The widespread popularity of olive oil is attributable not only to its sensory characteristics and organoleptic properties, but also to its significant health benefits, primarily due to its high content of monounsaturated fatty acids and antioxidants, such as tyrosol and oleocanthal. The potential therapeutic effects of olive oil are supported by a wealth of in vitro, in vivo, and clinical studies. This chapter provides a comprehensive review of olive oil’s impact on various aspects of human health, including cardiometabolic health, inflammation, oxidation stress, and cancer. Furthermore, the authors discuss its potential effects on neurodegenerative diseases and gut microbiome modulation, while emphasizing the pharmacological and nutritional significance of bioactive constituents, such as polyphenols.