Gastrointestinal Cancer
Conditions
Keywords
FAPI dimer
Brief summary
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.
Detailed description
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.
Interventions
DIAGNOSTIC_TEST68Ga-FAPI dimer(68Ga-LNC1013)
68Ga-LNC1013 was evaluated in a pilot clinical PET imaging study involving seven patients with gastrointestinal cancer.
Sponsors
Xiangya Hospital of Central South University
Study design
Observational model
CASE_ONLY
Time perspective
PROSPECTIVE
Eligibility
Sex/Gender
ALL
Age
18 Years to 80 Years
Inclusion criteria
1. Histologically and/or clinically confirmed and/or suspicious of gastrointestinal cancer. 2. Signed informed consent.
Exclusion criteria
1. pregnancy; 2. breastfeeding; 3. any medical condition that in the opinion of the investigator may significantly interfere with study compliance.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Number of discrepancies between [68Ga]Ga-LNC1013 and 68Ga-FAPI-46 or 18F-FDG PET scans | 5 months | Compare the diagnostic performance between \[68Ga\]Ga-LNC1013 and 68Ga-FAPI-46 or 18F-FDG in patients with gastrointestinal cancer |
| SUVmaxFAPI and SUVmaxFDG for each target (Standardized Uptake Value) | 5 months | Comparison of 68Ga\]Ga-LNC1013, 68Ga-FAPI-46 and 18F-FDG Standardized Uptake Value in the primary tumor and possible metastases |
Countries
China
Outcome results
None listed