[²²⁵Ac]Ac-SibuDAB for Targeted Alpha Therapy of Prostate Cancer: Preclinical Evaluation and Comparison with [²²⁵Ac]Ac-PSMA-617.

ABSTRACT: In the present study, SibuDAB, an albumin-binding PSMA ligand, was investigated in combination with actinium-225 and the data were compared with those of [²²⁵Ac]Ac-PSMA-617. In vitro, [²²⁵Ac]Ac-SibuDAB and [²²⁵Ac]Ac-PSMA-617 showed similar tumor cell uptake and PSMA-binding affinities as their ¹⁷⁷Lu-labeled counterparts. The in vitro binding to serum albumin in mouse and human blood plasma, respectively, was 2.8-fold and 1.4-fold increased for [²²⁵Ac]Ac-SibuDAB as compared to [¹⁷⁷Lu]Lu-SibuDAB. In vivo, this characteristic was reflected by the longer retention of [²²⁵Ac]Ac-SibuDAB in the blood than previously seen for [¹⁷⁷Lu]Lu-SibuDAB. Similar to [²²⁵Ac]Ac-PSMA-617, [²²⁵Ac]Ac-Sibu

SUBMITTER: Busslinger SD 

PROVIDER: S-EPMC9688344 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature