A New Approach to Early ADME CYP450 Inhibition Profiling Using the Echo Liquid Handler
Jing Wang, Applications Scientist
Date and Time:
Tuesday, Oct 30, 2012
10 AM PDT/ 1 PM EDT/ 5 PM GMT
The high cost of drug discovery and the frequent failure of compounds due to poor ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) properties necessitate an earlier study of ADMET profiles. Efficient early profile determination is an expensive process unless the process is miniaturized, and the cost per data point is reduced. The CYP450 inhibition assay is one of the most important ADMET assays which identifies drug candidates that may have undesirable drug-drug interactions or sub-optimal pharmacokinetic properties. Here, we present two miniaturized, simplified and automated methods using the Echo® liquid handler to evaluate CYP450 inhibition and time-dependent inhibition potential. When utilized in tandem with an integrated microplate reader or with RapidFire/MS, the new methods generate high quality IC50 data while reducing reagent costs by up to 90%.
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