Berchemia zeyheri is a small-to-medium-sized deciduous fruit tree widely used as herbal medicine. This study was aimed at providing a critical review of the medicinal uses, phytochemistry, and biological activities of B. zeyheri. Documented information on the biological activities, medicinal uses, and phytochemistry of B. zeyheri was collected from several online sources which included BMC, Scopus, SciFinder, Google Scholar, ScienceDirect, Elsevier, PubMed, and Web of Science. Additional information on the biological activities, phytochemistry, and medicinal uses of B. zeyheri was gathered from pre-electronic sources such as book chapters, books, journal articles, and scientific publications obtained from the university library. This study showed that the bark and roots of B. zeyheri are used for magical purposes and as herbal medicine for anemia, backache, baby’s navel problems, cough, dysentery, headache, rectal ulcers, stomach problems, tonic, and vomiting and ethnoveterinary medicine for infectious diseases in cattle. Phytochemical analyses revealed that the aerial parts, bark, and heartwood of B. zeyheri are characterized by alkaloids, flavonoids, glycosides, polyphenols, and steroids. Pharmacological research revealed that B. zeyheri crude extracts have anthelmintic, antibacterial, antioxidant, and toxicity activities. Future ethnopharmacological research should focus on conducting detailed phytochemical, pharmacological, and toxicological studies.