BRC lab develops new way of preparing radiotracers

Dr Erik Arstad, who is leading the NIHR University College London Hospitals BRC Radiochemistry Laboratory, has developed a novel method for the preparation of radioactive iodine containing tracers for use in nuclear imaging. 

Nuclear imaging uses small amounts of radioactive material, or radiotracer, to diagnose a wide range of diseases. Radiotracers are designed to accumulate in the body and visualize the disease processes happening. Once the tracer has been administered, a specialized (gamma) camera is used to detect the radiation throughout the body. Distribution of the radiation gives information about disease.

However, because the radioactivity decays quickly it is important that the tracers are synthesized rapidly and used immediately. The efficient preparation of radiotracers with the right biological properties is challenging.

Dr Arstad and his team have developed a one-pot three-component reaction that enables highly complex radiotracers to be synthesized in one step. Results from their study, which has already been communicated in Angewandte Chemie Int. Ed, will be published in Journal of the American Chemical Society.

Science behind the development of a One-Pot Three-Component Radiochemical Reaction for Rapid Assembly of 125I-labeled Molecular Probes

Whilst the optimal choice of radionuclide depends on the intended application, as well as the structural requirements of the biological target, the numerous isotopes of iodine available support widespread use across biological research, diagnostic imaging and radiotherapy.

The three-component reaction enables functionalized azides and alkynes to be reacted in the presence of radioiodine to yield structurally diverse iodotriazoles. The ability to incorporate radioactive iodide into triazoles directly from the parent azides and alkynes makes the method broadly applicable, and offers the potential to rapidly assemble molecular probes from an array of structurally diverse, and readily available, building blocks.

This discovery has the potential to transform the development of tracers for biomedical imaging and therapeutic applications.