The binding to human serum albumin of two anti-inflammatory drugs, indomethacin and indoprofen, has been studied by chromatographic and spectroscopic techniques. The results shown indicate that the binding of both drugs--but more notably of indoprofen--is very sensitive to variations of the environmental conditions. The binding is also dependent upon limited modifications in the tertiary structure of the protein. The evidences shown tend to indicate that these two phenomena are related, and that the binding is permitted under conditions of a relatively open structure of the protein molecule.