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@ARTICLE{Mamlins:1028499,
author = {Mamlins, Eduards and Scharbert, Lara and Cardinale, Jens
and Krotov, Maria and Winter, Erik and Rathke, Hendrik and
Strodel, Birgit and Ankrah, Alfred O. and Sathekge, Mike and
Haberkorn, Uwe and Kratochwil, Clemens and Giesel, Frederik
L.},
title = {{T}he {T}heranostic {O}ptimization of {PSMA}-{GCK}01 {D}oes
{N}ot {C}ompromise the {I}maging {C}haracteristics of
[99m{T}c]{T}c-{PSMA}-{GCK}01 {C}ompared to {D}edicated
{D}iagnostic [99m{T}c]{T}c-{EDDA}/{HYNIC}-i{PSMA} in
{P}rostate {C}ancer},
journal = {Molecular imaging $\&$ biology},
volume = {26},
number = {1},
issn = {1536-1632},
address = {Cham},
publisher = {Springer Nature Switzerland},
reportid = {FZJ-2024-04651},
pages = {81 - 89},
year = {2024},
abstract = {PURPOSE: Radiolabeled PSMA-ligands play a major role in
today's nuclear medicine. Since approval of
[177Lu]Lu-PSMA-617 for therapy of metastatic prostate
cancer, availability of 177Lu became bottleneck of supply
due to the high demand. Recently, a theranostic PSMA-ligand,
PSMA-GCK01, was developed which can be labeled either
diagnostically with 99mTc or therapeutically with 188Re with
both nuclides available from well-known generator systems.
This novel tracer might aid to overcome aforementioned
supply limitations. In this investigation, the
biodistribution and general imaging characteristics of
[99mTc]Tc-PSMA-GCK01 were compared with the diagnostic
reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients
with advanced stage prostate cancer. In addition, the
binding of both ligands to PSMA was analyzed at the
molecular level using molecular docking.PROCEDURES: Two
cohorts (n = 19 vs. n = 21) of patients with metastatic
castration-resistant prostate cancer matched for age, tumor
stage, and Gleason score underwent a planar gamma camera
imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or
[99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for
PSMA-phenotyping. The imaging data were retrospective
analyzed for salivary gland, kidney, liver, soft tissue, and
tumor uptake on a semi-automated ROI-analysis using HERMES
Medical Solutions AB (HMS, Sweden).RESULTS: The data sets
were semi-automated quantified on a ROI-based analysis. The
tumor-to-background presented equal results of
[99mTc]Tc-PSMA-GCK01 compared to [99mTc]Tc-EDDA/HYNIC-iPSMA.
The physiological PSMA-positive organs like salivary gland
presented also equal uptake in counts/MBq (salivary gland
median 9.48 [99mTc]Tc-PSMA-GCK01 vs. median 9.11
[99mTc]Tc-EDDA/HYNIC-iPSMA), while liver-to-kidney ratio
presented a slight shift to the liver parenchyma using
[99mTc]Tc-PSMA-GCK01 (0.83) compared to
[99mTc]Tc-EDDA/HYNIC-iPSMA (0.55) with no statistical
significance. This is in agreement with the results from the
docking study revealing only a minor difference in the
docking scores for both ligands.CONCLUSIONS: The novel
theranostic tracer [99mTc]Tc/[188Re]Re-PSMA-GCK01
demonstrates comparable general imaging characteristic with
the reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA. These
results pave the way for the PSMA-targeting imaging and
theranostic agents for a broader, rather low-cost, generator
applied radio-ligand therapy utilization.},
cin = {IBI-7},
ddc = {570},
cid = {I:(DE-Juel1)IBI-7-20200312},
pnm = {5241 - Molecular Information Processing in Cellular Systems
(POF4-524)},
pid = {G:(DE-HGF)POF4-5241},
typ = {PUB:(DE-HGF)16},
pubmed = {38066252},
UT = {WOS:001117836400001},
doi = {10.1007/s11307-023-01881-y},
url = {https://juser.fz-juelich.de/record/1028499},
}