossRefPubMed
3.
go back to reference Kepe V, Barrio JR, Huang SC et al (2006) Serotonin 1A receptors in the living brain of Alzheimer’s disease patients. Proc Natl Acad Sci U S A 103:702–707CrossRefPubMedPubMedCentral Kepe V, Barrio JR, Huang SC et al (2006) Serotonin 1A receptors in the living brain of Alzheimer’s disease patients. Proc Natl Acad Sci U S A 103:702–707CrossRefPubMedPubMedCentral
4.
go back to reference Kish SJ, Tong J, Hornykiewicz O et al (2008) Preferential loss of serotonin markers in caudate versus putamen in Parkinson’s disease. Brain 131:120–131PubMed Kish SJ, Tong J, Hornykiewicz O et al (2008) Preferential loss of serotonin markers in caudate versus putamen in Parkinson’s disease. Brain 131:120–131PubMed
5.
go back to reference Carson RE, Lang L, Watabe H et al (2000) PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635. Nucl Med Biol 27:493–497CrossRefPubMed Carson RE, Lang L, Watabe H et al (2000) PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635. Nucl Med Biol 27:493–497CrossRefPubMed
6.
go back to reference Gunn RN, Sargent PA, Bench CJ et al (1998) Tracer kinetic modeling of the 5-HT1A receptor ligand [carbonyl-11C]WAY-100635 for PET. Neuroimage 8:426–440CrossRefPubMed Gunn RN, Sargent PA, Bench CJ et al (1998) Tracer kinetic modeling of the 5-HT1A receptor ligand [carbonyl-11C]WAY-100635 for PET. Neuroimage 8:426–440CrossRefPubMed
7.
go back to reference Lacan G, Plenevaux A, Rubins DJ et al (2008) Cyclosporine, a P-glycoprotein modulator, increases [18F]MPPF uptake in rat brain and peripheral tissues: microPET and ex vivo studies. Eur J Nucl Med Mol Imaging 35:2256–2266CrossRefPubMed Lacan G, Plenevaux A, Rubins DJ et al (2008) Cyclosporine, a P-glycoprotein modulator, increases [18F]MPPF uptake in rat brain and peripheral tissues: microPET and ex vivo studies. Eur J Nucl Med Mol Imaging 35:2256–2266CrossRefPubMed
8.
go back to reference Mukherjee J, Bajwa AK, Wooten DW et al (2015) Comparative assessment of F-Mefway as a serotonin 5-HT receptor PET imaging agent across species- rodents, nonhuman primates, and humans. J Comp Neurol 524:1457–1471CrossRefPubMed Mukherjee J, Bajwa AK, Wooten DW et al (2015) Comparative assessment of F-Mefway as a serotonin 5-HT receptor PET imaging agent across species- rodents, nonhuman primates, and humans. J Comp Neurol 524:1457–1471CrossRefPubMed
9.
go back to reference Saigal N, Pichika R, Easwaramoorthy B et al (2006) Synthesis and biologic evaluation of a novel serotonin 5-HT1A receptor radioligand, 18F-labeled mefway, in rodents and imaging by PET in a nonhuman primate. J Nucl Med 47:1697–1706PubMed Saigal N, Pichika R, Easwaramoorthy B et al (2006) Synthesis and biologic evaluation of a novel serotonin 5-HT1A receptor radioligand, 18F-labeled mefway, in rodents and imaging by PET in a nonhuman primate. J Nucl Med 47:1697–1706PubMed
10.
go back to reference Choi JY, Shin S, Lee M et al (2014) Acute physical stress induces the alteration of the serotonin 1A receptor density in the hippocampus. Synapse 68:363–368CrossRefPubMed Choi JY, Shin S, Lee M et al (2014) Acute physical stress induces the alteration of the serotonin 1A receptor density in the hippocampus. Synapse 68:363–368CrossRefPubMed
11.
go back to reference Lee M, Ryu YH, Cho WG et al (2014) Dopaminergic neuron destruction reduces hippocampal serotonin 1A receptor uptake of trans-[18F]Mefway. Appl Radiat Isot 94:30–34CrossRefPubMed Lee M, Ryu YH, Cho WG et al (2014) Dopaminergic neuron destruction reduces hippocampal serotonin 1A receptor uptake of trans-[18F]Mefway. Appl Radiat Isot 94:30–34CrossRefPubMed
12.
