Plasma Protein Binding



Sekisui XenoTech's Discovery Plus™ Protein Binding service allows you to understand the binding properties of your drug early in the discovery process. Binding of a compound to plasma proteins can potentially affect the pharmacokinetics, efficacy and toxicity of a drug. This is because only the free unbound form of the drug is available in the body to exert its pharmacological effect, be biotransformed or be excreted. Generally, acidic drugs tend to bind strongly to serum albumin, whereas basic compounds also bind to α-acid glycoprotein (AGP) or lipoprotein. Evaluating the plasma protein binding potential of a drug is an essential component of the drug development process.

Discovery Plus™ Protein Binding Overview
  • Utilizes Rapid Equilibrium Dialysis methodology
  • Simultaneously evaluate batches of 6-8 compounds and a positive control at a single concentration
  • Up to six different species of plasma at a single concentration
  • Duplicate determinations
  • Positive control included upon request
  • LC-MS/MS analysis
  • Tabular data summary typically provided within 10 business days or method development

Discovery Plus™ Protein Binding Results
A tabular summary of the following will be provided:
  • % Fraction Unbound (fu)
  • % Recovery (Mass Balance)
  • % Remaining (Plasma Stability)
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Metabolic Stability
CYP Inhibition
Enzyme Induction
Drug Transporter Inhibition
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