Non-invasive visualization of liver fibrosis with [68Ga]Ga-DOTA-FAPI-04 PET from preclinical insights to clinical translation.

Purpose: The reversibility of early liver fibrosis highlights the need for improved early detection and monitoring techniques. Fibroblast activation protein (FAP) is a promising theranostics target significantly upregulated during fibrosis. This preclinical and preliminary clinical study investigate...

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Publicado en:European Journal of Nuclear Medicine & Molecular Imaging Vol. 51; no. 12; pp. 3572 - 3585
Autores principales: Song, Yangmeihui, Qin, Chunxia, Chen, Yixiong, Ruan, Weiwei, Gai, Yongkang, Song, Wenyu, Gao, Yu, Hu, Wenzhu, Qiao, Pengxin, Song, Xiangming, Lv, Xiaoying, Zheng, Danzha, Chu, Huikuan, Jiang, Dawei, Yang, Ling, Lan, Xiaoli
Formato: Journal Article
Publicado: Springer Nature Oct2024
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Oct2024
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      pub: Springer Nature
      place: New York, New York
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        atl: Non-invasive visualization of liver fibrosis with [68Ga]Ga-DOTA-FAPI-04 PET from preclinical insights to clinical translation.
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        au:
          Song, Yangmeihui
          Qin, Chunxia
          Chen, Yixiong
          Ruan, Weiwei
          Gai, Yongkang
          Song, Wenyu
          Gao, Yu
          Hu, Wenzhu
          Qiao, Pengxin
          Song, Xiangming
          Lv, Xiaoying
          Zheng, Danzha
          Chu, Huikuan
          Jiang, Dawei
          Yang, Ling
          Lan, Xiaoli
        affil: Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, No. 1277 Jiefang Ave, 430022, Wuhan, Hubei Province, China
      sug:
      ab: Purpose: The reversibility of early liver fibrosis highlights the need for improved early detection and monitoring techniques. Fibroblast activation protein (FAP) is a promising theranostics target significantly upregulated during fibrosis. This preclinical and preliminary clinical study investigated a FAP-targeted probe, gallium-68-labeled FAP inhibitor 04 ([68Ga]Ga-DOTA-FAPI-04), for its capability to visualize liver fibrosis. Methods: The preclinical study employed [68Ga]Ga-DOTA-FAPI-04 micro-positron emission tomography (PET)/computed tomography (CT) on carbon tetrachloride-induced mice model (n = 34) and olive oil-treated control group (n = 26), followed by validation of the probe's biodistribution. Hepatic uptake was correlated with fibrosis and inflammation levels, quantified through histology and serum assays. FAP and α-smooth muscle actin expression were determined by immunohistochemistry, as well as immunofluorescence. The subsequent clinical trial enrolled 26 patients with suspected or confirmed liver fibrosis to undergo [68Ga]Ga-DOTA-FAPI-04 PET/magnetic resonance imaging or PET/CT. Key endpoints included correlating [68Ga]Ga-DOTA-FAPI-04 uptake with histological inflammation grades and fibrosis stages, and evaluating its diagnostic and differential efficacy compared to established serum markers and liver stiffness measurement (LSM). Results: [68Ga]Ga-DOTA-FAPI-04 mean uptake in mice livers was notably higher than in control mice, increasing from week 6 [0.70 ± 0.11 percentage injected dose per cubic centimeter (%ID/cc)], peaking at week 10 (0.97 ± 0.15%ID/cc) and slightly reducing at week 12 (0.89 ± 0.28%ID/cc). The hepatic biodistribution and FAP expression showed a consistent trend. In the patient cohort, hepatic [68Ga]Ga-DOTA-FAPI-04 uptake presented moderate correlations with inflammation grades (r = 0.517 to 0.584, all P < 0.05) and fibrosis stages (r = 0.653 to 0.698, all P < 0.01). The average SUVmax to background ratio in the liver showed superior discriminative ability, especially between stage 0 and stage 1, outperforming LSM (area under curve 0.984 vs. 0.865). Conclusion: [68Ga]Ga-DOTA-FAPI-04 PET shows significant potential for non-invasive visualization and dynamic monitoring of liver fibrosis in both preclinical experiment and preliminary clinical trial, especially outperforming other common clinical indicators in the early stage. Trial registration: NCT04605939. Registered October 25, 2020, https://clinicaltrials.gov/study/NCT04605939
      pubtype: Academic Journal
      doctype: Journal Article
      ougenre: Article
    language: English
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