Discovery DMPK Support for Active Lead Optimization Programs for Large Pharma


  • To qualify as the preferred service provider in a head-to-head proficiency assessment as compared to other service providers.
  • To set up and validate the in-vitro CYP inhibition and protein binding assays to the Large Pharmas desired level of detail/requirement.


  • Eurofins Advinus developed and validated all the in vitro assays.
  • Confirmed assay validation using Sponsors blinded compounds, and followed a screening cascade for the program compounds. Tier 1: Solubility, Microsomal Metabolic Stability, Caco-2 Permeability
  • Tier 2: CYP Inhibition in HLM by LC-MS/MS, Plasma Protein Binding and Microsomal Binding
  • Tier 3: Bioavailability studies in rat and dog
  • Collaborated with Sponsor to devise a definitive PPB equilibrium dialysis assay using LC-MS/MS based quantification (Zamek- Gliszczynski MJ et al. Validation of 96-well equilibrium dialysis with non-radiolabeled drug for definitive measurement of protein binding and application to clinical development of highly-bound drugs. J. Pharm. Sci. 2011 Jun: 100(6):2498-507).
  • All shipping and project management processes were worked out.
  • Eurofins Advinus turned around data within 1 week of receiving compounds to enable sponsor to quickly decide on moving compound along the screening cascade.