Preclinical Evaluation of a New Series of Albumin-Binding ¹⁷⁷Lu-Labeled PSMA-Based Low-Molecular-Weight Radiotherapeutics.

ABSTRACT: Prostate-specific membrane antigen (PSMA)-based low-molecular-weight agents using beta(β)-particle-emitting radiopharmaceuticals is a new treatment paradigm for patients with metastatic castration-resistant prostate cancer. Although results have been encouraging, there is a need to improve the tumor residence time of current PSMA-based radiotherapeutics. Albumin-binding moieties have been used strategically to enhance the tumor uptake and retention of existing PSMA-based investigational agents. Previously, we developed a series of PSMA-based, β-particle-emitting, low-molecular-weight compounds. From this series, ¹⁷⁷Lu-L1 was selected as the lead agent because of its reduced off-target radiotoxicity in preclinical studies. The ligand L1 contains a PSMA-targeting Lys-Glu urea moie

SUBMITTER: Boinapally S 

PROVIDER: S-EPMC10459686 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature