A particular field of analytical chemistry applied to forensic toxicology is represented by the anti-doping analysis, where biological samples (urine and in some instances blood) collected, either "in competition" or "out of competition", from athletes ruled for national/international sport federations, are analyzed to detect the putative use of prohibited substances and methods. Together with the official anti-doping activity to test the athletes (i.e. who engages in competitive sport) for the non-physiological enhancement of sport performance, it is mandatory to activate a new strategy of doping control, that should necessarily comprise a deep and exhaustive toxicological evaluation of the entire spectrum of doping substances and methods. An outline of the present status and of the future trends of the antidoping research is here presented, showing that most of the new tasks could greatly benefit from an approach based on in vitro methods, ranging from specific toxicity studies to the possible detection of new forms of doping.