Related Experiment Video
Updated: Jun 26, 2026
![Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F68356.jpg&w=3840&q=50)
Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
Published on: April 25, 2025
Development of Glycosylated and Dimeric FAP-Targeted Radiotracers for Preclinical Evaluation in FAP-Positive
Jin Tian1,2,3, Luming Sun2,4, Chaoquan Lai2,5
1School of Pharmacy and Food Engineering, Wuyi University, Jiangmen, Guangdong 529020, China.
Abstract:
Fibroblast activation protein (FAP) is an important target for tumor diagnosis and therapy. In this study, two FAP-targeted radioligands, the monomeric [68Ga]Ga-DOTA-T1-FAPI and the dimeric [68Ga]Ga-DOTA-T1-(FAPI)2, were designed by introducing a glucose linker into FAPI-04 and its dimer, and their FAP-targeting capability was further evaluated. In vitro studies demonstrated that [68Ga]Ga-DOTA-T1-(FAPI)2 exhibited specific uptake in FAP-positive U87 MG cells. Small animal positron emission tomography and computed tomography (PET/CT) imaging and biodistribution studies showed that the dimeric tracer exhibited higher tumor uptake (9.5 ± 1.75% ID/g at 30 min) and superior tumor-to-nontarget ratios compared with [68Ga]Ga-DOTA-T1-FAPI (3.02 ± 0.19% ID/g at 30 min) and [68Ga]Ga-DOTA-FAPI-04 (1.44 ± 0.34% ID/g at 30 min). Furthermore, [177Lu]Lu-DOTA-T1-(FAPI)2 displayed high tumor uptake (10.83 ± 1.92% ID/g at 4 h) and favorable imaging contrast. Overall, the combination of glycosylation and dimerization provides a promising strategy for developing efficient FAP-targeted diagnostic and therapeutic radioligands.
![An Automated Radiosynthesis of [68Ga]Ga-FAPI-46 for Routine Clinical Use](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F66708.jpg&w=3840&q=50)
