Coordinated efforts of the States and sports organizations to eliminate doping in sport all over the world have formed a unique legal model that stands out for high uniformity in its implementation and enforcement despite differences in national regulations, and this legal model continues to evolve. Erosion of the principles of amateurism, growing governmental interest in sport, concerns about the health of athletes have affected the shape of the modern anti-doping legal system. This study analyzes the key historical stages in the development of anti-doping rules and regulations, as well as the prerequisites for the formation of its modern legal principles and methods. The study details the first anti-doping rules adopted by the Jockey Club at the beginning of the 20th century and describes the legal activities of the International Olympic Committee, States and intergovernmental organizations on creating anti-doping rules and legislation before the adoption of the UNESCO Convention in 2005. Special emphasis is placed on the explanation of ideological and political influence on the development of anti-doping rules and assessing the roles of the main actors in the antidoping system.