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

Overview

Journal Pharmaceuticals (Basel)

Publisher MDPI

Specialty Chemistry

Date 2019 Nov 14

PMID 31717279

Citations 11

Authors

Lauren L Radford

Solana Fernandez

Rebecca Beacham

Retta El Sayed

Renata Farkas

Martina Benesova

Cristina Muller

Suzanne E Lapi

Affiliations

Soon will be listed here.

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 Co-labeled albumin-binding folate derivatives-[Co]Co-cm10 and [Co]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 Co-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 [Cu]Cu-rf42. Small animal PET/CT images confirmed the biodistribution results and showed the clear delineation of FR-expressing tumors.

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