Preliminary in-vivo evaluation of [68Ga]Ga-FAPI-46 in a fibroblast activation protein–negative breast cancer model

Hassan, Hishar and Othman, Muhamad Faiz and Jafperi, Nur Nadhira and Mustaffa, Mohd Faiz and Wan Kamal, Wan Hamirul Bahrin and Mohamad, Saifullizan and Sued, Anee Suryani and Muhamad, Siti Aminah and Waeleh, Nazreen and Abdul Razak, Hairil Rashmizal (2026) Preliminary in-vivo evaluation of [68Ga]Ga-FAPI-46 in a fibroblast activation protein–negative breast cancer model. Nuclear Medicine Communications, 47. pp. 672-678. ISSN 0143-3636

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Abstract

Objectives – Fibroblast activation protein (FAP), which is abundantly expressed in cancer-associated fibroblasts, is an attractive target for tumour imaging and therapy. [68Ga]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 [68Ga]Ga-FAPI-46 in a breast cancer mouse model using MCF-7 cell line, which is known to lack FAP expression. Methods – [68Ga]Ga-FAPI-46 was radiolabeled directly from FAPI-46 using 68Ga 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 [68Ga]Ga-FAPI-46 and free 68Ga was also performed. Results – [68Ga]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, [68Ga]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 68Ga showed a non-specific distribution in blood (29.13%ID/g), lungs (18.50%ID/g), and bone (13.37%ID/g). Conclusion – [68Ga]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.

Item Type:	Article
Uncontrolled Keywords:	Biodistribution, Breast cancer, Fibroblast activation protein, MCF-7, Preclinical PET imaging, [68Ga]Ga-FAPI-46
Divisions:	Faculty Of Electronics And Computer Technology And Engineering
Depositing User:	Sabariah Ismail
Date Deposited:	20 Jul 2026 07:46
Last Modified:	20 Jul 2026 07:46
URI:	http://eprints.utem.edu.my/id/eprint/30036
Statistic Details:	View Download Statistic

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