Mediterranean countries have lower rates of mortality from cardiovascular disease and cancer than Northern European or other Western countries. This has been attributed, at least in part, to the so-called Mediterranean diet, which is composed of specific local foods, including olive oil. Traditionally, many beneficial properties associated with this oil have been ascribed to its high oleic acid content. Today, it is clear that many of the beneficial effects of ingesting virgin olive oil are due to its minor compounds. This review summarizes the existing knowledge concerning the chemistry, pharmacokinetics, and toxicology of hydroxytyrosol, a minor compound of virgin olive oil, as well as this compound's importance for health. The main findings in terms of its beneficial effects in cardiovascular disease and cancer, including its properties against inflammation and platelet aggregation, are emphasized. New evidence and strategies regarding the use of hydroxytyrosol as a natural drug for the prevention and treatment of diseases with high incidences in Western countries are also presented.