PO-1777 68Ga-fibroblast activation protein inhibitor PET/CT on GTV delineation of oesophageal cancer

2021 ◽  
Vol 161 ◽  
pp. S1503-S1504
Author(s):  
L. Zhao ◽  
H. Chen ◽  
Q. Lin
Keyword(s):  
Oesophageal Cancer ◽  
Fibroblast Activation Protein ◽  
Protein Inhibitor ◽  
Fibroblast Activation ◽  
Pet Ct

Fibroblast Activation Protein Inhibitor PET/CT

2020 ◽  
Vol Publish Ahead of Print ◽  
Author(s):  
Punit Sharma ◽  
Shashank Shekhar Singh ◽  
Shankaramurthy Gayana
Keyword(s):  
Fibroblast Activation Protein ◽  
Protein Inhibitor ◽  
Fibroblast Activation ◽  
Pet Ct

scholarly journals Clinical Translational Evaluation of Al18F-NOTA-FAPI for Fibroblast Activation Protein Targeted Tumour Imaging

2021 ◽  
Author(s):  
Shuailiang Wang ◽  
Xin Zhou ◽  
Xiaoxia Xu ◽  
Jin Ding ◽  
Song Liu ◽  
...  
Keyword(s):  
Cancer Patients ◽  
Fibroblast Activation Protein ◽  
Ct Imaging ◽  
Whole Body ◽  
Tumour Imaging ◽  
Tumour Detection ◽  
Fibroblast Activation ◽  
Tumour Bearing ◽  
Pet Ct ◽  
18F Fdg

Abstract PurposeIn this study, a novel Al18F-NOTA-FAPI probe was developed for fibroblast activation protein (FAP) targeted tumour imaging, which was available to achieve curie level radioactivity by automatic synthesizer. The tumour detection efficacy of Al18F-NOTA-FAPI was further validated both in preclinical and clinical translational studies. MethodsThe radiolabeling procedure of Al18F-NOTA-FAPI was optimized. Cell uptake and competitive binding assay were completed with U87MG and A549 cell lines, to evaluate the affinity and specificity of Al18F-NOTA-FAPI probe. The biodistribution, pharmacokinetics, radiation dosimetry and tumour imaging efficacy of Al18F-NOTA-FAPI probe were researched with healthy Kunming (KM) and/or U87MG model mice. After the approval of ethical committee, Al18F-NOTA-FAPI probe was translated into clinical for the PET/CT imaging of first 10 cancer patients. ResultsThe radiolabeling yield of Al18F-NOTA-FAPI was 33.8 ± 3.2% through manually operation (n = 10), with the radiochemical purity over than 99% and the specific activity of 9.3-55.5 MBq/nmol. Whole body effective dose of Al18F-NOTA-FAPI was estimated to be 1.24E-02 mSv/MBq, lower than several other FAPI probes ( 68Ga-FAPI-04, 68Ga-FAPI-46 and 68Ga-FAPI-74). In U87MG tumour bearing mice, Al18F-NOTA-FAPI showed good tumor detection efficacy from the results of micro PET/CT imaging and biodistribution studies. In organ biodistribution study of human patients, Al18F-NOTA-FAPI showed lower SUVmean than 2-[18F]FDG in most organs, especially in liver (1.1 ± 0.2 vs. 2.0 ± 0.9), brain (0.1 ± 0.0 vs. 5.9 ± 1.3), and bone marrow (0.9 ± 0.1 vs. 1.7 ± 0.4). Meanwhile, Al18F-NOTA-FAPI do not show extensive bone uptakes, and was able to find out more tumour lesions than 2-[18F]FDG in the PET/CT imaging of several patients. ConclusionAl18F-NOTA-FAPI probe was successfully fabricated and applied in fibroblast activation protein targeted tumour PET/CT imaging, which showed excellent imaging quality and tumour detection efficacy in U87MG tumour bearing mice as well as in human cancer patients.

scholarly journals Fibroblast-Activated Protein Inhibitor PET/CT: Cancer Diagnosis and Management

2021 ◽  
Vol 11 ◽  
Author(s):  
Serkan Kuyumcu ◽  
Yasemin Sanli ◽  
Rathan M. Subramaniam
Keyword(s):  
Fibroblast Activation Protein ◽  
Radiotherapy Planning ◽  
Cancer Associated Fibroblasts ◽  
Protein Inhibitor ◽  
Clinical Role ◽  
Pet Ct ◽  
Cancer Types ◽  
Novel Target ◽  
Low Sensitivity ◽  
Theranostic Applications

Fibroblast activation protein (FAP), overexpressed on cancer-associated fibroblasts (CAFs), is a novel target for molecular imaging of various tumors. Recently, the development of several small-molecule FAP inhibitors for radiolabeling with 68Ga has resulted in the emergence of studies evaluating its clinical role in cancer imaging. Preliminary findings have demonstrated that, in contrast to radiotracers taking advantage of cancer-specific targets such as PSMA and DOTATATE, FAPs as a target are the most promising that can compete with 18FDG in terms of widespread indications. They also have the potential to overcome the shortcomings of 18FDG, particularly false-positive uptake due to inflammatory or infectious processes, low sensitivity in certain cancer types, and radiotherapy planning. In addition, the attractive theranostic properties may facilitate the treatment of many refractory cancers. This review summarizes the current FAP variants and related clinical studies, focusing on radiopharmacy, dosimetry, and diagnostic and theranostic applications.

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