An approach to estimating the levels of drug-related metabolites in human plasma in the absence of synthesized chemical standards has been developed. High-performance liquid chromatography/mass spectrometry (LC/MS) in combination with radiometric detection was used in this method. Biologically derived [(14)C] metabolites from preclinical in vitro and in vivo matrices are used as [(14)C] metabolite standards and their concentrations in matrices are calculated based on the corresponding radioactivity.
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