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Open AccessArticle

New 55Co-labeled Albumin-Binding Folate Derivatives as Potential PET Agents for Folate Receptor Imaging

1
Department of Radiology, University of Alabama at Birmingham, Birmingham, AL 35233, USA
2
Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Paul Scherrer Institute, 5232 Villigen-PSI, Switzerland
3
Department of Chemistry and Applied Biosciences, ETH Zurich, 8093 Zurich, Switzerland
4
Department of Chemistry, University of Alabama at Birmingham, Birmingham, AL 35205, USA
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2019, 12(4), 166; https://doi.org/10.3390/ph12040166
Received: 9 October 2019 / Revised: 2 November 2019 / Accepted: 4 November 2019 / Published: 8 November 2019
Overexpression of folate receptors (FRs) on different tumor types (e.g., ovarian, lung) make FRs attractive in vivo targets for directed diagnostic/therapeutic agents. Currently, no diagnostic agent suitable for positron emission tomography (PET) has been adopted for clinical FR imaging. In this work, two 55Co-labeled albumin-binding folate derivatives-[55Co]Co-cm10 and [55Co]Co-rf42-with characteristics suitable for PET imaging have been developed and evaluated. High radiochemical yields (≥95%) and in vitro stabilities (≥93%) were achieved for both compounds, and cell assays demonstrated FR-mediated uptake. Both 55Co-labeled folate conjugates demonstrated high tumor uptake of 17% injected activity per gram of tissue (IA/g) at 4 h in biodistribution studies performed in KB tumor-bearing mice. Renal uptake was similar to other albumin-binding folate derivatives, and liver uptake was lower than that of previously reported [64Cu]Cu-rf42. Small animal PET/CT images confirmed the biodistribution results and showed the clear delineation of FR-expressing tumors. View Full-Text
Keywords: folic acid; folate receptors; cobalt-55; PET imaging; albumin binder; ovarian cancer folic acid; folate receptors; cobalt-55; PET imaging; albumin binder; ovarian cancer
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MDPI and ACS Style

Radford, L.L.; Fernandez, S.; Beacham, R.; El Sayed, R.; Farkas, R.; Benešová, M.; Müller, C.; Lapi, S.E. New 55Co-labeled Albumin-Binding Folate Derivatives as Potential PET Agents for Folate Receptor Imaging. Pharmaceuticals 2019, 12, 166.

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