Improved synthesis of anti-[18F]FACBC: improved preparation of labeling precursor and automated radiosynthesis

McConathy, Jonathan; Voll, Ronald J.; Yu, Winston; Crowe, Ronald J.; Goodman, Mark M.

doi:10.1016/s0969-8043(03)00029-0

Cited by 75 publications

(78 citation statements)

References 12 publications

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“…F-FACBC has been previously reported ( 20 ). The decay-corrected radiochemical yield of the desired product was 24%, and its radiochemical purity was 99% 80 minutes after the end of bombardment.…”

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confidence: 76%

Detection of Recurrent Prostate Carcinoma withanti-1-Amino-3-¹⁸F-Fluorocyclobutane-1-Carboxylic Acid PET/CT and¹¹¹In–Capromab Pendetide SPECT/CT

Schuster

Savir-Baruch²,

Nieh³

et al. 2011

Radiology

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Purpose:To compare the diagnostic performance of the synthetic amino acid analog radiotracer anti -1-amino-3-fl uorine 18-fl uorocyclobutane-1-carboxylic acid ( anti -3-18 F-FACBC) with that of indium 111 ( 111 In)-capromab pendetide in the detection of recurrent prostate carcinoma. Materials andMethods:This prospective study was approved by the institutional review board and complied with HIPAA guidelines. Written informed consent was obtained. In-capromab pendetide single photon emission computed tomography (SPECT)/CT were performed within 6 weeks of each other. Studies were evaluated by two experienced interpreters for abnormal uptake suspicious for recurrent disease in the prostate bed and extraprostatic locations. The reference standard was a combination of tissue correlation , imaging, laboratory, and clinical data. Diagnostic performance measures were calculated and tests of the statistical signifi cance of differences determined by using the McNemar x 2 test as well as approximate tests based on the difference between two proportions. Results:For disease detection in the prostate bed, anti -3-18 F-FACBC had a sensitivity of 89 % (32 of 36 patients; 95% confi dence interval [CI]: 74%, 97%), specifi city of 67% (eight of 12 patients; 95% CI: 35%, 90%), and accuracy of 83% (40 of 48 patients; 95% CI: 70%, 93%).111 In-capromab pendetide had a sensitivity of 69% (25 of 36 patients; 95% CI: 52%, 84%), specifi city of 58% (seven of 12 patients; 95% CI: 28%, 85%), and accuracy of 67% (32 of 48 patients; 95% CI: 52%, 80%). In the detection of extraprostatic recurrence, anti -3-18 F-FACBC had a sensitivity of 100% (10 of 10 patients; 95% CI: 69%, 100%), specifi city of 100% (seven of seven patients; 95% CI: 59%, 100%), and accuracy of 100% (17 of 17 patients; 95% CI: 80%, 100%).111 In-capromab pendetide had a sensitivity of 10% (one of 10 patients; 95% CI: 0%, 45%), specifi city of 100% (seven of seven patients; 95% CI: 59%, 100%), and accuracy of 47% (eight of 17 patients; 95% CI: 23%, 72%). Conclusion:anti -3-18 F-FACBC PET/CT was more sensitive than 111 Incapromab pendetide SPECT/CT in the detection of recurrent prostate carcinoma and is highly accurate in the differentiation of prostatic from extraprostatic disease.

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confidence: 76%

Detection of Recurrent Prostate Carcinoma withanti-1-Amino-3-¹⁸F-Fluorocyclobutane-1-Carboxylic Acid PET/CT and¹¹¹In–Capromab Pendetide SPECT/CT

Schuster

Savir-Baruch²,

Nieh³

et al. 2011

Radiology

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130

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“…The 18 F-fluciclovine is produced under Investigational New Drug Application 72,437 via the FastLab Cassette System (GE Healthcare) or automated synthesis (21). The patients are imaged on a Discovery MV690 PET/CT scanner (GE Healthcare) after fasting for at least 4 h to normalize amino acid levels.…”

Section: F-fluciclovine Production and Imagingmentioning

confidence: 99%

“…The investigational classes of radiotracers include fatty acid analogs (acetate), cell membrane analogs (choline), amino acid analogs (fluciclovine), and newer-generation prostate-specific membrane antigen ligands (16)(17)(18)(19)(20)(21). In this context, 18 F-fluciclovine (anti-1-amino-3-18 F-fluorocyclobutane-1-carboxylic acid), which is transported in a manner similar to glutamine, has shown promising imaging characteristics for the detection of prostate cancer recurrence.…”

