Radioiodine Labeling Reagents and Methods for New Chemical Entities and Biomolecules

Several radioisotopes of iodine (¹²³I, ¹²⁴I, ¹²⁵I, and ¹³¹I) are available for medical use. One of them can be used, depending on the application, for radioiodine labeling of New Chemical Entities (NCEs) and biomolecules (peptides, proteins, protein fragments, monoclonal antibodies, etc.) for the development of novel imaging and therapeutic pharmaceuticals. Direct, using inorganic and organic oxidizing agents and enzyme catalysts, and indirect, using prosthetic groups, radioiodine-labeling methods have been used routinely in the past. In this report, a comprehensive review of the physical properties of various iodine radionuclides, their medical applications, and a summary of various radioiodine labeling reagents and methods for NCEs and biomolecules are provided.