Nuclear medicine communications · 2026
Preliminary in-vivo evaluation of [ 68 Ga]Ga-FAPI-46 in a fibroblast activation protein-negative breast cancer model.
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Hassan Hishar, Jafperi Nur Nadhira, Wan Kamal Wan Hamirul Bahrin, Mohamad Saifullizan, Sued Anee Suryani, Muhamad Siti Aminah, Mustaffa Mohd Faiz, Waeleh Nazreen, Abdul Razak Hairil Rashmizal, Othman Muhamad Faiz
Аннотация
OBJECTIVES: Fibroblast activation protein (FAP), which is abundantly expressed in cancer-associated fibroblasts, is an attractive target for tumour imaging and therapy. [ 68 Ga]Ga-FAPI-46, a gallium-68-labelled FAP inhibitor, has demonstrated favourable pharmacokinetics for PET. This study evaluated the radiolabelling efficiency, stability, and biodistribution of [ 68 Ga]Ga-FAPI-46 in a breast cancer mouse model using MCF-7 cell line, which is known to lack FAP expression.
METHODS: [ 68 Ga]Ga-FAPI-46 was radiolabeled directly from FAPI-46 using 68 Ga in acetate buffer and analysed for radiochemical purity (RCP) by radio-TLC. Stability at room temperature was assessed up to 5 h post-radiolabeling. Biodistribution studies were conducted in female BALB/c nude mice with MCF-7 tumours. Organ uptake was determined 1 h after injection and expressed as a percentage of injected dose per gramme of tissue (%ID/g). A comparative study between [ 68 Ga]Ga-FAPI-46 and free 68 Ga was also performed.
RESULTS: [ 68 Ga]Ga-FAPI-46 consistently achieved high RCP values (>95%, maximum 99.1%) and remained stable for up to 5 h without added radioprotectant. At 1 h, [ 68 Ga]Ga-FAPI-46 showed higher uptake in kidneys (4.15%ID/g), heart (3.59%ID/g), and liver (1.70%ID/g), and low uptake in muscle (0.31%ID/g) and bone (0.57%ID/g). Mean tumour uptake was low (0.92%ID/g), consistent with the FAP-negative status of MCF-7 cells. In contrast, free 68 Ga showed a non-specific distribution in blood (29.13%ID/g), lungs (18.50%ID/g), and bone (13.37%ID/g).
CONCLUSION: [ 68 Ga]Ga-FAPI-46 showed efficient radiolabelling with high RCP and short-term stability. Its low accumulation in FAP-negative tumours supports tracer selectivity and provides a baseline for comparative studies in FAP-expressing tumour models.
METHODS: [ 68 Ga]Ga-FAPI-46 was radiolabeled directly from FAPI-46 using 68 Ga in acetate buffer and analysed for radiochemical purity (RCP) by radio-TLC. Stability at room temperature was assessed up to 5 h post-radiolabeling. Biodistribution studies were conducted in female BALB/c nude mice with MCF-7 tumours. Organ uptake was determined 1 h after injection and expressed as a percentage of injected dose per gramme of tissue (%ID/g). A comparative study between [ 68 Ga]Ga-FAPI-46 and free 68 Ga was also performed.
RESULTS: [ 68 Ga]Ga-FAPI-46 consistently achieved high RCP values (>95%, maximum 99.1%) and remained stable for up to 5 h without added radioprotectant. At 1 h, [ 68 Ga]Ga-FAPI-46 showed higher uptake in kidneys (4.15%ID/g), heart (3.59%ID/g), and liver (1.70%ID/g), and low uptake in muscle (0.31%ID/g) and bone (0.57%ID/g). Mean tumour uptake was low (0.92%ID/g), consistent with the FAP-negative status of MCF-7 cells. In contrast, free 68 Ga showed a non-specific distribution in blood (29.13%ID/g), lungs (18.50%ID/g), and bone (13.37%ID/g).
CONCLUSION: [ 68 Ga]Ga-FAPI-46 showed efficient radiolabelling with high RCP and short-term stability. Its low accumulation in FAP-negative tumours supports tracer selectivity and provides a baseline for comparative studies in FAP-expressing tumour models.