Imaging COX-2 expression in cancer using PET/SPECT radioligands: current status and future directions


  • This article is published in the Journal of Labelled Compounds and Radiopharmaceuticals as a special issue on ‘Current Developments in PET and SPECT Imaging’, edited by Jonathan R. Dilworth, University of Oxford and Sofia I. Pascu, University of Bath.


The role of cyclooxygenase (COX)-2 as a driving force in early tumourigenesis and the current interest in the combination of COX-2 inhibitors with standard therapy in clinical trials creates an urgent need to establish clinically relevant diagnostic tests for COX-2 expression. Molecular imaging using small-molecule probes radiolabelled for both positron emission tomography (PET) and single photon emission computed tomography (SPECT) offers the potential to meet this need, providing a minimally invasive readout for the whole disease burden. This review summarises current approaches to the radiolabelling of small-molecule COX-2 inhibitors and their analogues for PET and SPECT imaging, and gives an overview of their biological evaluation and likely success of clinical application.