Concerted, Selective Radiometallation and Photo-triggered Release of Ready-to-Inject Radiopharmaceuticals from the Solid Phase

Background

Radiopharmaceuticals are agents which enable non-invasive patient diagnosis and personalized therapeutic intervention strategies. Radionuclides used in nuclear medicine applications must be purified after nuclear synthesis to separate them from the target material. Radioisotopes used in radiopharmaceutical production often have short half-lives, and require fast, simple and modular synthesis methods to produce the target with high yield, purity, and molar activity. However, current radiosynthesis strategies are time-consuming, multi-step processes which often leads to the decay of a significant amount of the radionuclide before it can be used. There remains a need for improved radiosynthesis strategies which can condense the steps required to prepare radiopharmaceuticals in a more rapid, clean fashion than existing methods.

Technology

The Boros Lab has developed a solid-phase, concerted separation and radiosynthesis strategy with photochemical release of radiotracers in biocompatible solvents to prepare injectable radiopharmaceuticals. This Solid Phase Radiometallation Photorelease (SPRP) method involves the selective capture of the radionuclide by a solid-phase appended peptide chelator conjugate, allowing for simultaneous radiochemical labeling and selective removal of excess trace metal impurities from large stock volumes. Photochemical release provided radiopharmaceuticals with >95% radiochemical purity and excellent in vivo performance in a preclinical mouse model. SPRP has the potential to accelerate and simplify selective metallation beyond the radiochemical synthesis of radiopharmaceuticals, and provide a versatile platform technology for the development of a large class of metal-based pharmaceuticals