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Metabolic stability early drug metabolism screening

One of the early in vitro assays that is used as part of the new drug discovery paradigm is the metabolic stability assay. This assay is also referred to as the microsomal stability assay or the hepatocyte stability assay or sometimes simply the in vitro stability assay (Thompson, 2000, 2001 Xu et ah, 2002 Jenkins et ah, 2004 Baranczewski et ah, 2006). As these names suggest, there are various ways to perform the in-life part of the assay some departments prefer to screen with liver microsomes, while others find that hepatocytes provide more meaningful data (Lau et ah, 2002). Regardless of the in-life part of the in vitro stability assay, the analytical part represents a significant challenge because the analyst must have compound-specific methods in order to properly analyze the samples. [Pg.387]


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