Poor absorption is an important cause of costly late-stage failures in functional food development, and therefore, it has become widely appreciated that pharmacokinetic parameters should be considered as early as possible in the functional food development process. In many cases, the molecular structure of bioactive ingredients is known, but information is lacking on how they interact with other food components, what their fate is upon consumption, what they do in the body and what their target site is. This information is of major importance, as the biological effects of food bioactive compounds (CBAs) are ultimately determined by their bioavailability and their temporal and spatial distribution in the body. In this chapter, we propose the phases to perform nutrikinetic studies of food CBAs from the simplest in vitro assays, applicable in early stages of the development of a functional food, to human intervention studies, which are required by the European Food Safety Authority and are aimed to establish the dose-exposure relationship (pharmacokinetic studies) and at last the exposure-response relationship (pharmacodynamic studies).