Korea Atomic Energy Research Institute

Young-Don Hong

So-Young Lee

Sun-Ju Choi

Jae Deok Lim

Dong Eun Lee

Sun Ju Choi

Kang-Hyuk Choi

Ok Ja Choi

Novel NSchelator-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 NSchelator-folate derivatives or a pharmaceutically acceptable salt thereof are easily introduced into the cells using receptor binding to tumor expressing &#x3b1;-folate receptor (&#x3b1;-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.

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Disclosed are chelating agent-conjugated &#x3b1;-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 &#x3b1;-MSH peptide derivatives conjugated with chelating agent according to the present invention are highly selective to the melanocortin-1 receptor which is &#x3b1;-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.

Chelating agent conjugated &#x3b1;-MSH peptide derivatives, preparation method thereof and composition for diagnosis and treatment of melanoma comprising the same as an active ingredient

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 withTc,Ho,In,Y,Sm,Re,Re,Ga, orLu, 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.

DTPA derivatives and metal complexes thereof, and radiation source and contrast agent including the metal complexes

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Daejeon, South Korea

Young-Don Hong