In vitro-in vivo correlation for low-clearance compounds using hepatocyte relay method

Drug Metab Dispos. 2013 Dec;41(12):2018-23. doi: 10.1124/dmd.113.053322. Epub 2013 Jul 15.

Abstract

In vitro-in vivo correlation (IVIVC) of intrinsic clearance in preclinical species of rat and dog was established using the hepatocyte relay method to support high-confidence prediction of human pharmacokinetics for low-clearance compounds. Good IVIVC of intrinsic clearance was observed for most of the compounds, with predicted values within 2-fold of the observed values. The exceptions involved transporter-mediated uptake clearance or metabolizing enzymes with extensive extrahepatic contribution. This is the first assay available to address low clearance challenges in preclinical species for IVIVC in drug discovery. It extends the utility of the hepatocyte relay method in addressing low clearance issues.

MeSH terms

  • Animals
  • Dogs
  • Drug Discovery / methods
  • Drug Evaluation, Preclinical
  • Hepatocytes / metabolism*
  • Male
  • Membrane Transport Proteins / metabolism
  • Metabolic Clearance Rate / drug effects*
  • Rats
  • Rats, Wistar

Substances

  • Membrane Transport Proteins