Pharmacokinetics and radiation dosimetry of 18F-fluorocholine

Timothy R DeGrado, Robert E. Reiman, David T. Price, Shuyan Wang, R. Edward Coleman

Research output: Contribution to journalArticle

148 Citations (Scopus)

Abstract

18F-Fluorocholine (fluoromethyl-dimethyl-2-hydroxyethylammonium [FCH]) has been developed as an oncologic probe for PET. This study evaluates the kinetics and radiation dosimetry of 18F-FCH using murine and human biodistribution data. Methods: The biodistribution of 18F-FCH was obtained at time points up to 10 h after administration in control and tumor-bearing anesthetized nude mice. Human biodistribution data within the first hour after injection were obtained from attenuation-corrected whole-body PET scans of male (n = 7) and female (n = 5) cancer patients. Radiation dosimetry estimates were calculated using the murine and human biodistribution data assuming no redistribution of tracer after 1 h. Results: Rapid pharmacokinetics were observed for 18F-FCH in mice and humans. The biodistribution is nearly static after 10 min. The dose-critical organ is the kidney, which receives 0.17 ± 0.05 and 0.16 ± 0.07 mSv/MBq (0.64 ± 0.18 and 0.55 ± 0.32 rad/mCi) for females and males, respectively. The effective dose equivalent (whole body) from administration of 4.07 MBq/kg (0.110 mCi/kg) is approximately 0.01 Sv for females and males. Conclusion: 18F-FCH is rapidly cleared from the circulation and its biodistribution changes very slowly at >10 min after administration. The kidney is the dose-critical organ and limits administration levels of 18F-FCH to 4.07 MBq/kg (0.110 mCi/kg) in human research studies.

Original languageEnglish (US)
Pages (from-to)92-96
Number of pages5
JournalJournal of Nuclear Medicine
Volume43
Issue number1
StatePublished - 2002
Externally publishedYes

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Radiometry
Pharmacokinetics
Kidney
Whole Body Imaging
Nude Mice
Positron-Emission Tomography
fluorocholine
Neoplasms
Injections
Research

Keywords

  • F-fluorocholine
  • Oncology
  • PET

ASJC Scopus subject areas

  • Radiological and Ultrasound Technology

Cite this

DeGrado, T. R., Reiman, R. E., Price, D. T., Wang, S., & Coleman, R. E. (2002). Pharmacokinetics and radiation dosimetry of 18F-fluorocholine. Journal of Nuclear Medicine, 43(1), 92-96.

Pharmacokinetics and radiation dosimetry of 18F-fluorocholine. / DeGrado, Timothy R; Reiman, Robert E.; Price, David T.; Wang, Shuyan; Coleman, R. Edward.

In: Journal of Nuclear Medicine, Vol. 43, No. 1, 2002, p. 92-96.

Research output: Contribution to journalArticle

DeGrado, TR, Reiman, RE, Price, DT, Wang, S & Coleman, RE 2002, 'Pharmacokinetics and radiation dosimetry of 18F-fluorocholine', Journal of Nuclear Medicine, vol. 43, no. 1, pp. 92-96.
DeGrado, Timothy R ; Reiman, Robert E. ; Price, David T. ; Wang, Shuyan ; Coleman, R. Edward. / Pharmacokinetics and radiation dosimetry of 18F-fluorocholine. In: Journal of Nuclear Medicine. 2002 ; Vol. 43, No. 1. pp. 92-96.
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N2 - 18F-Fluorocholine (fluoromethyl-dimethyl-2-hydroxyethylammonium [FCH]) has been developed as an oncologic probe for PET. This study evaluates the kinetics and radiation dosimetry of 18F-FCH using murine and human biodistribution data. Methods: The biodistribution of 18F-FCH was obtained at time points up to 10 h after administration in control and tumor-bearing anesthetized nude mice. Human biodistribution data within the first hour after injection were obtained from attenuation-corrected whole-body PET scans of male (n = 7) and female (n = 5) cancer patients. Radiation dosimetry estimates were calculated using the murine and human biodistribution data assuming no redistribution of tracer after 1 h. Results: Rapid pharmacokinetics were observed for 18F-FCH in mice and humans. The biodistribution is nearly static after 10 min. The dose-critical organ is the kidney, which receives 0.17 ± 0.05 and 0.16 ± 0.07 mSv/MBq (0.64 ± 0.18 and 0.55 ± 0.32 rad/mCi) for females and males, respectively. The effective dose equivalent (whole body) from administration of 4.07 MBq/kg (0.110 mCi/kg) is approximately 0.01 Sv for females and males. Conclusion: 18F-FCH is rapidly cleared from the circulation and its biodistribution changes very slowly at >10 min after administration. The kidney is the dose-critical organ and limits administration levels of 18F-FCH to 4.07 MBq/kg (0.110 mCi/kg) in human research studies.

AB - 18F-Fluorocholine (fluoromethyl-dimethyl-2-hydroxyethylammonium [FCH]) has been developed as an oncologic probe for PET. This study evaluates the kinetics and radiation dosimetry of 18F-FCH using murine and human biodistribution data. Methods: The biodistribution of 18F-FCH was obtained at time points up to 10 h after administration in control and tumor-bearing anesthetized nude mice. Human biodistribution data within the first hour after injection were obtained from attenuation-corrected whole-body PET scans of male (n = 7) and female (n = 5) cancer patients. Radiation dosimetry estimates were calculated using the murine and human biodistribution data assuming no redistribution of tracer after 1 h. Results: Rapid pharmacokinetics were observed for 18F-FCH in mice and humans. The biodistribution is nearly static after 10 min. The dose-critical organ is the kidney, which receives 0.17 ± 0.05 and 0.16 ± 0.07 mSv/MBq (0.64 ± 0.18 and 0.55 ± 0.32 rad/mCi) for females and males, respectively. The effective dose equivalent (whole body) from administration of 4.07 MBq/kg (0.110 mCi/kg) is approximately 0.01 Sv for females and males. Conclusion: 18F-FCH is rapidly cleared from the circulation and its biodistribution changes very slowly at >10 min after administration. The kidney is the dose-critical organ and limits administration levels of 18F-FCH to 4.07 MBq/kg (0.110 mCi/kg) in human research studies.

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