Bioorthogonal chemistry: implications for pretargeted nuclear (PET/SPECT) imaging and therapy

Am J Nucl Med Mol Imaging. 2014 Mar 20;4(2):96-113. eCollection 2014.


Due to their rapid and highly selective nature, bioorthogonal chemistry reactions are attracting a significant amount of recent interest in the radiopharmaceutical community. Over the last few years, reactions of this type have found tremendous utility in the construction of new radiopharmaceuticals and as a method of bioconjugation. Furthermore, reports are beginning to emerge in which these reactions are also being applied in vivo to facilitate a novel pretargeting strategy for the imaging and therapy of cancer. The successful implementation of such an approach could lead to dramatic improvements in image quality, therapeutic index, and reduced radiation dose to non-target organs and tissues. This review will focus on the potential of various bioorthogonal chemistry reactions to be used successfully in such an approach.

Keywords: PET; Pretargeting; SPECT; bioorthogonal chemistry; click chemistry; molecular imaging.

Publication types

  • Review