The Role of Plasma Protein Binding in Drug Discovery

Understanding of the molecular properties that control binding is of fundamental importance in the drug discovery process. The extent of plasma protein binding of a candidate drug molecule has an influence on a number of critical areas listed below, and many of these areas will be reviewed in this article, i.e.: • determination of margins in safety assessment/toxicology studies • the efficacy of a drug • drug metabolism and pharmacokinetics • drug–drug interactions • blood–brain barrier penetration