Ehretia cymosa Thonn. is a deciduous medium-sized to large tree which occurs naturally from Sierra Leone in West Africa to Eritrea and Kenya in East Africa, and Zimbabwe in southern Africa. This study aims to provide a comprehensive review of medicinal uses, phytochemistry and biological activities of E. cymosa. This review examines the existing literature on the medicinal uses, phytochemistry and biological activities of E. cymosa. This study revealed that the bark, leaf juice, leaves, roots, seeds, stems, twigs and whole plant parts of E. cymosa are mainly used as aphrodisiac, laxative and ethnoveterinary medicines and as traditional medicines for gastro-intestinal problems, wounds, malaria, fever, typhoid, convulsions, epilepsy, toothache and respiratory infections. Phytochemical research revealed that the species is characterized by alkaloids, anthraquinones, essential oils, fatty acids, flavonoids, glycosides, phenolics, proanthocyanidins, pseudotannins, reducing sugars, saponins, steroids, tannins and terpenes. Ethnopharmacological research revealed that the extracts of E. cymosa and phytochemical compounds isolated from the species showed antibacterial, antidiabetic, antihyperglycaemic and antioxidant activities. Ehretia cymosa should be subjected to detailed phytochemical, pharmacological and toxicological evaluations aimed at correlating its medicinal uses with its phytochemistry and pharmacological properties.