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        Evaluation of Therapeutic Monitoring of Prostate Cancer (PCa) using [18F]Florastamin, Diagnostic Radiopharmaceutical for PCa: Non-clinical Ex vivo Whole-body Autoradiographic Analysis

        김민환,이경규,길희섭,권순정,이용진,이교철,지대윤 대한방사성의약품학회 2023 Journal of radiopharmaceuticals and molecular prob Vol.9 No.1

        n this study, we evaluated the targeting of prostate cancer (PCa) using [18F]Florastamin in non-clinical study, for the purpose of therapeutic monitoring of [177Lu]Ludotadipep, a therapeutic radiopharmaceutical for PCa, [18F]Florastamin/[177Lu]Ludotadipep was co-administered to a single-individual prostate tumor bearing mouse model, mimicking clinical condition. Considering the difference in half-life of the two isotopes (18F or 177Lu), image scan of whole-body autoradiography was performed at 24 or 48 h after preparation of frozen section, respectively. Then, it was confirmed whether they showed the same targeting efficiency for the area of tumor. A tumor xenograft model was prepared using PSMA-overexpressing PC3-PIP prostate cancer cells. [18F]Florastamin [111 MBq (3 mCi) in 100 µL]/[177Lu]Ludotadipep [3.7 MBq (100 μCi) in 100 μL] was co-administered through the tail vein, and 2 hours after administration, the mice were frozen, and after freezing for 24 hours, whole-body cryosection was performed at 24 h after freezing. Image scanning using cryosection was performed after 24 or 48 hours after freezing, respectively. In the scan image after 24 hours, tumor uptake of [ 18F] Florastamin/[177Lu]Ludotadipep were simultaneously observed specific uptake in the tumor. In the scan image after 48 hours in the same section, signal of 18F was lost by decay of radioisotope, and specific uptake image for [177Lu]Ludotadipep was observed in the tumor. Uptake of [177Lu]Ludotadipep was specific to the same tumor region where [18F]Florastamin/[177Lu]Ludotadipep was uptake. These results suggested that [18F]Florastamin showed the same tumor uptake efficiency to PCa as [177Lu]Ludotadipep, and effective therapeutic monitoring is expected to be enable using [18F]Florastamin during [177Lu]Ludotadipep therapy for PCa.

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        The Development of Radiopharmaceutical Synthesizer and its FDG Synthesis Verification

        김종민,정일구,박찬수,길희섭,이철수 대한방사성의약품학회 2022 Journal of radiopharmaceuticals and molecular prob Vol.8 No.2

        [18F]FDG is known as the most widely used radiopharmaceutical in the imaging field of nuclear medicine worldwide. With the introduction of PET equipment, the demand for [18F]FDG has increased and the production volume has also increased. However, in order to increase production, the use of 18F radioisotope must be increased or [18F]FDG must be synthesized in high yield. Therefore, in order to meet the high yield and purity of radiopharmaceuticals, a radiopharmaceutical automatic synthesizer was required. As the use of [18F]FDG increased, automated synthesizer manufacturers supplied various types of radiopharmaceutical automated synthesizers to the market. In this study, we developed a commercialized [18F]FDG radiopharmaceutical automatic synthesizer (sCUBE FDG) using a disposable cassette type that complies with GMP developed by FutureChem, a leading radiopharmaceutical company. We used sCUBE FDG to verify the production process, radiopharmaceutical’s quality (radiochemical purity, etc.), and radiochemical yield of [18F]FDG. As a result of optimizing the automatic synthesis process and synthesizing a total of 30 times, the production time was 35 ± 3 minutes and the average production yield was 65.6%.

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        Clinical Usefulness of 18F-FC119S Positron-Emission Tomography as an Auxiliary Diagnostic Method for Dementia: An Open-Label, Single-Dose, Evaluator-Blind Clinical Trial

        이인기,나해리,변병현,임일한,김병일,최창운,고인옥,이교철,김경민,박수연,김유경,이준영,부선희,김정화,길희섭,박찬수,지대윤,하정호,임상무 대한신경과학회 2020 Journal of Clinical Neurology Vol.16 No.1

        Background and Purpose The aim of this study was to determine the diagnostic performance and safety of a new 18F-labeled amyloid tracer, 18F-FC119S. Methods This study prospectively recruited 105 participants, comprising 53 with Alzheimer’s disease (AD) patients, 16 patients with dementia other than AD (non-AD), and 36 healthy controls (HCs). In the first screening visit, the Seoul Neuropsychological Screening Battery cognitive function test was given to the dementia group, while HC subjects completed the Korean version of the Mini Mental State Examination. Individuals underwent 18F-FC119S PET, 18F-fluorodeoxyglucose (FDG) PET, and brain MRI. The diagnostic performance of 18F-FC119S PET for AD was compared to a historical control (comprising previously reported and currently used amyloid-beta PET agents), 18F-FDG PET, and MRI. The standardized uptake value (SUV) ratio (ratio of the cerebral cortical SUV to the cerebellar SUV) was measured for each PET data set to provide semiquantitative analysis. All adverse effects during the clinical trial periods were monitored. Results Visual assessments of the 18F-FC119S PET data revealed a sensitivity of 92% and a specificity of 84% in detecting AD. 18F-FC119S PET demonstrated equivalent or better diagnostic performance for AD detection than the historical control, 18F-FDG PET (sensitivity of 80.0% and specificity of 76.0%), and MRI (sensitivity of 98.0% and specificity of 50.0%). The SUV ratios differed significantly between AD patients and the other groups, at 1.44±0.17 (mean±SD) for AD, 1.24±0.09 for non-AD, and 1.21±0.08 for HC. No clinically significant adverse effects occurred during the trial periods. Conclusions 18F-FC119S PET provides high sensitivity and specificity in detecting AD and therefore may be considered a useful diagnostic tool for AD.

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