13.
go back to reference Hillmer AT, Wooten DW, Bajwa AK et al (2014) First-in-human evaluation of 18F-mefway, a PET radioligand specific to serotonin-1A receptors. J Nucl Med 55:1973–1979CrossRefPubMedPubMedCentral Hillmer AT, Wooten DW, Bajwa AK et al (2014) First-in-human evaluation of 18F-mefway, a PET radioligand specific to serotonin-1A receptors. J Nucl Med 55:1973–1979CrossRefPubMedPubMedCentral
14.
go back to reference Shoup TM, Yokell DL, Rice PA et al (2013) A concise radiosynthesis of the tau radiopharmaceutical, [18F]T807. J Label Compd Radiopharm 56:736–740CrossRef Shoup TM, Yokell DL, Rice PA et al (2013) A concise radiosynthesis of the tau radiopharmaceutical, [18F]T807. J Label Compd Radiopharm 56:736–740CrossRef
15.
go back to reference Hines CS, Liow JS, Zanotti-Fregonara P et al (2011) Human biodistribution and dosimetry of 11C-CUMI-101, an agonist radioligand for serotonin-1a receptors in brain. PLoS One 6:e25309CrossRefPubMedPubMedCentral Hines CS, Liow JS, Zanotti-Fregonara P et al (2011) Human biodistribution and dosimetry of 11C-CUMI-101, an agonist radioligand for serotonin-1a receptors in brain. PLoS One 6:e25309CrossRefPubMedPubMedCentral
16.
go back to reference Zanotti-Fregonara P, Lammertsma AA, Innis RB (2013) Suggested pathway to assess radiation safety of 18F-labeled PET tracers for first-in-human studies. Eur J Nucl Med Mol Imaging 40:1781–1783CrossRefPubMed Zanotti-Fregonara P, Lammertsma AA, Innis RB (2013) Suggested pathway to assess radiation safety of 18F-labeled PET tracers for first-in-human studies. Eur J Nucl Med Mol Imaging 40:1781–1783CrossRefPubMed
17.
go back to reference Constantinescu CC, Sevrioukov E, Garcia A et al (2013) Evaluation of [18F]Mefway biodistribution and dosimetry based on whole-body PET imaging of mice. Mol Imaging Biol 15:222–229CrossRefPubMed Constantinescu CC, Sevrioukov E, Garcia A et al (2013) Evaluation of [18F]Mefway biodistribution and dosimetry based on whole-body PET imaging of mice. Mol Imaging Biol 15:222–229CrossRefPubMed
18.
go back to reference Parsey RV, Belanger MJ, Sullivan GM et al (2005) Biodistribution and radiation dosimetry of 11C-WAY100,635 in humans. J Nucl Med 46:614–619PubMed Parsey RV, Belanger MJ, Sullivan GM et al (2005) Biodistribution and radiation dosimetry of 11C-WAY100,635 in humans. J Nucl Med 46:614–619PubMed
19.
go back to reference Anjos DA, Etchebehere EC, Ramos CD et al (2007) 18F-FDG PET/CT delayed images after diuretic for restaging invasive bladder cancer. J Nucl Med 48:764–770CrossRefPubMed Anjos DA, Etchebehere EC, Ramos CD et al (2007) 18F-FDG PET/CT delayed images after diuretic for restaging invasive bladder cancer. J Nucl Med 48:764–770CrossRefPubMed
20.
go back to reference Diehl M, Manolopoulou M, Risse J et al (2004) Urinary fluorine-18 fluorodeoxyglucose excretion with and without intravenous application of furosemide. Acta Med Austriaca 31:76–78PubMed Diehl M, Manolopoulou M, Risse J et al (2004) Urinary fluorine-18 fluorodeoxyglucose excretion with and without intravenous application of furosemide. Acta Med Austriaca 31:76–78PubMed
21.
go back to reference Koyama K, Okamura T, Kawabe J et al (2003) Evaluation of 18F-FDG PET with bladder irrigation in patients with uterine and ovarian tumors. J Nucl Med 44:353–358PubMed Koyama K, Okamura T, Kawabe J et al (2003) Evaluation of 18F-FDG PET with bladder irrigation in patients with uterine and ovarian tumors. J Nucl Med 44:353–358PubMed
22.
go back to reference Miraldi F, Vesselle H, Faulhaber PF et al (1998) Elimination of artifactual accumulation of FDG in PET imaging of colorectal cancer. Clin Nucl Med 23:3–7CrossRefPubMed Miraldi F, Vesselle H, Faulhaber PF et al (1998) Elimination of artifactual accumulation of FDG in PET imaging of colorectal cancer. Clin Nucl Med 23:3–7CrossRefPubMed
Metadata
Title
Biodistribution and Radiation Dosimetry of [18F]Mefway in Humans
Authors
Jae Yong Choi
Chul Hyoung Lyoo
Jin Su Kim
Kyeong Min Kim
Minkyung Lee
Young Hoon Ryu
Publication date
01-12-2016
Publisher
Springer US
Published in
Molecular Imaging and Biology / Issue 6/2016
Print ISSN: 1536-1632
Electronic ISSN: 1860-2002
DOI
https://doi.org/10.1007/s11307-016-0955-8

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