Pithecellobium dulce, an evergreen medium-sized, spiny tree, each part of the plant has vast nutritional values; stuffed with essential vitamins, amino acids, and minerals. The fruits of P. dulce were widely used in Ayurvedic medicines and home remedies. The plant has also been a rich source of biologically active compounds such as tannin, olein, and glycosides. Totally 38 active phytocompounds like quercetin, kaempferol, and dulcitol were identified from the various parts of the plant. Notably, this plant has catechol type of tannins in the bark. There are polyphenol classes of phytocompounds which have found to hold potent antivenom activity. Their fruits are a rich source of phenols, flavonoids, and saponins reported for their efficacy to treat diabetes, oxidative stress, and gastrointestinal disorders. The plant leaf and seed have an antibacterial, antifungal, and adulticidal activities. Thus, the present review describes on exploiting the medicinal properties of P. dulce and its biomedicinal applications in therapeutic development.