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confidence: 99%

Impact of ¹⁸F-Fluciclovine PET on Target Volume Definition for Postprostatectomy Salvage Radiotherapy: Initial Findings from a Randomized Trial

et al. 2016

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“…The preparation of anti-[ 18 F]FACBC has been previously reported [32]. One hour after tail vein injections of 150 μCi [ 18 F]FACBC in a volume of 150 μl, the animals were anesthetized and secured on an extended scanning bed before being moved into the interior of the Inveon Preclinical CT scanner (Siemens Medical Solutions Inc, Malvern, PA).…”

Section: Preparation Of Anti-[ 18 F]facbc and Micropet Imagingmentioning

confidence: 99%

Potential Biomarker of L-type Amino Acid Transporter 1 in Breast Cancer Progression

Liang

Cho

Williams

et al. 2010

Nucl Med Mol Imaging

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Purpose L-type amino acid transporter 1 (LAT1) is essential for the transport of large neutral amino acids. However, its role in breast cancer growth remains largely unknown. The purpose of the study is to investigate whether LAT1 is a potential biomarker for the diagnosis and treatment of breast cancer. Methods LAT1 mRNA and protein levels in breast cancer cell lines and tissues were analyzed. In addition, the effects of targeting LAT1 for the inhibition of breast cancer cell tumorigenesis were assessed with soft agar assay. The imaging of xenograft with anti-1-amino-3-[ 18 F]fluorocyclobutane-1-carboxylic acid (anti-[ 18 F]FACBC) PET was assessed for its diagnostic biomarker potential. Results Normal breast tissue or low malignant cell lines expressed low levels of LAT1 mRNA and protein, while highly malignant cancer cell lines and high-grade breast cancer tissue expressed high levels of LAT1. In addition, higher expression levels of LAT1 in breast cancer tissues were consistent with advanced-stage breast cancer. Furthermore, the blockade of LAT1 with its inhibitor, 2-aminobicyclo[2.2.1]heptane-2-carboxylic acid (BCH), or the knockdown of LAT1 with siRNA, inhibited proliferation and tumorigenesis of breast cancer cells. A leucine analog, anti-[ 18 F]FACBC, has been demonstrated to be an excellent PET tracer for the non-invasive imaging of malignant breast cancer using an orthotopic animal model. Conclusions The overexpression of LAT1 is required for the progression of breast cancer. LAT1 represents a potential biomarker for therapy and diagnosis of breast cancer. Anti-[ 18 F]FACBC that correlates with LAT1 function is a potential PET tracer for malignant breast tumor imaging.

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Improved synthesis of anti-[18F]FACBC: improved preparation of labeling precursor and automated radiosynthesis

Cited by 75 publications

References 12 publications

Detection of Recurrent Prostate Carcinoma withanti-1-Amino-3-¹⁸F-Fluorocyclobutane-1-Carboxylic Acid PET/CT and¹¹¹In–Capromab Pendetide SPECT/CT

Detection of Recurrent Prostate Carcinoma withanti-1-Amino-3-¹⁸F-Fluorocyclobutane-1-Carboxylic Acid PET/CT and¹¹¹In–Capromab Pendetide SPECT/CT

Impact of ¹⁸F-Fluciclovine PET on Target Volume Definition for Postprostatectomy Salvage Radiotherapy: Initial Findings from a Randomized Trial

Potential Biomarker of L-type Amino Acid Transporter 1 in Breast Cancer Progression

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Improved synthesis of anti-[18F]FACBC: improved preparation of labeling precursor and automated radiosynthesis

Cited by 75 publications

References 12 publications

Detection of Recurrent Prostate Carcinoma withanti-1-Amino-3-18F-Fluorocyclobutane-1-Carboxylic Acid PET/CT and111In–Capromab Pendetide SPECT/CT

Detection of Recurrent Prostate Carcinoma withanti-1-Amino-3-18F-Fluorocyclobutane-1-Carboxylic Acid PET/CT and111In–Capromab Pendetide SPECT/CT

Impact of 18F-Fluciclovine PET on Target Volume Definition for Postprostatectomy Salvage Radiotherapy: Initial Findings from a Randomized Trial

Potential Biomarker of L-type Amino Acid Transporter 1 in Breast Cancer Progression

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Product

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Detection of Recurrent Prostate Carcinoma withanti-1-Amino-3-¹⁸F-Fluorocyclobutane-1-Carboxylic Acid PET/CT and¹¹¹In–Capromab Pendetide SPECT/CT

Detection of Recurrent Prostate Carcinoma withanti-1-Amino-3-¹⁸F-Fluorocyclobutane-1-Carboxylic Acid PET/CT and¹¹¹In–Capromab Pendetide SPECT/CT

Impact of ¹⁸F-Fluciclovine PET on Target Volume Definition for Postprostatectomy Salvage Radiotherapy: Initial Findings from a Randomized Trial