• Journal of Radiopharmaceuticals and Molecular Probes
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• v.4 no.2
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• pp.99-105
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• 2018

$^{211}At$ is an alpha emitting radionuclide, which can be produced using cyclotron with alpha beam. In addition, its strong linear energy transfer and iodine-like chemistry make that $^{211}At$ is one of the most attractive radionuclide in the field of targeted alpha therapy. In this review, production, labeling, and radiopharmaceuticals of $^{211}At$ will be discussed.

• Journal of the Korean Society of Radiology
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• v.16 no.7
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• pp.1007-1014
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• 2022

Targeted radionuclide therapy (TRT) is a method of treating tumor cells using radiopharmaceuticals. Cells and nuclei constituting tissues of the human body are composed of spherical and oval shapes, but cancer cells are composed of various cell types. Therefore, this study analyzed the absorbed dose for each organelle according to the change in the size of the cell nucleus for beta-emitting nuclides during targeted radionuclide therapy through the Monte Carlo method. Cells were set in two sphere shapes, 5 ㎛ and 10 ㎛, and the internal structure was divided into cell nucleus, cytoplasm, and cell surface. Next, the absorbed dose according to the increase in the size of the cell nucleus was evaluated. As a result, ¹⁷⁷Lu among the target radionuclides showed the highest dose in all cell compartments. As the ratio of the nucleus in the cell increased, the absorbed dose on the cell surface increased, but the absorbed dose in the cytoplasm and nucleus tended to decrease. Accordingly, it is judged that it is important to select a radionuclide considering the size of cancer cells and determine an appropriate amount of radioactivity during targeted radionuclide treatment.

• Nuclear Medicine and Molecular Imaging
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• v.40 no.2
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• pp.90-95
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• 2006

Neuroendocrine tumors (NETs) consist of a heterogeneous group of tumors that are able to uptake neuroamine and/or specific receptors, such as somatostatin receptors, which can play important roles of the localization and treatment of these tumors. When considering therapy with radionuclides, the best radioligand should be carefully investigated. $^{131}I$-MIBG and beta-particle emitter labeled somatostatin analogs are well established radionuclide therapy modalities for NETs. $^{111}In,\;^{90}Y\;and\;^{177}Lu$ radiolabeled somatostatin analogues have been used for treatment of NETs. Further, radionuclide therapy modalities, for example, radioimmunotherapy, radiolabeled peptides such as minigastrin are currently under development and in different phases of clinical investigation. for all radionuclides used for therapy, long-term and survival statistics are not yet available and only partial tumour responses have been obtained using $^{131}I$-MIBG and $^{111}In$-octreotide. Experimental results using $^{90}Y$-DOTA-lanreotide as well as $^{90}Y-DOTA-D-Phe1-Tyr^3-octreotide$ and/or $^{177}Lu-DOTA-Tyr^3-octreotate$ have indicated the possible clinical potential of radionuclides receptor-targeted radiotherapy it may be hoped that the efficacy of radionuclide therapy will be improved by co-administration of chemotherapeutic drugs whose antitumoral properties may be synergistic with that of irradiation.

• Nuclear Medicine and Molecular Imaging
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• v.40 no.2
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• pp.58-65
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• 2006

Since the development of sophisticated molecular carriers such as octereotides for peptide receptor targeting and monoclonal antibodies against various antigens associated with specific tumor types, radionuclide therapy (RNT) employing open sources of therapeutic agents is promising modality for treatment of tumors. furthermore, the emerging of new therapeutic regimes and new approaches for tumor treatment using radionuclide are anticipated in near future. In targeted radiotherapy using peptides and other receptor based tarrier molecules, the use of radionuclide with high specific activity in formulating the radiopharmaceutical is essential in order to deliver sufficient number of radionuclides to the target site without saturating the target. In order to develop effective radiopharmaceuticals for therapeutic applications, it is crucial to carefully consider the choice of appropriate radionuclides as well as the tarrier moiety with suitable pharmacokinetic properties that could result in good in vivo localization and desired excretion. Up to date, only a limited number of radionuclides have been applied in radiopharmaceutical development due to the constraints in compliance with their physical half-life, decay characteristics, cost and availability in therapeutic applications. In this review article, we intend to provide with the improved understanding of the factors of importance of appropriate radionuclide for therapy with respect to their physical properties and therapeutic applications.

