Displacement of Drugs from Human Serum Albumin: From Molecular Interactions to Clinical Significance

Background: Human serum albumin (HSA) is the most abundant protein in human serum. It has numerous functions, one of which is transport of small hydrophobic molecules, including drugs, toxins, nutrients, hormones and metabolites. HSA has the ability to interact with a wide variety of structurally different compounds. This promiscuous, nonspecific affinity can lead to sudden changes in concentrations caused by displacement, when two or more compounds compete for binding to the same molecular site. Keywords: Human serum albumin, drug displacement, pharmacokinetic interactions, free concentration, drug design, Sudlow’s site I, Sudlow’s site II.