Carob tree (Ceratonia siliqua L.) is one of the most widespread medicinal plants in the Mediterranean area. Traditionally, it was cultivated for its ethnopharmacological benefits and, more especially, for the seeds, which served as unit of measurement of jewelers "carat." Hence, in the last half-century, numerous studies reported a wide range of phytoconstituents contained in all parts of Ceratonia siliqua such as phenolic compounds, flavonoids, tannins, anthocyanins, alkaloids, glycosides, proteins and minerals. This review article unveils the phytochemical constituents, bioactivity and pharmacological studies of Ceratonia siliqua. Recent studies have shown that the extracts of this plant exhibit an antioxidant, antidiarrheal, antibacterial, antifungal, anti-inflammatory, antidiabetic activities and also hepatoprotective and antiproliferative effects. In this review, we provide a summary of the most interesting data related to bioactivity and therapeutic potential of Ceratonia siliqua in a way to suggest possible future studies that may use Ceratonia siliqua as an undeniable natural alternative for neurodegenerative diseases treatment.