Synthesis of tritium-labeled Lu-PSMA-617: Alternative tool for biological evaluation of radiometal-based pharmaceuticals

Bauder-Wuest, Ulrike and Schaefer, Martin and Winter, Ruth and Remde, Yvonne and Roscher, Mareike and Breyl, Heinz and Poethko, Thorsten and Tömböly, Csaba and Benešová-Schäfer, Martina (2023) Synthesis of tritium-labeled Lu-PSMA-617: Alternative tool for biological evaluation of radiometal-based pharmaceuticals. APPLIED RADIATION AND ISOTOPES, 197. No-110819. ISSN 0969-8043

Text 1-s2.0-S0969804323001720-main.pdf - Published Version Restricted to Registered users only Download (4MB) | Request a copy

Abstract

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 ([alpha,ss-3H]Nal)PSMA-617. In particular, ([alpha,ss-3H]Nal)Lu-PSMA-617 exhibited high radiolytic as well as metalcomplex stability and was compared to the clinically-established radiopharmaceutical [177Lu]Lu-PSMA-617. The cell-based assays confirmed the applicability of ([alpha,ss-3H]Nal)Lu-PSMA-617 as a substitute of [177Lu]Lu-PSMA617 in pre-clinical biological settings.

Actions (login required)

Edit Item