Preclinical evaluation and pilot clinical study of [18F]AlF-NOTA-FAPI-04 for PET imaging of rheumatoid arthritis

Ge, Liangpeng; Fu, Zheng; Ye, Wei; Shi, Dandan; Geng, Yun; Fan, Huancai; Zhang, Ruojia; Zhang, Yuang; Li, Shufeng; Wang, Shijie; Shi, Huancong; Song, Guanhua; Pan, Jihong; Chen, Kai; Wang, Lin

doi:10.1007/s00259-022-05836-3

Cited by 24 publications

(14 citation statements)

References 33 publications

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“…Some articles focused particularly on the role of FAPI imaging for the assessment of RA in preclinical setting, with the demonstration of the high specificity of this tracer for arthritic joints, both in vitro and in vivo. In this setting, some pilot clinical evaluations for the use of radiolabeled FAPI PET/CT in subjects with RA have also been proposed, suggesting its potential application to visualize arthritic synovium related to the specific upregulation of the expression of FAP in this site [ 10 , 30 , 31 ].…”

mentioning

confidence: 99%

Emerging Role of FAPI PET Imaging for the Assessment of Benign Bone and Joint Diseases

Dondi

Albano

Treglia

et al. 2022

JCM

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mentioning

confidence: 99%

Emerging Role of FAPI PET Imaging for the Assessment of Benign Bone and Joint Diseases

Dondi

Albano

Treglia

et al. 2022

JCM

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“…Since [ 68 Ga]FAPI04 is metabolized by the kidney, the tumor-to-kidney ratio of [ 18 F]1a , b is greater than that of [ 68 Ga]FAPI04, which is expected to diagnose kidney-related diseases (Figure e). Consistent with the high expression of FAP in joints, [ 18 F]1a exhibited high uptake in joints (knees and shoulders), with uptake values of 1.42 ± 0.16, 1.48 ± 0.13% ID/g at 30 min post injection, respectively(Figure a). However, [ 18 F]1b did not show a significant bone joint uptake.…”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis, and Evaluation of ¹⁸F-Labeled Tracers Targeting Fibroblast Activation Protein for Brain Imaging

Yu,

Huang,

Chen

et al. 2023

ACS Pharmacol. Transl. Sci.

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Fibroblast activation protein (FAP) is closely related to central nervous system diseases such as stroke and brain tumors, but PET tracers that can be used for brain imaging have not been reported. Here, we designed, synthesized, and evaluated 18F-labeled UAMC1110 derivatives suitable for brain imaging targeting FAP. By substituting the F atom for the H atom on the aromatic ring of compound UAMC1110, 1a–c were designed and prepared. 1a–c were confirmed to have a high affinity for FAP through molecular docking and enzyme assay. [ 18 F]1a–c were successfully prepared and confirmed to have high affinity. The stability in vivo indicates that no obvious metabolites of [ 18 F]1a,b were found in the plasma 1 h after injection, which is beneficial for brain imaging. In vitro cell uptake experiments showed that [ 18 F]1a,b and [68Ga]FAPI04 exhibited similar uptake and internalization rates. PET imaging of U87MG subcutaneous tumor showed that [ 18 F]1a,b could penetrate the blood–brain barrier with higher uptake and longer retention time than [68Ga]FAPI04 (uptake at 62.5 min, 1.06 ± 0.23, 1.09 ± 0.25% ID/g vs 0.21 ± 0.10% ID/g, respectively). The brain-to-blood ratios of [ 18 F]1a,b were better than [68Ga]FAPI04. Biodistribution and PET imaging showed that [ 18 F]1a had better uptake on tumors and a higher tumor-to-muscle ratio than [ 18 F]1b and [68Ga]FAPI04. Further imaging of U87MG intracranial glioma showed that [ 18 F]1a outlined high-contrast gliomas in a short period of time compared to [ 18 F]1b. Therefore, [ 18 F]1a is expected to be useful in the diagnosis of FAP-related brain diseases.

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“…Studies have shown that the uptake values of nucleotide-labeled FAP antibodies or inhibitors correlate positively with the severity of arthritis. 32,33 To improve the reliability of the data obtained by the students, we optimized the experimental protocol by using mice with a more severe degree of joint pathogenesis, which would result in a more targeted distribution of 18 F-FAPi. Previous studies have demonstrated that 18 F-labeled FAP rapidly reaches equilibrium in the blood and that the concentration in the blood returns to a low value within a few minutes.…”

Section: Discussionmentioning

confidence: 99%

“…Because it has been shown that FAP expression is significantly elevated in diseased joints in the CIA model, 32 PET imaging can capture significantly increased uptake of 18 F‐FAPi in the inflamed joints. Studies have shown that the uptake values of nucleotide‐labeled FAP antibodies or inhibitors correlate positively with the severity of arthritis 32,33 . To improve the reliability of the data obtained by the students, we optimized the experimental protocol by using mice with a more severe degree of joint pathogenesis, which would result in a more targeted distribution of 18 F‐FAPi.…”

Section: Discussionmentioning

confidence: 99%

PET imaging to assess fibroblast activation protein inhibitor biodistribution: A training program adapted to pharmacology education

Song

Zhang

et al. 2022

Pharmacology Res & Perspec

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In the process of pharmacology education, practical teaching is an important complement to theoretical teaching. These activities include the use of experimental animals to obtain certain pharmacological parameters or to help students understand certain classical concepts. However, the growing interest in laboratory animal welfare, the rapid development of pharmacology research and the challenges of cultivating innovative pharmacy talent create a need for innovative and flexible in vitro experiments for teaching purposes. Here, we report the application of positron emission tomography (PET) imaging of 18 F‐labeled fibroblast activation protein inhibitor ( 18 F‐FAPi) to practical pharmacology teaching, enabling dynamic visualization of the distribution and excretion process of FAPi in mice. Students can quantitatively analyze the distribution of FAPi in various tissues and organs without sacrificing the mice. Furthermore, the newly implemented method resulted in highly reproducible results and was generally appreciated by the students. Additionally, the application of PET imaging in pharmacokinetic teaching can not only greatly reduce the use of experimental animals but also need not sacrificing animals. Of note is that dynamic scanning data from this project can be used for online practical teaching during COVID‐19 pandemic.

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Preclinical evaluation and pilot clinical study of [18F]AlF-NOTA-FAPI-04 for PET imaging of rheumatoid arthritis

Cited by 24 publications

References 33 publications

Emerging Role of FAPI PET Imaging for the Assessment of Benign Bone and Joint Diseases

Emerging Role of FAPI PET Imaging for the Assessment of Benign Bone and Joint Diseases

Design, Synthesis, and Evaluation of ¹⁸F-Labeled Tracers Targeting Fibroblast Activation Protein for Brain Imaging

PET imaging to assess fibroblast activation protein inhibitor biodistribution: A training program adapted to pharmacology education

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Preclinical evaluation and pilot clinical study of [18F]AlF-NOTA-FAPI-04 for PET imaging of rheumatoid arthritis

Cited by 24 publications

References 33 publications

Emerging Role of FAPI PET Imaging for the Assessment of Benign Bone and Joint Diseases

Emerging Role of FAPI PET Imaging for the Assessment of Benign Bone and Joint Diseases

Design, Synthesis, and Evaluation of 18F-Labeled Tracers Targeting Fibroblast Activation Protein for Brain Imaging

PET imaging to assess fibroblast activation protein inhibitor biodistribution: A training program adapted to pharmacology education

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Design, Synthesis, and Evaluation of ¹⁸F-Labeled Tracers Targeting Fibroblast Activation Protein for Brain Imaging