The clinical translation of new radioisotopes is accelerated by ease of synthesis of radiopharmaceuticals, specifically by shake-only kit formulations. To date, the routine use of radioisotopes using room temperature labeling compatible kits is hampered by the lack of corresponding radiochemical labeling approaches. Additionally, emerging isotopes such as 44Sc and 68Ga require secondary purification of cyclotron or generator eluate, which significantly reduces the ability of radiopharmacies to produce large numbers of patient doses. We proposed that these shortcomings could be addressed by a radiochemical synthesis approach that combines separation and radiochemical labeling steps efficiently and produces a ready-to-inject radiopharmaceutical using a resin-based, one-pot procedure. We demonstrate, that a solid-phased radiolabeling approach, followed by photochemical cleavage of the ready-made radiopharmaceutical is a convenient and feasible approach to concerted capture and radiolabeling of bifunctional bioconjugates. We successfully achieved the on-resin radiolabeling, subsequent photocleavage and formulation of two clinically translated radiopharmaceutical precursors, NOTA-Aca-BBN (targeting gastrin-releasing peptide receptor) and NOTA-PSMA on resin with 67Ga in under 30 minutes. We will also discuss the feasibility to expand of the scope of this radiolabeling approach to biomolecules and other radioisotopes of interest.

Solid-phase radiosynthesis accompanied by photocleavage strategy for synthesis of radiopharmaceuticals

ACS Spring 2022

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