Radiometals for nuclear medicine

Radiometals play an important role in nuclear medicine^1-3 for the diagnosis or therapy of various diseases. Beside technetium-99m, the most frequently used radionuclide for in-vivo- diagnosis because its optimal nuclide properties, economically supply by the ⁹⁹Mo/^99mTc generator and easy preparation of the ^99mTc-radiopharmaceutical in the clinic, current search for metalloradiopharmaceuticals focuses on both unconventional positron emitting metals (e.g. Cu-64, Ga-66, Y-86, Tc-94m) as potential agents for positron emission tomography (PET) and of radiometal agents labeled with particle emitters for radionuclide therapy³. Since the basic requirement for therapeutic radiopharmaceuticals, namely to induce high effective dose for the target but practically no interference with healthy tissue is not fulfilled yet, the number of therapeutic radiopharmaceuticals for routine use is limited.
Besides the availability of suitable nuclides, the design of chelate systems for stable binding of the radiometal is a crucial point in the development of new metalloradiopharmaceuticals. The chemistry of respective chelates designed in recent years for binding technetium and rhenium at various oxidation states will be discussed. Such chelates involve mixed-ligand complexes containing the metalnitrido core at oxidation state V, Tc(III)/Re(III) and organometallic Tc(I)/Re(I) complexes.
Finally, the application of these chelates for labeling peptides and receptor-affine coordination compounds will be demonstrated.