Biodistribution and internal radiation dosimetry of a novel probe for thymidine phosphorylase imaging, [I]IIMU, in healthy volunteers.

Objective: We evaluated the radiation dosage, biodistribution, human safety, and tolerability of the injection of a single dose of [I] 5-iodo-6-[(2-iminoimidazolidinyl)methyl]uracil (IIMU), a new radiotracer targeting thymidine phosphorylase (TP), in healthy volunteers.

Methods: Potential participants were tested at our hospital to confirm their eligibility. Two healthy male adults passed the screening tests. They were injected with 56 and 111 MBq of [I]IIMU, respectively. Safety assessments were performed before and at 1, 3, 6, 9, 24, 48 h, and 1-week post-injection. Whole-body emission scans were conducted at 1, 3, 6, 24, and 48 h post-injection. Regions of interest were manually drawn to enclose the entire body at each time point, identifying high-uptake organs to obtain the time-activity curves. Urine and blood samples were collected at 1, 2, 3, 4, 5, 6, 9, 24, and 48 h post-injection. The radiation dose for each organ and the effective doses were estimated using OLINDA/EXM 1.1 software.

Results: No adverse events were observed as of the follow-up visit > 1-week post-injection. In both subjects, the highest uptake of [I]IIMU occurred in the liver, with peak injected activity (%IA) values of 17.7% and 15.1%, respectively. The second highest uptake was in the thyroid (0.35% and 0.66% IA). The %IA decreased gradually toward the end of the study (48 h) in all organs except the liver and thyroid. By the end of the study, 52.5% and 51.5% of the injected activity of [I]IIMU had been excreted via the subjects' renal systems. The estimated mean effective doses of [I]IIMU were 9.19 μSv/MBq and 10.1 μSv/MBq, respectively.

Conclusion: In this preliminary study, [I]IIMU was safely administered to healthy adults, and its potential clinical use in TP imaging was revealed.