Radiosynthesis and biological evaluation of N -(2-[ 18 F]fluoropropionyl)-3,4-dihydroxy- l -phenylalanine as a PET tracer for oncologic imaging

Tang, Caihua; Nie, Dan; Tang, Ganghua; Gao, Siyuan; Liu, Shaoyu; Wen, Fuhua; Tang, Xiaolan

doi:10.1016/j.nucmedbio.2017.04.002

Cited by 9 publications

(8 citation statements)

References 26 publications

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“…13 Cai et al 4 quoted that apart from FDG, other PET tracers like F-18, Fluoromisonidazole (FMISO) PET, copper-60-diacetylbis (N4-methylthiosemicarbazone; Cu-60 ATSM), and 18F-Fluoroazomycin arabinoside ((18)F-FAZA) PET have application in the non-invasive assessment of hypoxia levels in NSCLC patients. In their study, Tang et al 14 examined radiosynthesis and biological evaluation of 18F-labeled l-DOPA analogue, N- (2-[18F] fluoropropionyl)-3,4-dihydroxy-l-phenylalanine ([18F]FPDOPA) for PET imaging in glioma (C6 gliomabearing mice models), lung adenocarcinoma (SPC-A-1 cell lines), and large cell carcinoma (H460 large cell lung cancer mice models). [18F]FPDOPA had intense accumulation in PET for different heterografts, 8.50 ± 0.40% ID/g in glioma, 6.30 ± 0.12% ID/g in lung adenocarcinoma, and 6.50 ± 0.10% ID/g in large cell lung carcinoma.…”

Section: Resultsmentioning

confidence: 99%

“…Furthermore, there was higher tumor to background ratio of [18F]FPDOPA than [18F]FDG in 1-h post-injection for both SPC-A-1 and H460 heterografts (p < 0.05). 14 In 70 patients with metastatic lymphadenopathy in thoracic CT who were subjected to whole-body PET/CT with 18F-FDG and 18F-FLT (within 1 week for each test), radiopharmaceutical uptake in the lymph node was determined by the calculation of SUV units for both tracers. 15 Then, the results of PET/CT were compared with the histopathological findings of the lymph nodes.…”

Section: Resultsmentioning

confidence: 99%

“…In their study, Tang et al 14 examined radiosynthesis and biological evaluation of 18F-labeled l-DOPA analogue, N -(2-[18F] fluoropropionyl)-3,4-dihydroxy-l-phenylalanine ([18F]FPDOPA) for PET imaging in glioma (C6 glioma-bearing mice models), lung adenocarcinoma (SPC-A-1 cell lines), and large cell carcinoma (H460 large cell lung cancer mice models). [18F]FPDOPA had intense accumulation in PET for different heterografts, 8.50 ± 0.40% ID/g in glioma, 6.30 ± 0.12% ID/g in lung adenocarcinoma, and 6.50 ± 0.10% ID/g in large cell lung carcinoma.…”

Section: Resultsmentioning

confidence: 99%

“…The results from the study of Tang et al 14 were encouraging and showed that 18F-FPDOPA could be useful for several oncological applications in PET imaging. For glioma imaging, 18F-FPDOPA showed better characteristics than 18F-FDG.…”

Section: Discussionmentioning

confidence: 95%

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Modern radiopharmaceuticals for lung cancer imaging with positron emission tomography/computed tomography scan: A systematic review

et al. 2020

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Introduction: In this study, we evaluated the use and the contribution of radiopharmaceuticals to the field of lung neoplasms imaging using positron emission tomography/computed tomography. Methods: We conducted review of the current literature at PubMed/MEDLINE until February 2020. The search language was English. Results: The most widely used radiopharmaceuticals are the following: Experimental/pre-clinical approaches: (18)F-Misonidazole (18F-MISO) under clinical development, D(18)F-Fluoro-Methyl-Tyrosine (18F-FMT), 18F-FAMT (L-[3-18F] (18)F-Fluorothymidine (18F-FLT)), (18)F-Fluoro-Azomycin-Arabinoside (18F-FAZA), (68)Ga-Neomannosylated-Human-Serum-Albumin (68Ga-MSA) (23), (68)Ga-Tetraazacyclododecane (68Ga-DOTA) (as theranostic agent), (11)C-Methionine (11C-MET), 18F-FPDOPA, ανβ3 integrin, 68Ga-RGD2, 64Cu-DOTA-RGD, 18F-Alfatide, Folate Radio tracers, and immuno-positron emission tomography radiopharmaceutical agents. Clinically approved procedures/radiopharmaceuticals agents: (18)F-Fluoro-Deoxy-Glucose (18F-FDG), (18)F-sodium fluoride (18F-NaF) (bone metastases), and (68)Ga-Tetraazacyclododecane (68Ga-DOTA). The quantitative determination and the change in radiopharmaceutical uptake parameters such as standard uptake value, metabolic tumor volume, total lesion glycolysis, FAZA tumor to muscle ratio, standard uptake value tumor to liver ratio, standard uptake value tumor to spleen ratio, standard uptake value maximum ratio, and the degree of hypoxia have prognostic and predictive (concerning the therapeutic outcome) value. They have been associated with the assessment of overall survival and disease free survival. With the positron emission tomography/computed tomography radiopharmaceuticals, the sensitivity and the specificity of the method have increased. Conclusion: In terms of lung cancer, positron emission tomography/computed tomography may have clinical application and utility (a) in personalizing treatment, (b) as a biomarker for the estimation of overall survival, disease free survival, and (c) apply a cost-effective patient approach because it reveals focuses of the disease, which are not found with the other imaging methods.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 95%

