Journal Article

DKFZ-2023-00866

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Synthesis of tritium-labeled Lu-PSMA-617: Alternative tool for biological evaluation of radiometal-based pharmaceuticals.

Bauder-Wüst, U. (First author)DKFZ* ; Schäfer, M.DKFZ* ; Winter, R.DKFZ* ; Remde, Y.DKFZ* ; Roscher, M.DKFZ* ; Breyl, H.DKFZ* ; Poethko, T. ; Tömböly, C. ; Benesova-Schäfer, M. (Last author)DKFZ*

2023
Elsevier Science Amsterdam [u.a.]

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Please use a persistent id in citations: doi:10.1016/j.apradiso.2023.110819

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 ([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.

Keyword(s): Labeling chemistry ; PSMA ligands ; PSMA-617 ; Pharmaceutical development ; Prostate cancer ; Radiometals ; Tritium

Note: #EA:E270#LA:E270#

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Contributing Institute(s):

1. NWG Molekularbiologie Systemischer Radiotherapie (E270)
2. Radiopharmazeutika und Präklinische Studien (W630)
3. Strahlenschutz und Dosimetrie (W060)

Research Program(s):

1. 315 - Bildgebung und Radioonkologie (POF4-315) (POF4-315)

Appears in the scientific report 2023

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Database coverage:
; Clarivate Analytics Master Journal List ; Current Contents - Physical, Chemical and Earth Sciences ; Ebsco Academic Search ; Essential Science Indicators ; IF < 5 ; JCR ; Nationallizenz ; SCOPUS ; Science Citation Index Expanded ; Web of Science Core Collection

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