Abstract Modern approaches to copper-mediated radiolabeling have proven an important addition to the radiochemical toolbox. Radiopharmaceuticals prepared using this methodology have been translated from preclinical PET studies into clinical trials, and it has been adapted for radionuclides beyond fluorine-18, enabling theranostic applications. The methodology is also beginning to benefit from AI-assisted radiochemistry development. This perspective discusses the history, state-of-the-art, and potential future impact of copper-mediated radiochemistry on radiopharmaceutical development.
