The advent of cancer nanomedicine has forged new pathways for the enhanced imaging and treatment of a broad range of cancers using new classes of materials. Among the many platforms being developed for drug delivery and imaging, nanodiamonds (NDs) possess several important attributes that may be beneficial toward improving the efficacy and safety of cancer nanomedicine applications. These include the uniquely faceted surfaces of the ND particles that result in electrostatic properties that mediate enhanced interactions with water and loaded therapeutic compounds, scalable processing and synthesis parameters, versatility as platform carriers, and a spectrum of other characteristics. In addition, comprehensive in vitro and in vivo studies have demonstrated that NDs are well tolerated. This chapter will examine several recent studies that have harnessed the ND agent as a foundation for both systemic and localized drug delivery, as well as the marked improvements in magnetic resonance imaging efficiency that has been observed following ND-contrast agent conjugation. In addition, insight into the important steps toward bringing the ND translational pathway to the clinic will be discussed.