Cissampelos owariensis is a perennial climber widely used as traditional medicine throughout its distributional range in tropical Africa. This study was aimed at providing a critical review of the pharmacological properties, phytochemistry and medicinal uses of C. owariensis. Documented information on medicinal uses, phytochemical and pharmacological properties of C. owariensis was collected from several online sources such as Scopus, Google Scholar, PubMed, Science Direct and MEDLINE and pre-electronic sources such as book chapters, books, journal articles and scientific publications obtained from the University library. This study showed that the bark, leaves, leaf sap, rhizomes, roots, stems and whole plant parts of C. owariensis are widely used as diuretic, and traditional medicine for ulcers, skin diseases, menstrual problems, gastro-intestinal problems, pregnancy problems, scorpion sting and snakebite. Phytochemical compounds identified from the species include alkaloids, anthraquinones, cardiac glycosides, essential oils, fatty acids, flavonoids, phenols, saponins, steroids, tannins and triterpenoid. Pharmacological research revealed that C. owariensis extracts have antibacterial, anti-mycobacterial, antifungal, antidiarrheal, anti-diabetic, antioxidant, antiproliferative, anti-ulcer, insecticidal, nephroprotective, tocolytic and cytotoxicity activities. There is need for extensive toxicological evaluations of crude extracts and compounds isolated from the species since C. owariensis contains potentially toxic compounds. © RJPT All right reserved.