The following paper sets out to analyse how the term ‘performance enhancement’ comes to be understood and utilised as a concept within discussions surrounding anti-doping in sport. At the most explicit level – that of discussing how we come to regulate drug use in sport – it is argued that performance enhancement is framed either as part of sport, the antithesis of sport, or an issue of health management. By contrast, it is suggested that it should not be assumed that performance enhancing drugs are necessarily efficacious. At a deeper analytical level it is argued that our regulatory understandings of performance enhancement are shaped by underlying tensions with respect to the significance of health and technology as elements of sport. By way of discussion and conclusion, it is argued that current social thinking on the issue of performance enhancement is contradictory with respect to values and practices. It is suggested that this contradiction stems from the overwhelming focus on performance enhancement as a form of drug abuse.