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

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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.

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References

  1. 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 974:82–87

    Article  CAS  PubMed  Google Scholar 

  2. Drevets WC, Frank E, Price JC et al (1999) PET imaging of serotonin 1A receptor binding in depression. Biol Psychiatry 46:1375–1387

    Article  CAS  PubMed  Google Scholar 

  3. 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 103:702–707

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  4. Kish SJ, Tong J, Hornykiewicz O et al (2008) Preferential loss of serotonin markers in caudate versus putamen in Parkinson’s disease. Brain 131:120–131

    PubMed  Google Scholar 

  5. 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 27:493–497

    Article  CAS  PubMed  Google Scholar 

  6. 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 8:426–440

    Article  CAS  PubMed  Google Scholar 

  7. 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 35:2256–2266

    Article  CAS  PubMed  Google Scholar 

  8. 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 524:1457–1471

    Article  PubMed  Google Scholar 

  9. 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 47:1697–1706

    CAS  PubMed  Google Scholar 

  10. 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 68:363–368

    Article  CAS  PubMed  Google Scholar 

  11. 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 94:30–34

    Article  CAS  PubMed  Google Scholar 

  12. Choi JY, Lyoo CH, Kim JS et al (2015) 18F-Mefway PET imaging of serotonin 1A receptors in humans: a comparison with 18F-FCWAY. PLoS One 10:e0121342

    Article  PubMed  PubMed Central  Google Scholar 

  13. 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 55:1973–1979

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  14. Shoup TM, Yokell DL, Rice PA et al (2013) A concise radiosynthesis of the tau radiopharmaceutical, [18F]T807. J Label Compd Radiopharm 56:736–740

    Article  CAS  Google Scholar 

  15. 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:e25309

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  16. 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 40:1781–1783

    Article  PubMed  Google Scholar 

  17. 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 15:222–229

    Article  PubMed  Google Scholar 

  18. Parsey RV, Belanger MJ, Sullivan GM et al (2005) Biodistribution and radiation dosimetry of 11C-WAY100,635 in humans. J Nucl Med 46:614–619

    CAS  PubMed  Google Scholar 

  19. 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 48:764–770

    Article  PubMed  Google Scholar 

  20. Diehl M, Manolopoulou M, Risse J et al (2004) Urinary fluorine-18 fluorodeoxyglucose excretion with and without intravenous application of furosemide. Acta Med Austriaca 31:76–78

    PubMed  Google Scholar 

  21. 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 44:353–358

    PubMed  Google Scholar 

  22. Miraldi F, Vesselle H, Faulhaber PF et al (1998) Elimination of artifactual accumulation of FDG in PET imaging of colorectal cancer. Clin Nucl Med 23:3–7

    Article  CAS  PubMed  Google Scholar 

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Acknowledgments

This research was supported by the Nuclear R&D Program of the National Research Foundation of Korea (Grant No. NRF-2015M2A2A7027110) and INHA UNIVERSITY Research Grant (INHA-52574). The authors would like to express their sincere gratitude to Tae Ho Song and Won Taek Lee (PET technologists) who managed all PET experiments.

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Correspondence to Young Hoon Ryu.

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The authors declare that they have no conflict of interest.

Ethical Approval

All procedures performed in studies involving human participants were in accordance with the ethical standards of the institutional and/or national research committee and with the 1964 Helsinki declaration and its later amendments or comparable ethical standards.

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Choi, J.Y., Lyoo, C.H., Kim, J.S. et al. Biodistribution and Radiation Dosimetry of [18F]Mefway in Humans. Mol Imaging Biol 18, 803–806 (2016). https://doi.org/10.1007/s11307-016-0955-8

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  • DOI: https://doi.org/10.1007/s11307-016-0955-8

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