Validation of an integrated series of ligand-binding assays for the quantitative determination of antibody-drug conjugates in biological matrices

Bioanalysis. 2016 Mar;8(6):519-31. doi: 10.4155/bio.16.13. Epub 2016 Feb 26.

Abstract

Background: The bioanalytical strategy for antibody-drug conjugates (ADC) includes multiple integrated measurements of pharmacologically relevant ADC.

Methods & results: Three ligand-binding assays were validated for the measurement of total antibody, active ADC and total ADC. Accuracy and precision demonstrate %bias from -8 to 14%, %CV from 3 to 11% and total error from 3 to 21%, with >98% samples meeting incurred sample reanalysis criteria. Each assay met stability, selectivity, dilutional integrity, carry over and specificity criteria with no interference from associated metabolite/impurity. Given the active ADC assay sensitivity to payload, active ADC was used to assess drug to antibody ratio.

Discussion & conclusion: Implementation of a microfluidic automated platform enabled high throughput sample analysis of multiple analytes with minimal sample processing.

Keywords: antibody–drug conjugate; drug antibody ratio; ligand-binding assays; payload; selectivity; specificity; total antibody.

Publication types

  • Validation Study

MeSH terms

  • Antibodies, Monoclonal / chemistry
  • Half-Life
  • Immunoassay* / standards
  • Immunoconjugates / analysis*
  • Immunoconjugates / pharmacokinetics
  • Lignans
  • Pharmaceutical Preparations / chemistry
  • Quality Control

Substances

  • Antibodies, Monoclonal
  • Immunoconjugates
  • Lignans
  • Pharmaceutical Preparations