The Opportunities of Metabolomics in Drug Safety Evaluation

Abstract

Although safety of drug candidates is carefully monitored in preclinical and clinical studies using a variety of approaches, drug toxicity may still occur in clinical practice. Therefore, novel approaches are needed to complement the current drug safety evaluation system. Metabolomics comprehensively analyzes the metabolites altered by drug exposure, which can therefore be used to profile drug metabolism, endobiotic metabolism, and drug-microbiota interactions. The information from metabolomic analysis can be used to determine the off-targets of a drug candidate, and thus provide a mechanistic understanding of drug toxicity. We herein discuss the opportunities of metabolomics in drug safety evaluation.

Keywords: Metabolomics; drug metabolites; drug safety evaluation; endobiotic metabolites.

Figure 1. The opportunities of metabolomics in drug safety evaluation

Metabolomics can systematically profile drug metabolism, endobiotic metabolism, and drug-microbiota interactions. The information from metabolomic analysis can be used to illustrate drug targets and provide a mechanistic understanding of drug toxicity. The following analyses are recommended for use of metabolomics in drug safety evaluation: (1) metabolomic analysis of blood, urine, and feces from preclinical to clinical studies; and (2) metabolomic analysis of major organs in preclinical studies.