Development of CD46 targeted alpha theranostics in prostate cancer using ¹³⁴Ce/²²⁵Ac-Macropa-PEG₄-YS5.

ABSTRACT: Rationale: ²²⁵Ac, a long-lived α-emitter with a half-life of 9.92 days, has garnered significant attention as a therapeutic radionuclide when coupled with monoclonal antibodies and other targeting vectors. Nevertheless, its clinical utility has been hampered by potential off-target toxicity, a lack of optimized chelators for ²²⁵Ac, and limitations in radiolabeling methods. In a prior study evaluating the effectiveness of CD46-targeted radioimmunotherapy, we found great therapeutic efficacy but also significant toxicity at higher doses. To address these challenges, we have developed a radioimmunoconjugate called ²²⁵Ac-Macropa-PEG₄-YS5, incorporating a stable PEGylated linker to maximize tumoral uptake and increase tumor-to-background ratios

SUBMITTER: Bobba KN 

PROVIDER: S-EPMC10879874 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature