Synthesis and Preclinical Evaluation of ¹⁷⁷Lu-Labeled Radiohybrid PSMA Ligands for Endoradiotherapy of Prostate Cancer.

ABSTRACT: The prostate-specific membrane antigen (PSMA)-targeted radiohybrid (rh) ligand [¹⁷⁷Lu]Lu-rhPSMA-7.3 has recently been assessed in a pretherapeutic dosimetry study on prostate cancer patients. In comparison to [¹⁷⁷Lu]Lu-PSMA I&T, application of [¹⁷⁷Lu]Lu-rhPSMA-7.3 resulted in a significantly improved tumor dose but also higher kidney accumulation. Although rhPSMA-7.3 has been initially selected as the lead compound for diagnostic application based on the characterization of its gallium complex, a systematic comparison of the most promising ¹⁷⁷Lu-labeled rhPSMA ligands is still missing. Thus, this study aimed to identify the rhPSMA ligand with the most favorable pharmacokinetics for ¹⁷⁷Lu-radioligand therapy. Methods: The 4 isome

SUBMITTER: Wurzer A 

PROVIDER: S-EPMC9536713 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature