%0 Journal Article
%A Hajduová, Katarína
%A Bendová, Kateřina Dvořáková
%A Petřík, Miloš
%A Benesova-Schäfer, Martina
%A Schäfer, Martin
%A Hajdúch, Marián
%A Nový, Zbyněk
%T Paving the way for future PSMA inhibitors: insights from comparative preclinical evaluations of structure modifications.
%J EJNMMI radiopharmacy and chemistry
%V 10
%N 1
%@ 2365-421X
%C [Cham, Switzerland]
%I Springer International Publishing
%M DKFZ-2025-01975
%P 63
%D 2025
%X 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.Radiolabelling of all three novel compounds with ⁶⁸Ga resulted in high radiochemical purity above 98
%K PSMA (Other)
%K Preclicnical PET/CT (Other)
%K Prostate cancer (Other)
%K Radiopharmaceuticals (Other)
%K Theranostics (Other)
%F PUB:(DE-HGF)16
%9 Journal Article
%$ pmid:41003962
%2 pmc:PMC12474757
%R 10.1186/s41181-025-00389-w
%U https://inrepo02.dkfz.de/record/304984