Determination of the Plasma Protein Binding of Liraglutide Using the EScalate* Equilibrium Shift Assay
A Sovicell White Paper
Evaluation of the Accuracy of the EScalate Assay:
The research shows that robust and precise determination of plasma protein binding, even for compounds that cannot be analyzed with standard assays is enabled with the novel EScalate assay.
The plasma protein binding capability of drug substances represents an important assay parameter in drug discovery and development. For very strong plasma protein binding molecules, however, the free fraction in plasma fu is very small and therefore difficult to determine with standard methods. To solve this problem, the EScalate equilibrium shift in vitro assay was developed.
The EScalate assay enables the robust and accurate determination of plasma protein binding, even for compounds that cannot be analyzed with standard assays such as equilibrium dialysis or ultrafiltration. This was shown by the example of liraglutide, a fatty acid-conjugated peptide with high affinity to serum albumin and 4 small molecules some of which exhibit strong plasma binding and significant non-specific adhesion.
The ability to handle various compound classes such as peptides, small molecules, and stabilized oligonucleotides (not shown here) and to determine plasma protein binding in different model species is making this assay a valuable tool for lead optimization and first-in-human dose estimation.
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