TY  - JOUR
AU  - Bauder-Wüst, Ulrike
AU  - Schäfer, Martin
AU  - Winter, Ruth
AU  - Remde, Yvonne
AU  - Roscher, Mareike
AU  - Breyl, Heinz
AU  - Poethko, Thorsten
AU  - Tömböly, Csaba
AU  - Benesova-Schäfer, Martina
TI  - Synthesis of tritium-labeled Lu-PSMA-617: Alternative tool for biological evaluation of radiometal-based pharmaceuticals.
JO  - Applied radiation and isotopes
VL  - 197
SN  - 0969-8043
CY  - Amsterdam [u.a.]
PB  - Elsevier Science
M1  - DKFZ-2023-00866
SP  - 110819
PY  - 2023
N1  - #EA:E270#LA:E270#
AB  - This project focuses on the generation and evaluation of functional alternatives to radiometal-based pharmaceuticals supporting basic research and the in vitro developmental phase. Employing robust tritium chemistry and non-radioactive metal surrogates in two synthetic and labeling strategies resulted in ([ring-3H]Nal)PSMA-617 and ([α,ß-3H]Nal)PSMA-617. In particular, ([α,ß-3H]Nal)Lu-PSMA-617 exhibited high radiolytic as well as metal-complex stability and was compared to the clinically-established radiopharmaceutical [177Lu]Lu-PSMA-617. The cell-based assays confirmed the applicability of ([α,ß-3H]Nal)Lu-PSMA-617 as a substitute of [177Lu]Lu-PSMA-617 in pre-clinical biological settings.
KW  - Labeling chemistry (Other)
KW  - PSMA ligands (Other)
KW  - PSMA-617 (Other)
KW  - Pharmaceutical development (Other)
KW  - Prostate cancer (Other)
KW  - Radiometals (Other)
KW  - Tritium (Other)
LB  - PUB:(DE-HGF)16
C6  - pmid:37119703
DO  - DOI:10.1016/j.apradiso.2023.110819
UR  - https://inrepo02.dkfz.de/record/275767
ER  -