Biodistribution and radiation dosimetry of [¹⁸F]-5-fluorouracil

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• 作者：Ayako Hino-Shishikura^a ; ^{ayako_s_1213@hotmail.com} ; ^{ayako_h@yokohama-cu.ac.jp} ; Akiko Suzuki^a ; Ryogo Minamimoto^a ; Kazuya Shizukuishi^a ; Takashi Oka^a ; Ukihide Tateishi^a ; Sadatoshi Sugae^b ; Yasushi Ichikawa^b ; Choichi Horiuchi^c ; Tomio Inoue^a
• 关键词：PET ; positron emission tomography ; TS ; thymidylate synthase ; F-RNA ; F-ribonucleic acid ; [18F]-5-FU ; 5-fluorouracil labeled with 18F ; DPD ; dihydropyrimidine dehydrogenase ; FBAL ; alpha-fluoro-beta-alanine ; OLINDA ; Organ Level Internal Dose Assessment Code
• 刊名：Applied Radiation and Isotopes
• 出版年：2013
• 出版时间：May, 2013
• 年：2013
• 卷：75
• 期：Complete
• 页码：11-17
• 全文大小：473 K

文摘

Purpose

To estimate the radiation dose and biodistribution of ¹⁸F-5-fluorouracil ([¹⁸F]-5-FU) from positron emission tomography/computed tomography (PET/CT) data, and to extrapolate mouse data to human data in order to evaluate cross-species consistency.

Methods

Fifteen cancer patients (head and neck cancer (n=11), colon cancer (n=4)) were enrolled. Sequential PET/CT images were acquired for 2 h after intravenous administration of [¹⁸F]-5-FU, and the percent of the injected dose delivered to each organ was derived. For comparison, [¹⁸F]-5-FU was administered to female BALB/cAJcl-nu/nu nude mice (n=19), and the percent of the injected dose delivered to mouse organs was extrapolated to the human model. Absorbed radiation dose was calculated using OLINDA/EXM 1.0 software.

Results

In human subjects, high [¹⁸F]-5-FU uptake was seen in the liver, gallbladder and kidneys. The absorbed dose was highest in the gallbladder wall. In mice, the biodistribution of [¹⁸F]-5-FU corresponded to that of humans. Estimated absorbed radiation doses for all organs were moderately correlated, and doses to organs (except the gallbladder and urinary bladder) were significantly correlated between mice and humans. The mean effective [¹⁸F]-5-FU dose was higher in humans (0.0124 mSv/MBq) than in mice (0.0058 mSv/MBq).

Conclusion

Biodistribution and radiation dosimetry of [¹⁸F]-5-FU were compared between humans and mice: biodistribution in mice and humans was similar. Data from mice underestimated the effective dose in humans, suggesting that clinical measurements are needed for more detailed dose estimation in order to ensure radiation safety. The observed effective doses suggest the feasibility of [¹⁸F]-5-FU PET/CT for human studies.