Biodistribution of the 18F-FPPRGD2 PET radiopharmaceutical in cancer patients: an atlas of SUV measurements

Minamimoto, Ryogo; Jamali, Mehran; Barkhodari, Amir; Mosci, Camila; Mittra, Erik; Shen, Bin; Chin, Frederick T.; Gambhir, Sanjiv S.; Iagaru, Andrei

doi:10.1007/s00259-015-3096-4

Cited by 41 publications

(29 citation statements)

References 48 publications

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“…46 Other manual approaches for radiolabeling various cRGDpeptides with uorine-18 have provided yields between 10-35% with total reaction times ranging between 90-218 minutes. [50][51][52][53][54][55] The yield obtained for cRGDyK([ 18 F]FPy) was also similar to the previously reported manual solid phase radiolabeling of cRGDyK with 6-[ 18 F]uorobenzoic acid (14 AE 2% yield in 90 minutes). 42 Overall, using the ELIXYS FLEX/CHEM® radiosynthesizer was faster, with a total synthesis time under a 100 minutes including HPLC purication, and provided similar radiochemical yields.…”

Section: Discussionsupporting

confidence: 86%

Fully automated peptide radiolabeling from [¹⁸F]fluoride

et al. 2019

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The biological properties of receptor-targeted peptides have made them popular diagnostic imaging and therapeutic agents. Typically, the synthesis of fluorine-18 radiolabeled receptor-targeted peptides for positron emission tomography (PET) imaging is a time consuming, complex, multi-step synthetic process that is highly variable based on the peptide. The complexity associated with the radiolabeling route and lack of robust automated protocols can hinder translation into the clinic. A fully automated batch production to radiolabel three peptides (YGGFL, cRGDyK, and Pyr-QKLGNQWAVGHLM) from fluorine-18 using the ELIXYS FLEX/CHEM® radiosynthesizer in a two-step process is described. First, the prosthetic group, 6-[ 18 F]fluoronicotinyl-2,3,5,6-tetrafluorophenyl ester ([ 18 F]FPy-TFP) was synthesized and subsequently attached to the peptide. The [ 18 F]FPy-peptides were synthesized in 13-26% decay corrected yields from fluorine-18 with high molar activity 1-5 Ci mmol À1 and radiochemical purity of >99% in an overall synthesis time of 97 AE 3 minutes.

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Section: Discussionsupporting

confidence: 86%

Fully automated peptide radiolabeling from [¹⁸F]fluoride

et al. 2019

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“…[ 18 F]Galacto‐RGD, radiolabeled by an indirect approach using 4‐nitrophenyl‐2‐[ 18 F]fluoropropionate, was the first fluorine‐18 labeled PET tracer of this class tested clinically . There are other conventional C‐ 18 F bond containing RGD‐based tracers . These tracers are prepared in multistep syntheses with several HPLC purifications, thus requiring a long synthesis time.…”

Section: Resultsmentioning

confidence: 99%

Fast indirect fluorine-18 labeling of protein/peptide using the useful 6-fluoronicotinic acid-2,3,5,6-tetrafluorophenyl prosthetic group: A method comparable to direct fluorination

Basuli

Zhang

Woodroofe

et al. 2017

J. Label Compd. Radiopharm

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Fluorine-18 labeling of biomolecules are mostly performed by an indirect labeling method using a prosthetic group. Fluorine-18 labeled 6-fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester is a useful prosthetic group to radiolabel a protein. Recently we reported an improved preparation of this prosthetic group. To test the conjugation efficiency of the labeled ester prepared by this method we have performed conjugation reactions with two different peptides and a protein. Prostate-specific membrane antigen (PSMA) targeting peptide [18F]DCFPyL, αvβ3 integrin receptors targeting peptide [18F]c(RGDfK) and [18F]albumin were prepared in good radiochemical yields. The conjugation reactions were completed at 40 - 50 °C in 10 min. The overall radiochemical yield was 25-43 % in 30-45 min.

