⁶⁸Ga-Citrate PET of Healthy Men: Whole-Body Biodistribution Kinetics and Radiation Dose Estimates

Abstract

⁶⁸Ga-citrate has one of the simplest chemical structures of all ⁶⁸Ga-radiopharmaceuticals, and its clinical use is justified by the proven medical applications using its isotope-labeled compound ⁶⁷Ga-citrate. To support broader application of ⁶⁸Ga-citrate in medical diagnosis, further research is needed to gain clinical data from healthy volunteers. In this work, we studied the biodistribution of ⁶⁸Ga-citrate and subsequent radiation exposure from it in healthy men. Methods: ⁶⁸Ga-citrate was prepared with an acetone-based radiolabeling procedure compliant with good manufacturing practices. Six healthy men (age 41 ± 12 y, mean ± SD) underwent sequential whole-body PET/CT scans after an injection of 204 ± 8 MBq of ⁶⁸Ga-citrate. Serial arterialized venous blood samples were collected during PET imaging, and the radioactivity concentration was measured with a γ-counter. Urinary voids were collected and measured. The MIRD bladder-voiding model with a 3.5-h voiding interval was used. A model using a 70-kg adult man and the MIRD schema was used to estimate absorbed doses in target organs and effective doses. Calculations were performed using OLINDA/EXM software, version 2.0. Results: Radioactivity clearance from the blood was slow, and relatively high radioactivity concentrations were observed over the whole of the 3-h measuring period. Although radioactivity excretion via urine was rather slow (biologic half-time, 69 ± 24 h), the highest decay-corrected concentrations in urinary bladder contents were measured at the 90- and 180-min time points. Moderate concentrations were also seen in kidneys, liver, and spleen. The source organs showing the largest residence times were muscle, liver, lung, and heart contents. The heart wall received the highest absorbed dose, 0.077 ± 0.008 mSv/MBq. The mean effective dose (International Commission on Radiological Protection publication 103) was 0.021 ± 0.001 mSv/MBq. Conclusion: PET imaging with ⁶⁸Ga-citrate is associated with modest radiation exposure. A 200-MBq injection of ⁶⁸Ga-citrate results in an effective radiation dose of 4.2 mSv, which is in the same range as other ⁶⁸Ga-labeled tracers. This suggests the feasibility of clinical studies using ⁶⁸Ga-citrate imaging in humans and the possibility of performing multiple scans in the same subjects across the course of a year.