A plethora of ethnotherapeutic properties and pharmacological actions have been attributed to Sclerocarya birrea (family: Anacardiaceae). It is one of the most highly valued indigenous trees of southern Africa. Reports in biomedical literature have indicated the presence of medicinally-important chemical constituents in the plant, notably: polyphenols, tannins, coumarins, flavonoids, triterpenoids, phytosterols, and so forth. Pharmacological studies by various groups of investigators have shown that S. birrea possesses antidiarrhoeal, antidiabetic, anti-inflammatory, antimicrobial, antiplasmodial, antihypertensive, anticonvulsant, antinociceptive and antioxidant properties, thus lending pharmacological support to the plant's folkloric, ethnotherapeutic uses in South African traditional medicine. In view of the immense medicinal importance of the plant, this review aimed at compiling all currently available information on S. birrea's chemical constituents, as well as its ethnomedicinal, pharmacological and toxicological properties.