Development of targeted radiopharmaceuticals for specific cellular receptors is an ongoing area of research to improve diagnosis and treatment of diseases. Metal-based radiopharmaceuticals are composed of a radionuclide, bifunctional chelator and a biologically active targeting agent. In order to drive reaction kinetics and improve yields, large excesses of targeting agent are used, which results in low specific activity samples. Without purification, unlabeled compounds can saturate the cellular receptors resulting in poor image quality. High specific activity material can often be obtained using purification (e.g., HPLC) after coordination of the metal, however; this purification method is not suitable for wide scale clinical applications of radiopharmaceuticals. With a suitable metal-cleavable linker, solid phase synthesis can be used to supply high specific activity radiopharmaceuticals with minimal purification. Using 2,2’-dipicolylamine as a chelator, a linker which is cleaved by coordination of fac-[MI(CO)3]+ (M = Re, 99mTc) was developed. This system was studied to determine labeling and cleavage efficiency, stability, effect of resin, and reactivity at different pH levels. Incorporation of biologically relevant molecules onto this system could potentially yield a method for synthesizing fac-[MI(CO)3]+ radiopharmaceuticals for clinical applications.

Development of a new solid-phase method for the production of high-specific activity fac-[MI(CO)3]+ (M = Re, 99mTc) radiopharmaceuticals

251st National Meeting (2016)

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