Cryptolepis buchananii R.Br. ex Roem. & Schult., a woody climber belonging to the family Apocynaceae, is increasing scientific attention for its rich ethnomedicinal properties and broad-spectrum pharmacological activities. The plant has been extensively used to treat skin disorders, fever, inflammation, rickets, and blood impurities. Recent phytochemical investigations have led to the isolation of several bioactive compounds, including alkaloids, glycosides, and a novel proteolytic enzyme named cryptolepain. Pharmacological studies have demonstrated significant antiinflammatory, analgesic, chondroprotective, antioxidant, and hypoglycemic activities. Botanical description of the plant with local names, bioactive compounds and pharmacological properties are described in detail.