Velvet antler is one of the most important animal medicines, and has been used with a variety of functions, such as anti-fatigue, tissue repair and health promotion. In the past few years, the investigation on chemical compositions, bioactive components, and pharmacological effects has been performed, which demonstrates that velvet antlers could be used as an important health-promoting tonic with great nutritional and medicinal values. This review focuses on the recent advance in studying the bioactive components of velvet antlers.