The present invention relates to tricarbonyl
technetium-99m or
rhenium-188 labeled cyclic RGD derivatives, a preparation method thereof, and a pharmaceutical composition containing the derivative as an
active ingredient for use in the diagnosis or treatment (radiotherapy) of
angiogenesis-related diseases. The tricarbonyl
technetium-99m or
rhenium-188 labeled cyclic RGD derivatives of the present invention has a high subnanomolar affinity to
integrin αvβ3 (also called as a
vitronectin receptor) that is activated in an angiogenic action induced by a tumor, reflects a high tumor image of the tricatvonyl
technetium-99m labeled cyclic RGD derivative after initial intake in an animal in which
cancer cells are transplanted, and acts exclusively upon
cancer cells having selectively activated
integrin αvβ3 because of a substantially low intake into the liver and intestines, compared to existing known radioactive
isotope labeled cyclic RGD derivatives. These results show that the
rhenium-188 labeled derivative, a therapeutic
nuclide using the same precursor as used in the technetium-99m labeling, effectively inhibits the growth of a tumor and demonstrates therapeutic
efficacy when administered via
tail vein injection to an
animal model bearing tumor, compared to a case where only
saline has been injected, thereby making it useful as a
medicine for the diagnosis or treatment of
angiogenesis-related diseases.