TY  - JOUR
AU  - Hajduová, Katarína
AU  - Bendová, Kateřina Dvořáková
AU  - Petřík, Miloš
AU  - Benesova-Schäfer, Martina
AU  - Schäfer, Martin
AU  - Hajdúch, Marián
AU  - Nový, Zbyněk
TI  - Paving the way for future PSMA inhibitors: insights from comparative preclinical evaluations of structure modifications.
JO  - EJNMMI radiopharmacy and chemistry
VL  - 10
IS  - 1
SN  - 2365-421X
CY  - [Cham, Switzerland]
PB  - Springer International Publishing
M1  - DKFZ-2025-01975
SP  - 63
PY  - 2025
AB  - 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
KW  - PSMA (Other)
KW  - Preclicnical PET/CT (Other)
KW  - Prostate cancer (Other)
KW  - Radiopharmaceuticals (Other)
KW  - Theranostics (Other)
LB  - PUB:(DE-HGF)16
C6  - pmid:41003962
C2  - pmc:PMC12474757
DO  - DOI:10.1186/s41181-025-00389-w
UR  - https://inrepo02.dkfz.de/record/304984
ER  -