Access to metabolites is critical at every stage of the drug discovery process. During the research stage, structure elucidation of drug metabolites allows faster metabolic stability optimization and also provides an opportunity to identify unique analogues.
At the pre-clinical stage, biological profiling and toxicology studies of lead compound metabolites are critical to improve the quality of the pipeline and reduce attrition rates. Significantly, the FDA published a guidance on safety studies of metabolites in 2008. (Guidance for industry, Safety testing of drug metabolites, FDA, February 2008).