In this study, a novel FAPI-04 dimer was synthesized and labeled with radionuclides to prolong the retention time in tumors for imaging and therapy. To prepare the FAPI-04 dimer complex, DOTA-Suc-Lys- (FAPI-04) 2, we used Fmoc-Lys (Boc)–OH as the linker to conjugate two FAPI-04 structures by an amide reaction.

FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68 Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios.

FAPI-04 turned out to be the most promising because of good stability in human serum, high affinity for FAP, and high tumor uptake. Two patients with metastatic breast cancer were evaluated with 68 Ga-FAPI-04 and then treated with 90 Y-FAPI-04.

Dec 22, 2024 · A bivalent agent, DOTA-NI-FAPI-04 (1), was developed by incorporating hypoxia-sensitive nitroimidazole (NI) into the FAP-targeting agent FAPI-04. Compound 1 exhibited a strong FAP binding affinity with an IC 50 of 7.44 nM.

Mar 6, 2025 · The purpose of this study was to determine the difference in fibroinflammatory activity shown on 68 Ga-FAPI-04 and 18 F-FDG PET/CT in the proliferative and fibrotic IgG4-RD subtypes.

Oct 1, 2024 · 68 Ga-FAPI-04 PET/CT imaging surpasses 18 F-FDG PET/CT in detecting the primary tumor, especially in poorly cohesive and signet-ring cell gastric cancer types, and offers improved accuracy in disease staging.

Apr 1, 2024 · This study aimed to assess the diagnostic efficiency of 68 Ga-labeled FAP inhibitor (FAPI)-04 PET/CT for detecting lymph node metastasis in non-small cell lung cancer (NSCLC) and to investigate the correlation between tumor 68 Ga-FAPI-04 uptake and FAP expression.

Dec 4, 2024 · 18F-FAPI-04 PET/CT exhibits higher uptake and TBR in most tumors demonstrating superior diagnostic efficacy for primary lesions, residual/recurrent disease, and metastases compared to 18F-FDG PET/CT, particularly beneficial …

PET/CT imaging in mice showed that physiological uptake of [18 F]AlF-NOTA-FAPI-04 was mainly in the biliary system and bladder, and [18 F]AlF-NOTA-FAPI-04 highly concentrated in tumor xenografts.

Jun 1, 2024 · In this study, nitroimidazole was added to FAPI-04 to give DOTA-NI-FAPI-04 (compound 1) which led to excellent tumor accumulation and prolonged residence time after labeling with Ga-68 and Lu-177.