A heterodimeric radioligand labeled with gallium-68 targeting fibroblast activation protein.

ABSTRACT:

Background

Fibroblast activation protein (FAP) targeting radiotracers have emerged as promising agents for cancer imaging and therapy. Recent advancements have focused on optimizing these agents for better tumor targeting and enhanced theranostic efficacy. In this study, we introduced a novel heterodimeric radioligand labeled with gallium-68, which targets FAP. We aimed to evaluate its in vitro and in vivo performance, comparing its efficacy with monomeric FAPI derivatives.

Results

The heterodimeric ligand BiFAPI was synthesized by conjugating a cyclic peptide with a quinoline-based motif via a DOTA chelator. [⁶⁸ Ga]Ga-BiFAPI demonstrated high radiochemical purity (> 95%) and exceptional stability in physiological conditions, as well as in both PBS and serum. In v

SUBMITTER: Xie C 

PROVIDER: S-EPMC12044090 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature