Warburgia salutaris (Bertol. F.) Chiov . Canellaceae, commonly referred to as the pepper-bark tree, holds significant cultural, medicinal, and economic value in Southern Africa. This review aims to provide an inclusive overview of the traditional uses, pharmacological activities and phytochemistry of W. salutaris in Southern Africa. The information on W. salutaris was collected for this review article by searching various scientific resources, including SciFinder, Google Scholar, Web of Science, Scopus, PubMed and Science Direct, and by using various keywords with no specific timeframe set to limit the search parameters. Indigenous communities have long revered this tree for its myriad of traditional uses in treating various ailments, including conditions such as abdominal pain, respiratory tract infections, malaria, febrile complaints, candidiasis, headache, tuberculosis, sexually transmitted diseases, sinus, and rheumatism. Various studies have reported W. salutaris as having significant antibacterial, antifungal, antimycobacterial, antimalarial and antioxidant activities as well as anti-inflammatory properties. Modern scientific research has shed light on its complex phytochemical composition and pharmacological properties, unveiling its potential therapeutic applications. W. salutaris extracts contain a collection of bioactive molecules such as sesquiterpenoids, drimane-type sesquiterpenes and other terpenoids, which warrant further in vivo efficacy studies to irrefutably validate observed in vitro pharmacological activities and ethnobotanical usage of this plant.