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Fractional Mass Filtering as a Means to Assess Circulating Metabolites in Early Human Clinical Studies by Philip R. Tiller; Sean Yu; Kevin P. Bateman; Jose Castro‐Perez; Ian S. Mcintosh; Yushin Kuo; Thomas A. Baillie is a Chemistry article available to read on EtoBox.

## Abstract Recent changes in the regulatory environment have led to a need for new methods to assess circulating human drug metabolites in early clinical studies with respect to their potential toxicological impact. The specific goals of such studies are to determine if the metabolites present in human plasma following administration of a drug candidate also are observed in plasma from the animal studies employed for preclinical toxicological evaluation, and to estimate corresponding exposure margins (animal:human) for the major metabolites. Until recently, the accepted best practice for the characterization of circulating drug metabolites utilized liquid chromatography/tandem mass spectrometry (LC/MS/MS)‐based methodologies, in conjunction with authentic chemical standards, for the detection and quantitative analyses of metabolites predicted from both animal studies and experiments with human liver preparations __in vitro__. While this approach is satisfactory for anticipated biotransformation products, metabolites that were not expected to circulate in human plasma frequently escape detection. Current accurate mass instruments enable the use of the technique of fractional mass f

Author

Philip R. Tiller; Sean Yu; Kevin P. Bateman; Jose Castro‐Perez; Ian S. Mcintosh; Yushin Kuo; Thomas A. Baillie

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0951-4198)

Published

2008

Language

EN

Field

Chemistry (Physical Sciences)