Medicinal plants are indispensable source of therapeutic agents, and have proved to be “warehouse” of lead drug candidates. Lecaniodiscus cupanioides Planch. ex Benth is a medicinal tree plant that is extensively distributed in both Asia and Africa. The species has many ethnomedicinal uses in the treatment of fever, cough, typhoid, wound, skin infection, measles, jaundice, diabetes, sexual dysfunction, cancer, bone fracture, and as galactogogues. In the recent decades, the extracts and phytochemicals of L. cupanioides have been investigated to possess antibacterial, anticancer, aphrodisiac, antifungal, cytotoxic, antidiabetic, antiprotozoal, antioxidant, antidiarrhoeal, analgesic and ameliorative properties. However, triterpenoids which have been linked to its anticancer and antifungal actions, are the only isolated active constituents identified from the species despite the results of the phytochemical screenings and reported biological activities. Moreover, the mechanisms of action of the extracts and active components are yet to be fully elucidated. This paper provides a general review on the ethnomedicinal, phytochemicals, and biological activities of L. cupanioides, and lays a solid foundation for future investigations on the plant.