Refined Chelator Spacer Moieties Ameliorate the Pharmacokinetics of PSMA-617.

ABSTRACT: Prostate-specific membrane antigen (PSMA) binding tracers are promising agents for the targeting of prostate tumors. To further optimize the clinically established radiopharmaceutical PSMA-617, novel PSMA ligands for prostate cancer endoradiotherapy were developed. A series of PSMA binding tracers that comprise a benzyl group at the chelator moiety were obtained by solid-phase synthesis. The compounds were labeled with ⁶⁸Ga or ¹⁷⁷Lu. Competitive cell-binding assays and internalization assays were performed using the cell line C4-2, a subline of the PSMA positive cell line LNCaP (human lymph node carcinoma of the prostate). Positron emission tomography (PET) imaging and biodistribution studies were conducted in a C4-2 tumor bearing BALB/c nu/nu mouse model. All ⁶⁸

SUBMITTER: Dos Santos JC 

PROVIDER: S-EPMC9396645 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature