Hydroxytyrosol is a phenolic phytochemical with antioxidant properties in vitro. It is a natural compound that can be found in olive leaves and oil. The main dietary source of hydroxytyrosol is extra virgin olive oil. Due to its bioavailability, chemical properties and easy formulation along with its lack of toxicity, hydroxytyrosol is considered an excellent food supplement by the nutraceutical and food industries. The purpose of this review is to discuss the potential therapeutic effects of hydroxytyrosol in vivo. To do so, we conducted an electronic search in PubMed and other literature databases using “hydroxytyrosol”, “beneficial effect/s”, “pharmacology” as key-words. From this search, we found that hydroxytyrosol has anti-inflammatory, anti-tumor, antiviral, antibacterial and antifungal properties. Hydroxytyrosol also improves endothelial dysfunction, decreases oxidative stress, and is neuro- and cardio-protective. Due to all these biological properties, hydroxytyrosol is currently the most actively investigated natural phenol. The evidence presented in this review suggests that hydroxytyrosol has great pharmacological potential.