A regulatory perspective on issues and approaches in characterizing human metabolites

Chem Res Toxicol. 2006 Dec;19(12):1561-3. doi: 10.1021/tx060203m.


This document captures the current thinking within FDA/CDER on the non-clinical safety assessment of human drug metabolites in new drug products. Examples are provided, which define a scientific based approach to the safety evaluation of human metabolites in new drug candidates. A discussion of the need for, and the adequacy of, the assessment of human drug metabolites with specific regard to their potential as mediators of toxicity is presented from a regulatory perspective.

MeSH terms

  • Animals
  • Drug Evaluation* / legislation & jurisprudence
  • Drug Evaluation* / methods
  • Drug Evaluation* / standards
  • Drug-Related Side Effects and Adverse Reactions / metabolism*
  • Government Regulation
  • Humans
  • Metabolic Detoxication, Phase I
  • Pharmaceutical Preparations / metabolism*
  • Safety
  • United States
  • United States Food and Drug Administration


  • Pharmaceutical Preparations