Biodistribution and radiation dosimetry of 18F-FTC-146 in humans

Trine Hjørnevik, Peter W. Cipriano, Bin Shen, Jun Hyung Park, Praveen Gulaka, Dawn Holley, Harsh Gandhi, Daehyun Yoon, Erik S. Mittra, Greg Zaharchuk, Sanjiv S. Gambhir, Christopher R. McCurdy, Frederick T. Chin, Sandip Biswal

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

The purpose of this study was to assess safety, biodistribution, and radiation dosimetry in humans for the highly selective s-1 receptor PET agent 18F-6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[d] thiazol-2(3H)-one (18F-FTC-146). Methods: Ten healthy volunteers (5 women, 5 men; age ± SD, 34.3 ± 6.5 y) were recruited, and written informed consent was obtained from all participants. Series of whole-body PET/MRI examinations were acquired for up to 3 h after injection (357.2 ± 48.8 MBq). Blood samples were collected, and standard vital signs (heart rate, pulse oximetry, and body temperature) were monitored at regular intervals. Regions of interest were delineated, time-activity curves were calculated, and organ uptake and dosimetry were estimated. Results: All subjects tolerated the PET/MRI examination well, and no adverse reactions to 18F-FTC-146 were reported. High accumulation of 18F-FTC-146 was observed in s-1 receptor-dense organs such as the pancreas and spleen, moderate uptake in the brain and myocardium, and low uptake in bone and muscle. High uptake was also observed in the kidneys and bladder, indicating renal tracer clearance. The effective dose of 18F-FTC-146 was 0.0259 ± 0.0034 mSv/MBq (range, 0.0215-0.0301 mSv/MBq). Conclusion: First-in-human studies with clinical-grade 18F-FTC-146 were successful. Injection of 18F-FTC-146 is safe, and absorbed doses are acceptable. The potential of 18F-FTC-146 as an imaging agent for a variety of neuroinflammatory diseases is currently under investigation.

Original languageEnglish (US)
Pages (from-to)2004-2009
Number of pages6
JournalJournal of Nuclear Medicine
Volume58
Issue number12
DOIs
StatePublished - Dec 1 2017

Keywords

  • Biodistribution
  • First-in-human
  • PET
  • Radiation dosimetry
  • Sigma-1 receptor

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

Fingerprint Dive into the research topics of 'Biodistribution and radiation dosimetry of <sup>18</sup>F-FTC-146 in humans'. Together they form a unique fingerprint.

  • Cite this

    Hjørnevik, T., Cipriano, P. W., Shen, B., Park, J. H., Gulaka, P., Holley, D., Gandhi, H., Yoon, D., Mittra, E. S., Zaharchuk, G., Gambhir, S. S., McCurdy, C. R., Chin, F. T., & Biswal, S. (2017). Biodistribution and radiation dosimetry of 18F-FTC-146 in humans. Journal of Nuclear Medicine, 58(12), 2004-2009. https://doi.org/10.2967/jnumed.117.192641