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Abstract
Aim. To conduct a clinical trial of [99mTc]Tc-PSMA-BQ in patients with prostate cancer (PCa), evaluating the tolerability and safety of bolus radiopharmaceutical administration, assessing the biological distribution of the labeled peptide, and calculating radiation dose estimates.
Materials and Methods. The study included 15 patients with PCa. All patients underwent dynamic monitoring following radiopharmaceutical administration, with continuous assessment of laboratory and clinical parameters. Whole-body planar scintigraphy and SPECT/CT were performed at 2, 4, 6, and 24 hours after administration of [99mTc]Tc-PSMA-BQ at varying peptide doses — 50, 100, or 150 μg (5 patients per group). The mean administered activity was 680 ± 140 MBq. Radiopharmaceutical uptake in organs was analyzed through post-processing imaging data, and absorbed doses were calculated using OLINDA/EXM 1.1 software.
Results. [99mTc]Tc-PSMA-BQ injections were well tolerated, with no clinically significant alterations in laboratory parameters observed during monitoring. The radiopharmaceutical was primarily eliminated via renal excretion. Physiological uptake was consistently demonstrated in lacrimal and salivary glands, liver, spleen, and kidneys across all peptide doses. Mean effective doses were 0.007 ± 0.001, 0.0049 ± 0.0003, and 0.0062 ± 0.0008 mSv/MBq for the 50, 100, and 150 μg doses, respectively. The total patient radiation burden per examination ranged from 4 to 7 mSv. Primary tumor uptake was detected in all patients, demonstrating a dose-dependent increase. Maximum accumulation in lymph node and bone metastases was observed at the 100 μg peptide dose. The optimal tumor-to-background ratio was achieved 6 hours post-injection using the 100 μg formulation.
Conclusion. [99mTc]Tc-PSMA-BQ demonstrates favorable safety profiles with low radiation exposure. This radiotracer enables effective detection of both primary and metastatic lesions in PSMA-positive PCa.
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