TY  - JOUR
AU  - Bhardwaj, Punita
AU  - Frohner, Caroline
AU  - Geppert, Christopher
AU  - Gorges, Christian
AU  - Brenner, Winfried
AU  - Claude, Guilhem
AU  - Spreckelmeyer, Sarah
TI  - Synthesis and in vitro characterization of [198Au]Auranofin.
JO  - EJNMMI radiopharmacy and chemistry
VL  - 10
IS  - 1
SN  - 2365-421X
CY  - [Cham, Switzerland]
PB  - Springer International Publishing
M1  - DKFZ-2025-02288
SP  - 71
PY  - 2025
AB  - Radiopharmaceuticals offer targeted treatment by combining diagnostic or therapeutic radionuclides with biologically active molecules. Auranofin is the only Food and Drug Administration (FDA) approved gold(I) complex, originally developed for the treatment of rheumatoid arthritis. Recent evidence has highlighted its potential as an anticancer agent due to its ability to disrupt redox signaling, inhibit thioredoxin reductase, and impair glycolytic metabolism. This study aims to incorporate the true theranostic radionuclide 198Au into the Auranofin scaffold and evaluate its impact in-vitro on cancer cells.Carrier-added (c.a.)198Au was produced via neutron activation of 197Au and subsequently converted into c.a. H [198Au] [AuCl₄]. Downscaled synthetic protocols were developed to sequentially generate c.a. [198Au] [Au(tht)Cl], [198Au] [Au(PEt₃)Cl], and [198Au]Auranofin. Radiochemical purity was evaluated using radio-high performance liquid chromatography, and in vitro stability was assessed in human serum albumin (HSA) over 72 h. Cytotoxic and metabolic activity were investigated in MCF7 and PC3 cancer cell lines using the cell viability assay 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT assay) and hexokinase assay, respectively. [198Au]Auranofin (c.a.) was obtained with a yield of 57.0 ± 3.2
KW  - 198Au (Other)
KW  - Auranofin (Other)
KW  - Cancer therapy (Other)
KW  - Gold(i) complex (Other)
KW  - Nuclear medicine (Other)
KW  - Radiotheranostics (Other)
KW  - Redox metabolism (Other)
KW  - SPECT imaging (Other)
LB  - PUB:(DE-HGF)16
C6  - pmid:41191187
DO  - DOI:10.1186/s41181-025-00401-3
UR  - https://inrepo02.dkfz.de/record/305656
ER  -