Our Solutions to Various Issues:

• cell permeability in models such as Caco-2 cells, MDCK cells, human Blood Brain Barrier models, along with the study of efflux transporters possibly involved in the passage through these natural barriers
• plasma protein binding (Rapid Equilibrium Dialysis, ultrafiltration)
• transporter inhibition or induction using the P-gp drug interaction model or various cell-based models coupled with bioanalytical methods allowing to quantify gene expression (RT-qPCR), protein amount (MS2PLex) and biological activity. Certain studies are performed according to the FDA recommendations

• CYPs inhibition/induction/down-regulation in liver microsomes, primary hepatocytes or rec.hCYPs P450 marketed worldwide by Bertin Pharma (protein amount & activity)
• interspecies comparative metabolic profiling
• Drug-Drug Interactions (DDI)
• identification of P450 pathways & determination of kinetic parameters

• metabolomic approach for metabolism studies
• drug clearance, tissue stability on hepatocytes or subcellular fractions (microsomes, S9 fractions), intestinal cells, keratinocytes, fibroblasts & Peripheral blood mononuclear cells (PBMC)

Biotransformation Technology

For multifunctional/complex molecules, we also offer our Biotransformation Technology to produce Phase I & Phase II metabolites using micro organisms or genetically modified yeast over-expressing human CYP 450 .

Quick & Reliable Bioanalysis Methods

For Bioanalysis applied to in vitro ADME, the main challenges for Bioanalysis within in vitro ADME studies are:

• to have generic methods whose implementation is quick, applicable to the larger number of molecules while maintaining specificity, reliability & robustness without fully GLP compliance and;
• to have methods to measure the activities or quantify enzymes or transporters
• to master the determination and quantification of metabolites.