Fibroblast Activation Protein (FAP) targeting homodimeric FAP inhibitor radiotheranostics: a step to improve tumor uptake and retention time.

ABSTRACT: Several radiopharmaceuticals targeting fibroblast activation protein (FAP) based on the highly potent FAP inhibitor UAMC1110 are currently under investigation. Pre-clinical as well as clinical research exhibited the potential of these imaging agents. However, the monomeric small molecules seemed to have a short retention time in the tumor in combination with fast renal clearance. Therefore, our strategy was to develop homodimeric systems having two FAP inhibitors to improve residence time and tumor accumulation. The homodimers with two squaramide coupled FAP inhibitor conjugates DOTA.(SA.FAPi)₂ and DOTAGA.(SA.FAPi)₂ were synthesized and radiochemically evaluated with gallium-68. [⁶⁸Ga]Ga-DOTAGA.(SA.FAPi)₂ was tested for its in vitro stabil

SUBMITTER: Moon ES 

PROVIDER: S-EPMC8727881 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature