Plasma protein binding is a drug property that is determinant of both drug elimination and drug pharmacological activity.

It is the unbound drug that distributes to the site of action and the unbound drug is the form of drug that is subject to metabolism or elimination. 

• Binding in plasma 
• Binding in liver microsomes
• Binding in hepatocytes 
• Binding in brain and other tissues of interest 
• Blood-to-plasma concentration ratio

Additional Services: 

• We also evaluate binding in liver microsomes and hepatocytes. The fraction unbound (fu) is used to calculate Ki,u and CL_int,u values. 
• For CNS compounds, Kp,uu values can be determined by conducting in vivo study together with in vitro evaluation of the binding to brain homogenate. 

Plasma protein binding and binding in liver microsomes (or other tissues) will be determined using equilibrium dialysis, ultracentrifugation or ultrafiltration techniques depending on the physicochemical property of the test compound. Binding in hepatocytes is typically conducted using ultracentrifugation with deactivated cells. 

Discover the following In Vitro services at Frontage

Metabolite Profiling and Identification

A key in supporting the development of your drug candidate.

Kinetics & Metabolic Stability

Evaluating pharmacokinetic parameters is essential for determining drug dosing and frequency.

Drug-Drug Interaction

Drug-drug interaction and evaluation is an important undertaking in drug development.

Permability and Transporters

Comprehensive transporter services to support projects from discovery to development.

Protein Binding and Blood Cell Partitioning

A determinant of both drug elimination and drug pharmacological activity.