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As a drug discovery program progresses, it becomes more important to know the types of biotransformation and the information on the metabolic site(s) that the lead compounds are subject to, so that structures can be optimized to improve factors such as bioavailability and pharmacokinetics. In addition, some insight into the species specificity of metabolism may be obtained, providing a basis for the selection of preclinical toxicology species. Then, as compounds move from discovery to development, the need for even more detailed and precise metabolite data becomes increasingly important, both to understand the characteristics of the candidate drug in humans and to fulfill the regulatory requirements that will underpin a successful drug registration.