ADME Properties Leading to Toxicity

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

The purpose of preclinical ADME, also referred to as early drug metabolism and pharmacokinetics (DMPK), is to reduce the risks and avoid spending valuable resources on molecules that have poor pharmacokinetic (PK) properties. This strategy allows drug discovery resources to be focused on fewer but higher-quality drug candidates. Since then, major technological advances have occurred in molecular biology and screening, which allow major aspects of ADME to be assessed earlier during the lead optimization stage. Bioavailability, tissue distribution, pharmacokinetics, metabolism, and toxicity are assessed typically in one rodent and one nonrodent species prior to administering a drug to a human to evaluate drug pharmacokinetics and exposure in a clinical trial. The progress of ADME profiling has decreased the proportion of drug candidates failing in clinical trials for ADME reasons and providing important early input into safety and toxicity prediction of drug candidates.

Original languageEnglish (US)
Title of host publicationDrug Discovery Toxicology
Subtitle of host publicationFrom Target Assessment to Translational Biomarkers
Publisherwiley
Pages82-92
Number of pages11
ISBN (Electronic)9781119053248
ISBN (Print)9781119053330
DOIs
StatePublished - Jan 1 2016
Externally publishedYes

Keywords

  • ADME optimization strategy
  • Drug discovery
  • Human transporters
  • In vitro experiments
  • Pharmacokinetic properties
  • Toxicity

ASJC Scopus subject areas

  • Medicine(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Chemistry(all)
  • Biochemistry, Genetics and Molecular Biology(all)

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