Recent developments in MS for the detection of small molecules in the context of doping control analysis are reviewed. Doping control analysis is evolving together with MS, which is the technique of choice in order to accomplish the analytical requirements in this field. Since these analytical requirements for the detection of a doping agent depend on the substance, in the first section we review the different scenarios. The commonly established approaches, together with their achievements and drawbacks are described. New developments in hyphenated MS techniques (both GC-MS/MS and LC-MS/MS) concerning interfaces and analyzers are mentioned. The use (or potential use) of these developments in order to minimize the limitations of the commonly established approaches in the doping control field is discussed. Finally, a brief discussion about trends and remaining limitations is presented.