• Nuclear Medicine and Molecular Imaging
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• v.40 no.2
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• pp.82-89
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• 2006

Bone metastasis is a common sequelae of solid malignant tumors such as prostate, breast, lung, and renal cancers, which can lead to various complications, including fractures, hypercalcemia, and bone pain, as well as reduced performance status and quality of life it occurs as a result of a complex pathophysiologic process between host and tumor cells leading to cellular invasion, migration adhesion, and stimulation of osteoclastic and osteoblastic activity. Several sequelae occur as a result of osseous metastases and resulting bone pain can lead to significant debilitation. A multidisciplinary approach is usually required not only to address the etiology of the pain and its complicating factors but also to treat the patient appropriately. Pharmaceutical therapy of bone pain, includes non-steroidal analgesics, opiates, steroids, hormones, bisphosphonates, and chemotherapy. While external beam radiation therapy remains the mainstay of pain palliation of a solitary lesions, bone seeking radiopharmaceuticals have entered the therapeutic armamentarium for the treatment of multiple painful osseous lesions. $^{32}P,\;^{89}SrCl,\;^{153}Sm-EDTMP,\;^{188}Re/^{186}Re-HEDP,\;and\;^{177}Lu-EDTMP$ can be used to treat painful osseous metastases. These various radiopharmaceuticals have shown good efficacy in relieving bone pain secondary to bone metastasis. This systemic form of metabolic radiotherapy is simple to administer and complements other treatment options. This has been associated with improved mobility in many patients, reduced dependence on narcotic and non-narcotic analgesics, improved performance status and quality of life, and, in some studios, improved survival. All of these agents, although comprising different physical and chemical characteristics, offer certain advantages in that they are simple to administer, are well tolerated by the patient if used appropriately, and can be used alone or in combination with the other forms of treatment. This article illustrates the salient features of these radiopharmaceuticals, including the usual therapuetic dose, method of administration, and indications for use and also describe about the pre-management checklists, and jndication/contraindication and follow-up protocol.

• Journal of Radiation Industry
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• v.17 no.4
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• pp.417-425
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• 2023

Lutetium(¹⁷⁷Lu), with its theranostic properties, is one of the most widely used radioisotopes and has a large share of the radiopharmaceutical market due to its many applications and targeted therapeutic research using lutetium-based radiopharmaceuticals. However, lutetium-based radiopharmaceuticals currently approved by the US Food and Drug Administration (FDA) are limited to the indications of gastrointestinal cancer, pancreatic neuroendocrine cancer and metastatic castration-resistant prostate cancer. To overcome these limitations, we aimed to demonstrate the feasibility of expanding the use of lutetium-based radiopharmaceuticals by verifying the availability and therapeutic efficacy of lutetium produced in a research reactor(HANARO). In this study, we confirmed the therapeutic efficacy of lutetium by using cancer cells from different types of cancer. In addition, we selected cancer biomarkers based on characteristics common to various cancer cells and compared and evaluated the therapeutic efficacy of lutetium by regulating the expression of target genes. The results showed that modulation of cancer biomarker gene expression resulted in higher therapeutic efficacy compared to lutetium alone. In conclusion, this study verified the potential use and therapeutic efficacy of lutetium based on the production of a research reactor (HANARO), providing fundamental evidence for the development of lutetium-based radiopharmaceuticals and the expansion of their indications.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.129-133
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• 2017

Since carbon-fluorine (C-F) bonds play a key role to improve bioavailability and lipophilicity, they have found commonly in pharmaceuticals, radiopharmaceuticals, agrochemicals, and material science. Advances on the efficient method to introduce fluorine to complex organic molecules are mainly results of development of fluorination reagents and transition metal catalysts. In this mini-review, we want to emphasize two representative nucleophilic fluorinating reagents regarding carbon-fluorine bond formation, which were developed in the mid-2000s.

• The Korean Journal of Nuclear Medicine
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• v.34 no.3
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• pp.159-168
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• 2000

In the 1980s, techniques to image the human subjects in a three-dimensional direction were developed. Two major techniques are SPECT (Single Photon Emission Computed Tomography) and PET (Positron Emission Tomography) which allow the detector to detect a single photon or annihilation photons emitted from the subjects injected with radiopharmaceuticals. Since the latter two techniques can measure the density of receptors, enzymes and transporters in living human, it may be very important project to develop selective methods of labeling with radionuclides and to develop new radiopharmaceuticals. There has been a considerable interest in developing new compounds which specifically bind to dopamine and serotonin receptor and transporters, and it will be thus very useful to label those compounds with radionuclides in order to gain a better understanding in biochemical and pharmacological interactions in living human. This review mentions the characteristics of radioligands for the imaging of dopamine and serotonin receptors and transporters. Although significant progress has been achieved in the development of new PET and SPECT ligands for in vivo imaging of those receptors and transporters, there are continuous needs of new diagnostic radioligands.

