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The development of nanomedicines presents the potential to deliver more potent drugs targeted more specifically to the site(s) of disease than is currently achievable. While encouraging results have been achieved, including at the clinical level, significant challenges and opportunities for development remain, both in terms of further developing the technology and in understanding the underlying biology. Given the lessons learned regarding variations in nanomedicine delivery to different tumor types and between different patients with the same tumor type, this is an area of drug development that, rather than simply benefiting from a patient-specific approach, actually demands it. The only way that this distribution information can be obtained is through imaging, and this requires labeling of the nanomedicine to enable detection outside the body.In this review, we describe recent advances in the labeling of nanomedicines, how imaging studies are guiding nanomedicine development, and the role of imaging in the future development of nanomedicines.Radiolabeled nanotherapeutics and molecular imaging can be used to measure uptake of a therapeutic agent in the target tissue. This information can be used to individualize patient care.