
European Journal of Nuclear Medicine and Molecular Imaging, Journal Year: 2025, Volume and Issue: unknown
Published: Feb. 15, 2025
This study aims to investigate the efficacy and safety of prostate-specific membrane antigen (PSMA) radiolabeled with copper-64 (64Cu) using bifunctional chelating agents (BFCAs) NOTA (1,4,7-triazacyclononane-1,4,7-triacetic acid) DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid). As widely utilized BFCAs in development radiopharmaceuticals, play a critical role ensuring stable chelation 64Cu. evaluates stability, bioavailability, therapeutic potential these compounds preclinical models initial clinical trials. 64Cu-DOTA-PSMA-3Q 64Cu-NOTA-PSMA-3Q were synthesized by manual labeling. The radiochemical purity, specificity biological distribution product evaluated studies. In 23 patients suspected prostate cancer, PET/CT imaging was used evaluate differences diagnosis. purities are more than 98% have good stability vitro. Biodistribution studies healthy mice revealed that both tracers primarily underwent renal excretion post-injection. Liver uptake significantly higher at 1 h after injection (P<0.05). Micro-PET/CT 22Rv1 tumor-bearing demonstrated similar tumor for (P>0.05). However, 24 h, exhibited better retention compared involving no adverse reactions or significant changes vital signs observed, underscoring tracers. Notably, lacrimal glands (17.73 vs. 10.84), parotid (20.98 16.30), submandibular (20.26 17.28) 64Cu-DOTA-PSMA-3Q. Conversely, sublingual lower (7.10 7.49). Of particular relevance, liver (4.04 8.18), highlighting key difference their biodistribution profiles. Both suitable chelators 64Cu-labeled PSMA-3Q imaging. showed injection, while liver, addition, salivary glands, tissues. Overall, findings highlight importance selecting right agent optimize outcomes. Chinese Clinical Trial Registry ChiCTR2300072655, Registered 20 June 2023.
Language: Английский