• Proceedings of the Korean Nuclear Society Conference
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• 2005.05a
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• pp.940-941
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• 2005

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.2 no.1
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• pp.51-55
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• 2016

Organofluorine compounds have become increasingly important as pharmaceuticals, radiopharmaceuticals, agrochemicals, and material science. Recent advances on the efficient introduction of fluorine to organic molecules are mainly results of development of transition metal catalysts and fluorination reagents. Among the various fluorination reagents, we have been interested in developing more efficient sulfur-based deoxyfluorinating reagents. Here we report various electronic properties of five popular sulfur-based deoxyfluorinating reagents using density functional theory calculation. We believe that the theoretical study on the reagents will assist the rational design of new deoxyfluorinating reagents.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.8 no.1
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• pp.25-32
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• 2022

Malignant melanoma has an aggressive nature and high metastatic potential that result in one of the highest cancer mortality rates. Over the past three decades, primary and metastatic melanoma incidence has rapidly increased. The recent advances in diagnostic technology have shown promise, but there is still an enormous need for specific detection methods to diagnose malignant melanoma. Positron emission tomography can visualize a particular biomarker of malignant melanoma and promise a noninvasive image of micrometastases. However, the development of PET radiopharmaceuticals remains necessary for diagnosing malignant melanoma by using positron emission tomography. In this review, the history and a general overview of PET radionuclide labeled benzamide derivatives, including their radiosynthesis, in vivo characterization, and evaluation, are provided as imaging agents for malignant melanoma.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.7 no.1
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• pp.50-55
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• 2021

Low-dose radiotherapy has been known to have anti-inflammatory activity and been used for treatment of pneumonia together with anti-serum and sulfanilamide. However, it rapidly discontinued after the development of various antibiotics showing outstanding effect. Recently, it was re-considered to treat COVID-19 which has very limited treatment such as remdesivir and dexamethasone. So, several studies of COVID-19 therapy using low-dose radiation were reported very recently. They showed that low-dose radiation of 0.5~1.5 Gy were useful for decreasing the oxygen consumption and hospitalization period of COVID-19 patients without adverse reaction. Radiopharmaceuticals such as [⁹⁹mTc]Tc-macroaggregated albumin (MAA) also might be used for low-dose radiotherapy. Administration of vitamin D having anti-inflammatory effect would also be helpful for therapy with synergistic effect.

• Korean Journal of Clinical Laboratory Science
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• v.55 no.4
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• pp.253-260
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• 2023

The germanium-68/gallium-68 (⁶⁸Ge/⁶⁸Ga) generator has high spatial utilization and requires little maintenance, making it economical and easy to produce. Thus, the frequency of use of ⁶⁸Ga radiopharmaceuticals is rapidly increasing worldwide. Therefore, this study attempted to develop an automated synthesizer for the routine clinical application of ⁶⁸Ga radiopharmaceuticals. The automated synthesizer was based on a fixed tubing system and the structure was designed after adjusting the position of the parts to reflect the synthesis method. Using various components that can be supplied in Korea, the automated synthesizer was manufactured at a much lower price cost than that of a commercialized automated synthesizer sold by companies. ⁶⁸Ga-DOTA-[Tyr3]-octreotide (⁶⁸Ga-DOTATOC) was synthesized to evaluate the performance of the automated synthesizer. ⁶⁸Ga-DOTATOC could be synthesized with about 65% of non-decay corrected yield, and the synthesized ⁶⁸Ga-DOTATOC met all quality control standards. We have synthesized ⁶⁸Ga-DOTATOC more than 100 times, and only faced a few problems caused by mechanical errors. In this study, we successfully developed a simple automated synthesizer for ⁶⁸Ga radiopharmaceuticals with high reproducibility. As various ⁶⁸Ga radiopharmaceuticals have recently been developed, it is expected that the automated synthesizer developed in this study will be useful for routine clinical use.

• 대한핵의학회:학술대회논문집
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• 1999.05a
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• pp.196-199
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• 1999

Radiation synovetomy with various radiopharmaceuticals has been used to alleviate pain and swelling of rheumatoid arthritis and related joint diseases for more than 40 years. It is an attractive alternative to the surgical synovectomy for the management of the various joint diseases. Recently, the development of new radiopharmaceuticals labeled with $^{90}Y,\;^{32}P,\;^{186}Re,\;^{188}Re,\;^{153}Sm,\;^{165}Dy$ and $^{166}Ho$, for the effective management of synovial inflammation and related arthritic problems are gaining attention. In this article the general concepts and the clinical application of radiation synovectomy are reviewed.