Optimization of ADMET properties for lead structures and drug candidates by using state-of-the-art medium and high through-put in vitro DMPK and genotoxicological Assays.
We play a central role in multidisciplinary drug discovery projects by giving guidance of the chemical optimization through rapid learning cycles in a multidimensional space. We offer data fast, reliable and of highest quality and provide scientific support by explanation of results and the suggestion of appropriate screening strategies to overcome ADMET liabilities.
Our in vitro compound profiling services include state-of-the-art assays for in vitro metabolic stability (liver microsomes and hepatocytes), permeability and transporters, in vitro plasma protein binding, CYP inhibition (reversible and irreversible) and induction, phenotyping of drug metabolizing enzymes (I.e. CYPs, UGTs) as well as genotoxicity assays as non-GLP AMES and in vitro Micronucleus assay.
We have a strong understanding of interpretation of these data in the specific project context and how to identify early and overcome DMPK related development risks, such as: absorption risks by using permeability assays, insufficient exposure using metabolic stability assays, prediction of drug-drug interaction (DDI) potential by inhibition and induction studies of CYP P450 enzymes as perpetrator and victim as well as risks associated with formations of reactive metabolite species or disproportionate drug metabolites performing in vitro metabolite ID studies.