Molecular imaging is expected to change the face of drug discovery and development. The ability to link imaging to biology for guiding therapy should improve the rate at which novel imaging technologies, probes, contrast agents, drugs and drug delivery systems can be transferred into clinical practice. Nuclear medicine imaging, in particular, positron emission tomography (PET) allows the detection and monitoring of a variety of biological and pathophysiological processes, at tracer quantities of the radiolabelled target agents, and at doses free from pharmacological effects. In the field of drug discovery and development, the use of radiotracers for radiolabelling target agents has now become one of the essential tools in identifying, screening and development of new target agents. In this regard, (64)Cu (t(1/2)=12.7 h) has been identified as an emerging PET isotope. Its half-life is sufficiently long for radiolabelling a range of target agents and its ease of production and adaptable chemistry make it an excellent radioisotope for use in molecular imaging. This review describes recent advances, in the routes of (64)Cu production, design and application of bi-functional ligands for use in radiolabelling with (64/67)Cu(2+), and their significance and anticipated impact on the field of molecular imaging and drug development.