Tricarbonyl technetium-99m, rhenium-185/187, or rhenium-188 labeled cyclic RGD derivatives and uses thereof

摘要

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 α_vβ₃ (also called as a vitronectin receptor) that is activated in an angiogenic action induced by a tumor, and acts exclusively upon cancer cells having selectively activated integrin α_vβ₃ because of a substantially low intake into the liver and intestines.