Abstract The goal of this research is to develop a new agent based on multiwalled carbon nanotubes (MWCNT) for the diagnosis and monitoring of advanced breast cancer. MWCNT consist of sheets of graphene carbon rolled into multiwalled tubes and possess many properties that make them extremely useful in biomedical applications, including targeted molecular imaging. Foremost is their ability to deliver large numbers of imaging agents per each targeted molecular recognition event, which can improve the sensitivity of imaging; secondly, they can deliver several different types of imaging agents (such as magnetic resonance imaging or photoacoustic agents) to perform multimodality imaging; thirdly, they can be used for therapeutic applications including chemotherapeutic drug or gene delivery, and as mediators for photothermal cancer therapy. As early and accurate diagnosis is still the most effective approach to treating cancer, improvements in the use of imaging technology to detect and monitor cancer will have a dramatic effect on human health. Breast cancer cells have alterations in the normal metabolism of the sugar, glucose, and exhibit increased glucose uptake and decreased glucose clearance. The hypothesis to be tested is that MWCNTs targeted to glucose transporters will be taken up by cancer cells with high efficiency, and that such MWCNT can be engineered to be effective cancer diagnostic agents. To this end, we have chemically engineered MWCNTs to display deoxyglucose on their surface, which rendered them water soluble, and targets them to cancer cells. It is anticipated that this agent will serve as the basis for a multimodal platform for future combined cancer therapy and diagnostic applications. We now report on our initial findings with this agent, and describe: 1) a new, glycosylated MWCNT which can be traced by radiolabelling; 2) data on clinically-relevant issues relating to blood compatibility, and preclinical data on toxicity (clot formation), biodistribution, blood, urinary, and fecal clearance of intravenously injected glycosylated MWCNT, all of which will be essential for any future translational applications; 3) a new nanomedical platform technology, developed specifically to target and diagnose invasive breast cancer, but with broad applicability to many types of cancer. Citation Format: Ravi N. Singh. Tumor targeting and diagnostic applications of glycosylated nanotubes. [abstract]. In: Proceedings of the AACR Special Conference on Advances in Breast Cancer Research: Genetics, Biology, and Clinical Applications; Oct 3-6, 2013; San Diego, CA. Philadelphia (PA): AACR; Mol Cancer Res 2013;11(10 Suppl):Abstract nr B063.