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“…There have been a few studies using RGD-based PET probes such as 18 F-galacto-RGD, 18 F-AH111585, 18 F-FPPRGD2, and 68 Ga-PRGD2 in the clinic for breast cancer patients (19)(20)(21)(22)(23)(24). Generally, these PET tracers have shown satisfactory performance in terms of safety, feasibility, and usefulness.…”

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confidence: 99%

¹⁸F-Alfatide II PET/CT for Identification of Breast Cancer: A Preliminary Clinical Study

Wang

Zhang

et al. 2018

J Nucl Med

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F-alfatide II has been proven to have excellent clinical translational potential. In this study, we investigated F-alfatide II for identifying breast cancer and compared the performances betweenF-alfatide II and F-FDG. Forty-four female patients with suspected primary breast cancer were recruited. PET/CT images using F-alfatide II andF-FDG were acquired within 7 d. Tracer uptake in breast lesions was evaluated by visual analysis, and semiquantitative analysis with SUV and SUV Forty-two breast cancer lesions and 11 benign breast lesions were confirmed by histopathology in 44 patients. BothF-alfatide II and F-FDG had higher uptake in breast cancer lesions than in benign breast lesions ( < 0.05 for F-alfatide II, < 0.05 for F-FDG). The area under the curve ofF-alfatide II was slightly less than that of F-FDG. BothF-alfatide II and F-FDG had high sensitivity (88.1% vs. 90.5%), high positive predictive value (88.1% vs. 88.4%), moderate specificity (54.5% vs. 54.5%), and moderate negative predictive value (54.5% vs. 60.0%) for differentiating breast cancer from benign breast lesions. By combiningF-alfatide II and F-FDG, the sensitivity and negative predictive value significantly increased to 97.6% and 85.7%, respectively, with positive predictive value slightly increased to 89.1% and no change to the specificity (54.5%). The uptake ofF-alfatide II (SUV: 3.77 ± 1.78) was significantly lower than that of F-FDG (SUV: 7.37 ± 4.48) in breast cancer lesions ( < 0.05). F-alfatide II uptake in triple-negative subtype was significantly lower than that in luminal A and luminal B subtypes. By contrast, human epidermal growth factor receptor-2 (HER-2)-overexpressing subtype had higherF-FDG uptake than the other 3 subtypes. There were 8 breast cancer lesions with higher F-alfatide II uptake thanF-FDG uptake, which all had a common characteristic that HER-2 expression was negative and estrogen receptor expression was strongly positive. F-alfatide II is suitable for clinical use in breast cancer patients.F-alfatide II is of good performance, but not superior to F-FDG in identifying breast cancer.F-alfatide II may have superiority to F-FDG in detecting breast cancer with strongly positive estrogen receptor expression and negative HER-2 expression.

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Biodistribution of the 18F-FPPRGD2 PET radiopharmaceutical in cancer patients: an atlas of SUV measurements

Abstract: The biodistribution of (18)F-FPPRGD2 in cancer patients is similar to that of other RGD dimer peptides and it is suitable for clinical use. The lack of significant correlation between (18)F-FPPRGD2 and (18)F-FDG uptake confirms that the information provided by each PET tracer is different.

Cited by 41 publications

References 48 publications

Fully automated peptide radiolabeling from [¹⁸F]fluoride

Fully automated peptide radiolabeling from [¹⁸F]fluoride

Fast indirect fluorine-18 labeling of protein/peptide using the useful 6-fluoronicotinic acid-2,3,5,6-tetrafluorophenyl prosthetic group: A method comparable to direct fluorination

¹⁸F-Alfatide II PET/CT for Identification of Breast Cancer: A Preliminary Clinical Study

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Biodistribution of the 18F-FPPRGD2 PET radiopharmaceutical in cancer patients: an atlas of SUV measurements

Cited by 41 publications

References 48 publications

Fully automated peptide radiolabeling from [18F]fluoride

Fully automated peptide radiolabeling from [18F]fluoride

Fast indirect fluorine-18 labeling of protein/peptide using the useful 6-fluoronicotinic acid-2,3,5,6-tetrafluorophenyl prosthetic group: A method comparable to direct fluorination

18F-Alfatide II PET/CT for Identification of Breast Cancer: A Preliminary Clinical Study

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Product

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Fully automated peptide radiolabeling from [¹⁸F]fluoride

Fully automated peptide radiolabeling from [¹⁸F]fluoride

¹⁸F-Alfatide II PET/CT for Identification of Breast Cancer: A Preliminary Clinical Study