Cancer nanotechnology, defi n ed as nanotechnology applicable for diagnosis, prognosis, and therapy of cancer, offers exciting possibilities but also challenges. Although nanotechnology became fruitful in the fi eld of diagnostics, to date the desire of improving current cancer treatments through nanotechnology has surpassed the research or development stage only in a handful of cases. However, efforts to clinically translate more of these treatments remain highly focused. Drug-bearing nanoparticles, which are usually injected directly into the bloodstream, are sent on a journey full of obstacles to overcome such as bypassing RES organs and crossing endothelial cells, as well as various membranes of cellular and extracellular compartments, before fi nally encountering tumor tissue. Therefore, a cornucopia of different nanoparticle designs varying in size, architecture, and surface properties has been designed to be deployed to tumor sites within the human body either passively or promoting the association with a particular cell or tissue type through targeting. Early clinical results with nanomedicines were indeed able to show reduced toxicity, improving patients' quality of life, but are still in need of stronger coupling with superior clinical effi cacy to help justify the often high costs associated with this new class of therapeutics and their complexity. Nanotechnology aiming for the development of novel cancer therapeutics must focus in on potential, unforeseen toxicities and also consider the emerging role of epigenetics. The following chapter introduces most of the basic nanoconstructs developed to date, which inevitably will continue to evolve and eventually fi nd an important place in health care, though to become the cancer medicines of tomorrow, nanotechnology's future success and translation must early on be connected to diagnostic and therapeutic potential for clinical applications. To be equally aware of potential benefi ts, risks and costs will be necessary to stimulate future research with emphases on how to improve therapeutic outcomes such as the extension of life in patients with cancer in times burdened with unsustainable healthcare costs.