Development of a Novel Imaging Agent for Determining Albumin Uptake in Solid Tumors View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2019-02-20

AUTHORS

S. Daum, J. P. Magnusson, L. Pes, J. Garcia Fernandez, S. Chercheja, F. Medda, F. I. Nollmann, S. D. Koester, P. Perez Galan, A. Warnecke, K. Abu Ajaj, Felix Kratz

ABSTRACT

The purpose of this study was to investigate the albumin-binding compound 111In-C4-DTPA as an imaging agent for the detection of endogenous albumin accumulation in tumors. 111In-C4-DTPA was injected in healthy nude mice for pharmacokinetic and biodistribution studies (10 min, 1, 6, 24, and 48 h, n = 4) and subsequently in tumor-bearing mice for single-photon emission computed tomography/X-ray-computed tomography (SPECT/CT) imaging studies. Four different human tumor xenograft models (LXFL529, OVXF899, MAXFTN401, and CXF2081) were implanted subcutaneously unilaterally or bilaterally (n = 4–8). After intravenous administration of 111In-C4-DTPA, SPECT/CT images were collected over 72 h at 4–6 time points. Additionally, gamma counting was performed for the blood, plasma, lungs, heart, liver, spleen, kidneys, muscle, and tumors at 72 h post-injection. 111In-C4-DTPA bound rapidly to circulating albumin upon injection, and the radiolabeled albumin conjugate thus formed was stable in murine and human serum. SPECT/CT images demonstrated a time-dependent uptake with a maximum of 2.7–3.8% ID/cm3 in the tumors at approximately 24 h post-injection and mean tumor/muscle ratios in the range of 3.2–6.2 between 24 and 72 h post-injection. The kidneys and bladder were the predominant elimination organs. Gamma counting at 72 h post-injection showed 1.3–2.5% ID/g in the tumors and mean tumor/muscle ratios in the range of 4.9–9.4. 111In-C4-DTPA bound rapidly to circulating albumin upon injection and showed time-dependent uptake in the tumors demonstrating a potential for clinical application as a companion imaging diagnostic for albumin-binding anticancer drugs. More... »

PAGES

1-10

References to SciGraph publications

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s13139-019-00587-w

DOI

http://dx.doi.org/10.1007/s13139-019-00587-w

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1112262229


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