Schisandra sphenanthera Rehd. et Wils (S. sphenanthera) is a single species of Schisandra genus, Magnoliaceae family, and it is a famous medicinal herb mostly growing in southern China, China Taiwan and Vietnam. S. sphenanthera is usually used for the treatments of hepatitis, Alzheimer’s disease, renal transplantation, osteoporosis, and insomnia. In present studies, approximately 310 natural constituents have been isolated from S. sphenanthera, including lignans, triterpenes, volatile oils, and polysaccharides, which were mainly obtained from the fruits and stems of S. sphenanthera. Pharmocological studies have shown that the extracts and monomeric compounds of S. sphenanthera possessed wide-range bioactivities, such as antitumor, anti-oxidant, anti-inflammatory, osteoblastic, immune regulation, neuroprotective, kidney protection, hepatoprotective, and antiviral activities. However, resource availability, quality control measures, in-depth in vivo pharmacological study, and clinical application are still insufficient and deserve further studies. This review systematically summarized literatures on the botany, phytochemistry, pharmacology, development utilization, and clinical application of S. sphenanthera, in hopes of provide a useful reference for researchers for further studies of this plant.