Picralima nitida Durand and Hook, (fam. Apocynaceae) is a West African plant with varied applications in African folk medicine. Various parts of the plant have been employed ethnomedicinally as remedy for fever, hypertension, jaundice, dysmenorrheal, gastrointestinal disorders and malaria. In order to reveal its full pharmacological and therapeutic potentials, the present review focuses on the current medicinal uses, phytochemistry, pharmacological and toxicological activities of this species. Literature survey on scientific joals, books as well as electronic sources have shown the isolation of alkaloids, tannins, polyphenols and steroids from different parts of the plant, pharmacological studies revealed that the extract or isolated compounds from this species posses analgesic, anti-inflammatory, hypoglyceamic, hypotensive, antiplasmodial, antimicrobial, antiulcer and antitumorigenic activities. Results from various scientific investigations to date have revealed the potential of the extract from the plant or isolated compounds for use in the treatment and prevention of various kinds of human diseases. However, further studies on the extracts and pure compounds from this species is required to completely assess its phytochemical, pharmacological and toxicological profile as well as the mechanism of action behind these pharmacological activities exhibited by the compounds isolated from this species.