Actovegin® is a deproteinized serum extract of bovine origin, and in recent years it has been used widely in treating sport injuries with many anecdotal reports of success. However, the use of Actovegin® in sport medicine has caused a substantial amount of controversy, especially concerning its supposed oxygen-enhancing capacity and an anecdotal belief that its use can increase an athlete's performance. In 2009, a sports physician was arrested with this "performance-enhancing drug," while an editorial in a sports medicine journal strongly questioned the evidence base for using this drug for acute muscle injury. There is also a report that suggested that Actovegin® might have induced anaphylactic shock in a cyclist. In this review, we have systematically examined the current evidence on Actovegin®. Its mechanism of action, clinical evidence, legal status with sports governing bodies, and its potential role in sport injuries will be discussed.