Abstract: Novel N3S1 chelator-folate derivatives, a preparation method thereof, and a composition for diagnosis and treatment of tumor including the same as an active ingredient are provided. The novel N3S1 chelator-folate derivatives or a pharmaceutically acceptable salt thereof are easily introduced into the cells using receptor binding to tumor expressing ?-folate receptor (?-FR). Accordingly, the folate derivatives, labeled with radioisotope such as technetium, or rhenium, can be advantageously used for the diagnosis and treatment of tumor using tumor imaging and irradiation from the isotope, and therefore, can be widely used for the purpose of labeling a variety of radiopharmaceuticals.

Abstract: Novel N3S1 chelator-folate derivatives, a preparation method thereof, and a composition for diagnosis and treatment of tumor including the same as an active ingredient are provided. The novel N3S1 chelator-folate derivatives or a pharmaceutically acceptable salt thereof are easily introduced into the cells using receptor binding to tumor expressing ?-folate receptor (?-FR). Accordingly, the folate derivatives, labeled with radioisotope such as technetium, or rhenium, can be advantageously used for the diagnosis and treatment of tumor using tumor imaging and irradiation from the isotope, and therefore, can be widely used for the purpose of labeling a variety of radiopharmaceuticals.

Abstract: Disclosed are chelating agent-conjugated ?-MSH peptide derivatives, preparation methods thereof, and compositions for use in a diagnosis or treatment of a melanoma tumor containing the same as an active ingredient. The novel ?-MSH peptide derivatives conjugated with chelating agent according to the present invention are highly selective to the melanocortin-1 receptor which is ?-MSH receptor expressing in melanoma tumor and their labeling rate of a radioactive isotope is high. Also, they remain in kidney shortly and have high taking rate of the melanoma tumor. Therefore, with the aforesaid reasons, they may be effectively used for early diagnosis or treatment of melanoma tumor.

Abstract: The present invention relates to diethylenetriamine pentaacetic acid (DTPA) derivates and metal complexes thereof, and radiation sources and contrast agents including the metal complexes. More particularly, the present invention relates to DTPA derivatives, which contain iodine and are useful as contrast agents for diagnosing renal function, metal complexes of the DTPA derivatives with 99mTc, 166Ho, 111In, 90Y, 153Sm, 186Re, 188Re, 68Ga, or 177Lu, which are useful as liquid radiation sources for treating vascular stenosis and contrast agents for diagnosing renal function, and radiation sources and contrast agents including the metal complexes. The DTPA derivatives and metal complexes thereof are safe because the metal complexes are excreted via the kidneys and bladder within several minutes from the time of use as liquid radiation sources for treating vascular stenosis, and are cost-effective because they are potentially useful as contrast agents and as agents for diagnosing renal function.

Abstract: Disclosed are chelating agent-conjugated ?-MSH peptide derivatives, preparation methods thereof, and compositions for use in a diagnosis or treatment of a melanoma tumor containing the same as an active ingredient. The novel ?-MSH peptide derivatives conjugated with chelating agent according to the present invention are highly selective to the melanocortin-1 receptor which is ?-MSH receptor expressing in melanoma tumor and their labeling rate of a radioactive isotope is high. Also, they remain in kidney shortly and have high taking rate of the melanoma tumor. Therefore, with the aforesaid reasons, they may be effectively used for early diagnosis or treatment of melanoma tumor.

Abstract: A radio-immunoconjugate for diagnosis and treatment of cancer or metastasis and development of metastasis inhibitory formulations using the same is provided. Also, a radio-immunoconjugate is used as a material indicating a metastatic cancer that has antibody marked with any lanthanum radionuclide and/or gamma, beta or alpha ray emitting radioisotopes targeting a vascular endothelial growth factor receptor (VEGFR) is provided. Such a radio-immunoconjugate is advantageous in that it maintains structural stability of a protein and immune activity thereof and is effectively adsorbed to the surface of vascular endothelial cells. This makes it useful as a pre-metastatic site detection factor. When the radio-immunoconjugate is administered to an animal model with cancer, the radio-immunoconjugate is accumulated in cancerous tissues. Therefore, it is useful for development of radioactive metastasis inhibitory formulations.

Abstract: The present invention relates to diethylenetriamine pentaacetic acid (DTPA) derivates and metal complexes thereof, and radiation sources and contrast agents including the metal complexes. More particularly, the present invention relates to DTPA derivatives, which contain iodine and are useful as contrast agents for diagnosing renal function, metal complexes of the DTPA derivatives with 99mTc, 166Ho, 111In, 90Y, 153Sm, 186Re, 188Re, 68Ga, or 177Lu, which are useful as liquid radiation sources for treating vascular stenosis and contrast agents for diagnosing renal function, and radiation sources and contrast agents including the metal complexes. The DTPA derivatives and metal complexes thereof are safe because the metal complexes are excreted via the kidneys and bladder within several minutes from the time of use as liquid radiation sources for treating vascular stenosis, and are cost-effective because they are potentially useful as contrast agents and as agents for diagnosing renal function.

Abstract: A method for labelling a sulfide compound with technetium or rhenium, comprising the reaction of a disulfide compound with pertechnetate or perrhenate in the presence of borohydride exchange resin to obtain a complex of technetium or rhenium with the sulfide compound. The method can directly label disulfide compounds with technetium or rhenium, can skip the synthetic step of thiol-protected S-precursor, and is useful for high value-added radiopharmaceuticals.

Abstract: The present invention relates to a method of preparing technetium or rhenium complex for radiopharmaceuticals, through reaction of pertechnetate or perrhenate with a ligand in the presence of a reducing agent, wherein the reducing agent is a borohydride exchange resin (BER). The borohydride exchange resin of the present invention has advantages of being stable in a wide range of Ph, including acidic or alkaline condition(Ph 2˜14) and thus being applicable to biological materials as well as being easily removable through filtration when being administrated. Also since the radiolabelled complex is produced under conditions milder than those required for the conventional reducing agents as well as has high radiochemical purity and high labeling efficiency, the conventional reducing agents can be replaced by the BER of the present invention.

Abstract: The present invention relates to a method of preparing technetium or rhenium complex for radiopharmaceuticals, through reaction of pertechnetate or perrhenate with a ligand in the presence of a reducing agent, wherein the reducing agent is a borohydride exchange resin (BER) . The borohydride exchange resin of the present invention has advantages of being stable in a wide range of Ph, including acidic or alkaline condition(Ph 2˜14) and thus being applicable to biological materials as well as being easily removable through filtration when being administrated. Also since the radiolabelled complex is produced under conditions milder than those required for the conventional reducing agents as well as has high radiochemical purity and high labeling efficiency, the conventional reducing agents can be replaced by the BER of the present invention.

Abstract: The present invention relates to a method for labelling a sulfide compound with technetium or rhenium, comprising the reaction of a disulfide compound with pertechnetate or perrhenate in the presence of borohydride exchange resin to obtain a complex of technetium or rhenium with the sulfide compound. The method can directly label disulfide compounds with technetium or rhenium, can skip the synthetic step of thiol-protected S-precursor, and is useful for high value-added radiopharmaceuticals.