Chapter 8. Labelling of biotin with 188Re

Different chemical strategies have been employed for labelling biotin using 188Re with the aim to develop a sterile and pyrogen free kit formulation that is suitable for clinical use. A number of biotin conjugated 188Re complexes were prepared and evaluated to determine their affinity for avidin. The most difficult challenge was to devise an efficient reaction pathway that was able to obtain the final radiocompounds in a high radiochemical yield. This work describes the molecular design and the chemical strategy that were followed to obtain reliable preparation of the new radiopharmaceuticals starting from generator produced [188ReO4]–.