Paving the way for future PSMA inhibitors: insights from comparative preclinical evaluations of structure modifications.

ABSTRACT:

Background

Prostate-specific membrane antigen (PSMA) is an established target for the imaging and treatment of prostate cancer. This study focused on the preclinical evaluation of three novel PSMA inhibitors-P15, P16, and P19-which were structurally modified compared to the clinically used PSMA-617. Two main strategies were pursued: a chemical approach following the so-called reversed synthetic strategy, and the replacement of the naphthyl-based linker moiety with an analogous diphenyl-based moiety. The aim was to assess the impact of these modifications on physicochemical properties, in vitro behaviour, and in vivo pharmacokinetics following radiolabelling with ⁶⁸Ga.

Results

Radiolabelling of all three novel compounds with ⁶⁸Ga resulted in high radiochemical purity above 98

SUBMITTER: Hajduova K 

PROVIDER: S-EPMC12474757 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature