Fibroblast activation protein (FAP) emerges as a highly promising target for cancer diagnostic imaging and targeted radionuclide therapy. To exploit the therapeutic potential of current FAP inhibitors (FAPIs), this study presented the design and synthesis of a series of FAPI dimers to increase tumor uptake and retention. Preclinical evaluation and a pilot clinical PET imaging study were conducted to screen the lead compound with the potential for radionuclide therapy.
Three new FAPI dimers were synthesized by linking two quinoline-based FAPIs with different spacers. The in vitro binding affinity and preclinical small animal PET imaging of the compounds were compared with their monomeric counterparts, FAPI-04 and FAPI-46. The lead compound, 68Ga-LNC1013, was then evaluated in a pilot clinical PET imaging study involving seven patients with gastrointestinal cancer.
Study Type
OBSERVATIONAL
Enrollment
7
68Ga-LNC1013 was evaluated in a pilot clinical PET imaging study involving seven patients with gastrointestinal cancer.
Jian Li
Changsha, Hunan, China
Number of discrepancies between [68Ga]Ga-LNC1013 and 68Ga-FAPI-46 or 18F-FDG PET scans
Compare the diagnostic performance between \[68Ga\]Ga-LNC1013 and 68Ga-FAPI-46 or 18F-FDG in patients with gastrointestinal cancer
Time frame: 5 months
SUVmaxFAPI and SUVmaxFDG for each target (Standardized Uptake Value)
Comparison of 68Ga\]Ga-LNC1013, 68Ga-FAPI-46 and 18F-FDG Standardized Uptake Value in the primary tumor and possible metastases
Time frame: 5 months
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