Developments of fluorescence study on the combination of drugs with serum albumin are reviewed. Basic theory and experimental methods for the detection of binding site of drugs on protein, binding number, binding constant and the sort of binding forces are introduced. The iN_fluence of drugs on the structure of serum albumin and the iN_fluence of coexist ions on the combination reaction are discussed. Some experimental results of drugs reacting with serum albumin are listed in a table. Finally, problems existing in the study and the development trends of this area are briefly discussed.