Research Article
In Vivo Evaluation of Gallium-68-Labeled IRDye800CW as a
Necrosis Avid Contrast Agent in Solid Tumors
Marcus C.M. Stroet ,
1,2
Erik de Blois ,
1
Joost Haeck ,
3
Yann Seimbille ,
1,4
Laura Mezzanotte ,
1,2
Marion de Jong ,
1
ClemensW.G.M.L¨ owik ,
1,2,5
and Kranthi M. Panth
1,2
1
Erasmus MC, University Medical Center Rotterdam, Department of Radiology & Nuclear Medicine, Rotterdam, Netherlands
2
Erasmus MC, University Medical Center Rotterdam, Department of Molecular Genetics, Rotterdam, Netherlands
3
AMIE Core Facility, Erasmus MC, Rotterdam, Netherlands
4
Life Sciences Division, TRIUMF, Vancouver, Canada
5
CHUV Department of Oncology, University of Lausanne, Lausanne, Switzerland
Correspondence should be addressed to Clemens W.G.M. L¨ owik; c.lowik@erasmusmc.nl and Kranthi M. Panth; k.panth@
erasmusmc.nl
Received 15 October 2021; Revised 17 November 2021; Accepted 18 November 2021; Published 13 December 2021
Academic Editor: Guillermina Ferro Flores
Copyright © 2021 Marcus C.M. Stroet et al. is is an open access article distributed under the Creative Commons Attribution
License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is
properly cited.
Necrosis only occurs in pathological situations and is directly related to disease severity and, therefore, is an important biomarker.
Tumor necrosis occurs in most solid tumors due to improperly functioning blood vessels that cannot keep up with the rapid
growth, especially in aggressively growing tumors. e amount of necrosis per tumor volume is often correlated to rapid tumor
proliferation and can be used as a diagnostic tool. Furthermore, efficient therapy against solid tumors will directly or indirectly
lead to necrotic tumor cells, and detection of increased tumor necrosis can be an early marker for therapy efficacy. We propose the
application of necrosis avid contrast agents to detect therapy-induced tumor necrosis. Herein, we advance gallium-68-labeled
IRDye800CW, a near-infrared fluorescent dye that exhibits excellent necrosis avidity, as a potential PETtracer for in vivo imaging
of tumor necrosis. We developed a reliable labeling procedure to prepare [
68
Ga]Ga-DOTA-PEG
4
-IRDye800CW ([
68
Ga]Ga-1)
with a radiochemical purity of >96% (radio-HPLC). e prominent dead cell binding of fluorescence and radioactivity from
[
68
Ga]Ga-1 was confirmed with dead and alive cultured 4T1-Luc2 cells. [
68
Ga]Ga-1 was injected in 4T1-Luc2 tumor-bearing mice,
and specific fluorescence and PET signal were observed in the spontaneously developing tumor necrosis. e ip injection of
D-luciferin enabled simultaneous bioluminescence imaging of the viable tumor regions. Tumor necrosis binding was confirmed
ex vivo by colocalization of fluorescence uptake with TUNEL dead cell staining and radioactivity uptake in dichotomized tumors
and frozen tumor sections. Our presented study shows that [
68
Ga]Ga-1 is a promising PET tracer for the detection of
tumor necrosis.
1.Introduction
Excessive occurrence of cell death is a hallmark for severe
disease in many pathologies, such as sepsis [1], pancreatitis
[2], or acute myocardial infarction [3]. Moreover, most solid
tumors develop necrotic tissue due to the growth rate of the
tumor mass surpassing the rate of vascularization. As a
result, tumor necrosis is often associated with aggressive
tumor types and poor disease prognosis [4, 5]. Currently,
noninvasive techniques for necrosis detection are lacking in
the clinic. ere have been several agents reaching clinical
trials targeting apoptosis markers, for instance, radiolabeled
Annexin V, which targets exposed phosphoserines [6], or
[
18
F]ICMT-11 targeting caspase-3/7 activation [7, 8].
However, due to the lack of specificity, these tracers have so
far failed to reach the clinic [9–11].
Hindawi
Contrast Media & Molecular Imaging
Volume 2021, Article ID 2853522, 8 pages
https://doi.org/10.1155/2021/2853522