Clinical Applications of Small-molecule PET Radiotracers: Current Progress and Future Outlook

Radiotracers, or radiopharmaceuticals, are bioactive molecules tagged with a radionuclide used for diagnostic imaging or radiotherapy and, when a positron-emitting radionuclide is chosen, the radiotracers are used for PET imaging. The development of novel PET radiotracers in many ways parallels the development of new pharmaceuticals, and small molecules dominate research and development pipelines in both disciplines. The 4 decades since the introduction of [¹⁸F]FDG have seen the development of many small molecule PET radiotracers. Ten have been approved by the US Food and Drug Administration as of 2016, whereas hundreds more are being evaluated clinically. These radiotracers are being used in personalized medicine and to support drug discovery programs where they are greatly improving our understanding of and ability to treat diseases across many areas of medicine including neuroscience, cardiovascular medicine, and oncology.