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

Pharmaceuticals

Renata Farkas¹  Martina Benešová¹  Cristina Müller¹  Rebecca Beacham²  LaurenL. Radford²  Solana Fernandez²  Retta El Sayed²  SuzanneE. Lapi² 

[1] Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Paul Scherrer Institute, 5232 Villigen-PSI, Switzerland;Department of Radiology, University of Alabama at Birmingham, Birmingham, AL 35233, USA;

关键词: folic acid;    folate receptors;    cobalt-55;    pet imaging;    albumin binder;    ovarian cancer;   

DOI  :  10.3390/ph12040166

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown