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


ABSTRACT: 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.

SUBMITTER: Radford LL 

PROVIDER: S-EPMC6958329 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature

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New <sup>55</sup>Co-labeled Albumin-Binding Folate Derivatives as Potential PET Agents for Folate Receptor Imaging.

Radford Lauren L LL   Fernandez Solana S   Beacham Rebecca R   El Sayed Retta R   Farkas Renata R   Benešová Martina M   Müller Cristina C   Lapi Suzanne E SE  

Pharmaceuticals (Basel, Switzerland) 20191108 4


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 <sup>55</sup>Co-labeled albumin-binding folate derivatives-[<sup>55</sup>Co]Co-cm10 and [<sup>55</sup>Co]Co-rf42-with characteristics suitable for PET imaging have been developed and evaluated.  ...[more]

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