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Journal of Nuclear Medicine Vol. 43 No. 1 92-96
© 2002 by Society of Nuclear Medicine


Basic Science Investigations

Pharmacokinetics and Radiation Dosimetry of 18F-Fluorocholine

Timothy R. DeGrado, PhD1, Robert E. Reiman, MD2, David T. Price, MD3, Shuyan Wang1 and R. Edward Coleman, MD1

1 Department of Radiology, Duke University Medical Center, Durham, North Carolina
2 Division of Radiation Safety, Duke University Medical Center, Durham, North Carolina
3 Department of Surgery, Duke University Medical Center, Durham, North Carolina

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.

Key Words: 18F-fluorocholine • PET • oncology




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