Synthesis, Preclinical Evaluation, and a Pilot Clinical PET Imaging Study of ⁶⁸Ga-Labeled FAPI Dimer.

ABSTRACT: Cancer-associated fibroblasts (CAFs) are crucial components of the tumor microenvironment. Fibroblast activation protein (FAP) is overexpressed in CAFs. FAP-targeted molecular imaging agents, including the FAP inhibitors (FAPIs) 04 and 46, have shown promising results in tumor diagnosis. However, these molecules have a relatively short tumor-retention time for peptide-targeted radionuclide therapy applications. We aimed to design a ⁶⁸Ga-labeled FAPI dimer, ⁶⁸Ga-DOTA-2P(FAPI)₂, to optimize the pharmacokinetics and evaluate whether this form is more effective than its monomeric analogs. Methods:⁶⁸Ga-DOTA-2P(FAPI)₂ was synthesized on the basis of the quinoline-based FAPI variant (FAPI-46), and its binding properties were assayed in

SUBMITTER: Zhao L 

PROVIDER: S-EPMC9157726 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature