Preclinical Evaluation of Biodistribution and Toxicity of [²¹¹At]PSMA-5 in Mice and Primates for the Targeted Alpha Therapy against Prostate Cancer.

ABSTRACT: Astatine (²¹¹At) is a cyclotron-produced alpha emitter with a physical half-life of 7.2 h. In our previous study, the ²¹¹At-labeled prostate-specific membrane antigen (PSMA) compound ([²¹¹At]PSMA-5) exhibited excellent tumor growth suppression in a xenograft model. We conducted preclinical biodistribution and toxicity studies for the first-in-human clinical trial. [²¹¹At]PSMA-5 was administered to both normal male ICR mice (n = 85) and cynomolgus monkeys (n = 2). The mice were divided into four groups for the toxicity study: 5 MBq/kg, 12 MBq/kg, 35 MBq/kg, and vehicle control, with follow-ups at 1 day (n = 10 per group) and 14 days (n = 5 per group). Monkeys were observed 24 h post-administration of [²¹¹At]P

SUBMITTER: Watabe T 

PROVIDER: S-EPMC11172375 | biostudies-literature | 2024 May

REPOSITORIES: biostudies-literature