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2.3.4 Experimental Approaches for Assessing Reactive Metabolites

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The structural alerts for formation of RMs sometimes do not imply actual formation of RMs. In this circumstance, experimental evidence is needed to assess whether a drug candidate is bioactivated to RMs. We discuss some selected experimental approaches here, including covalent binding assay, electrophile trapping experiment and time‐dependent inactivation of CYP450.

Transporters and Drug-Metabolizing Enzymes in Drug Toxicity

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