Using Human Serum Albumin Binding Affinities as a Proactive Strategy to Affect the Pharmacodynamics and Pharmacokinetics of Preclinical Drug Candidates.

We report on a new preclinical drug optimization strategy that measures drug candidates' binding affinity with human serum albumin (HSA) as an assessment of increasing or decreasing serum T. Three common scaffolds were used as drug prototypes. Common polar and nonpolar substituents attached to the scaffolds have been identified as opportunities for increasing or decreasing the HSA binding affinity.