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Modern radiopharmaceuticals for lung cancer imaging with positron emission tomography/computed tomography scan: A systematic review

et al. 2020

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“…The method of determining the extent of protein incorporation of [ 18 F]AlF-NOTA-NSC-GLU was previously reported [31]. Brie y, 400 μL(185-296 KBq) [ 18 F]AlF-NOTA-NSC-GLU was added to the Hep3B cells and incubated at 37℃ for 30 min.…”

Section: Incorporation Of [ 18 F]alf-nota-nsc-glu Into Proteinmentioning

confidence: 99%

Biological evaluation of [18F]AlF-NOTA-NSC-GLU as a PET tracer for hepatocellular carcinoma

Lin

Xiang

et al. 2020

Preprint

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Purpose 18F-labeled amino acids (AAs) as tumor-specific imaging agents play a critical role in hepatocellular carcinoma (HCC) imaging. In this work, we evaluated the synthesis and biological properties of a simple 18F-labeled glutamate analogue, [18F]AlF-1,4,7-triazacyclononane-1,4,7-triacetic-acid-2-S-(4-isothiocyanatobenzyl))-l-glutamate ([18F]AlF-NOTA-NSC-GLU) for HCC imaging via one-step reaction sequence. Methods [18F]AlF-NOTA-NSC-GLU was synthesized via the one-step reaction sequence from NOTA-NSC-GLU. In order to investigate the imaging value of [18F]AlF-NOTA-NSC-GLU in HCC, we conducted PET/CT imaging and competitive binding of [18F]AlF-NOTA-NSC-GLU in human Hep3B tumor-bearing mice. The transport mechanism of [18F]AlF-NOTA-NSC-GLU was determined by competitive inhibition and protein incorporation experiments in vitro. Results [18F]AlF-NOTA-NSC-GLU was prepared without decay-corrected radiochemical yield of 29.3 ± 5.6% (n=10) within 20 min. In vitro competitive inhibition experiments demonstrated that Na+-dependent Systems XAG-, B0+, ASC and minor XC- were involved in the uptake of [18F]AlF-NOTA-NSC-GLU, with Na+-dependent System XAG- possibly playing a more dominant role. Protein incorporation studies of the Hep3B human hepatoma cell line found almost no protein incorporation. Micro-PET/CT imaging with [18F]AlF-NOTA-NSC-GLU showed good tumor-to-background contrast in Hep3B human hepatoma-bearing mouse models. After [18F]AlF-NOTA-NSC-GLU injection, the tumor-to-liver uptake ratio of [18F]AlF-NOTA-NSC-GLU was 2.06 ± 0.17 at 30 min post-injection. In vivo competitive binding experiments exhibited that the tumor-to-liver uptake ratio decreased by the addition of the inhibitors to block the system XAG-. Conclusion We have successfully synthesized [18F]AlF-NOTA-NSC-GLU as a novel PET tracer with good radiochemical yield and high radiochemical purity. Our findings indicate that [18F]AlF-NOTA-NSC-GLU might have good clinical potential as a PET tumor-detecting agent for HCC imaging.

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Future Challenges of Multimodality Imaging

López-Mora¹,

Lagos²,

Estorch³

et al. 2020

Recent Results in Cancer Research

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Radiosynthesis and biological evaluation of N -(2-[ 18 F]fluoropropionyl)-3,4-dihydroxy- l -phenylalanine as a PET tracer for oncologic imaging

Cited by 9 publications

References 26 publications

Modern radiopharmaceuticals for lung cancer imaging with positron emission tomography/computed tomography scan: A systematic review

Modern radiopharmaceuticals for lung cancer imaging with positron emission tomography/computed tomography scan: A systematic review

Biological evaluation of [18F]AlF-NOTA-NSC-GLU as a PET tracer for hepatocellular carcinoma

Future Challenges of Multimodality Imaging

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