• Radioisotope journal
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• v.21 no.3
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• pp.46-60
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• 2006

In recent years the progress of nuclear medicine advanced dramatically in imaging and targeted radionuclide therapy is able to open op exciting perspectives as standard diagnostic and therapeutic modalities, complementing conventional modalities. Positron emission tomography/computed tomography (PET/CT) technology with FDG has been developed clinically in less than 10 years as a routine standard in oncological imaging, including a number of other fluorinated radiopharmaceuticals being evaluated for their ability to complement FDG. However, the limitation of FDG-PET such as non-specific uptake and its short half-life is not compatible with the time necessary for optimal tumour targeting. Therefore, a development of innovative positron-emitting radionuclides with half-lives longer than 10 h is needed. For therapeutic applications, the injection of higher activities is required to reach efficient adsorbed doses in radioresistant solid tumours, while limiting the irradiation of vital organs. In this application, the longer half-life of radiolsotopes are more fit well for radionuclide therapy. To achieve this, researches have to be carried in a largor spectrum of radionuclides for diagnosis and therapy. In the context of rapidly growing nuclear medicine and strong demanding innovative radionuclides, a high-energy (100 MeV), high-intensity (-mA) accelerator with proton (PEFF at KAFRI). will be operating in 2011. The priorities of PEFP will include supporting the nuclear medicine research community by providing those radionuclides with current limited availability by means of a high-energy, high-intensity accelerator.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.9 no.1
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• pp.49-55
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• 2023

Tumors are encircled by various non-cancerous cell types in the extracellular matrix, including fibroblasts, endothelial cells, immune cells, and cytokines. Fibroblasts are the most critical cells in the tumor stroma and play an important role in tumor development, which has been highlighted in some epithelial cancers. Many studies have shown a tight connection between cancerous cells and fibroblasts in the last decade. Regulatory factors secreted into the tumor environment by special fibroblast cells, cancer-associated fibroblasts (CAFs), play an important role in tumor and vessel development, metastasis, and therapy resistance. This review addresses the development of FAP inhibitors, emphasizing the first, second, and latest generations. First-generation inhibitors exhibit low selectivity and chemical stability, encouraging researchers to develop new scaffolds based on preclinical and clinical data. Second-generation enzymes such as UAMC-1110 demonstrated enhanced FAP binding and better selectivity. Targeted treatment and diagnostic imaging have become possible by further developing radionuclide-labeled fibroblast activation protein inhibitors (FAPIs). Although all three FAPIs (01, 02, and 04) showed excellent preclinical and clinical findings. The final optimization of these FAPI scaffolds resulted in FAPI-46 with the highest tumor-to-background ratio and better binding affinity.

• Journal of radiological science and technology
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• v.45 no.5
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• pp.433-438
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• 2022

Targeted radionuclides treatment (TRT) requires the establishment of treatment plans that consider various factors, such as the type of radionuclides, target organs, and administration methods. For this reason, in this study, the absorption dose of a single cell was analyzed according to the type of radioisotope used to treat target radionuclides. In this study, a simulation was performed on beta rays used in the treatment of target radionuclides at the cell level using MCNPX (ver. 2.5.0). First, according to the calculation formula, the beam path according to the type of radioisotope for treatment was calculated. Second, the amount of self-radiation by beta rays emitted from cell diameters of 5 ㎛ and 10 ㎛ cell nuclei was evaluated. As a result, it showed a high range proportional to the maximum energy of the beta-ray, and the highest self-dose distribution from 177 Lu radiation sources among therapeutic radioisotopes. This was analyzed as a result that is inversely proportional to the maximum energy of the beta-ray, and it suggests that the selection of a nuclide considering the range of the beta-ray is necessary in the treatment of target radionuclides in the future.