Synthesis, Radiolabeling and In Vivo Tissue Distribution of an Anti-Oestrogen Glucuronide Compound, Tc-99m-TOR-G

Toremifene (TOR) has been used as an anti-oestrogen drug for the treatment and prevention of human breast cancer. The aim of this study was the addition of the hydrophilic groups diethylenetriamine pentaacetic acid (DTPA) and glucuronic acid to the starting substance TOR and to label it with technetium-99m (Tc-99m) radionuclide and to investigate radiopharmaceutical potential of the new compound. The synthesis reactions are completed in four steps, including enzymatic reaction, with the following sub-steps; preparation of microsomal fraction from Hutu 80 cell line and subsequent purification of UDP-glucuronyl transferase (UDPGT), estimation of protein quantity in microsomal samples and glucuronidation reaction. The results indicate that Tc-99m-TOR-G may be proposed as a new anti-oestrogen glucuronide imaging agent for ovarian tumours.