Preclinical characterization of 3p-C-DEPA_-NCS and 3p-C-DEPA_-TFP-PEG₄ as potential Actinium-225 bifunctional chelators using DOTA_-NCS and macropa_-NCS as benchmarks.

ABSTRACT:

Background

Actinium-225 (²²⁵Ac) based targeted alpha therapies (TAT) have emerged as a promising strategy for the treatment of several cancer types due to its favourable decay properties, including high linear energy transfer and short particle range, which enable precise tumour targeting. However, there are limited bifunctional chelators (BFCs) available for ²²⁵Ac. In this study, we aim to evaluate the potential of DEPA-based chelators for ²²⁵Ac-labelling.

Results

The BFCs 3p-C-DEPA-_NO2, 3p-C-DEPA-_NCS, and 3p-C-DEPA_-TFP-PEG₄ were synthesized with high yield (≥ 86%) and purity (> 96%). Excellent radiochemical conversions (RCCs) were achieved for [²²⁵Ac]Ac-3p-C-DEPA-_NO2 across a

SUBMITTER: Pougoue Ketchemen J 

PROVIDER: S-EPMC12722590 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature