Selection of the first-time dose in humans: comparison of different approaches based on interspecies scaling of clearance

J Clin Pharmacol. 2003 Jul;43(7):692-7.

Abstract

The authors describe four approaches to selecting a safe starting dose for humans in clinical drug trials based on interspecies scaling of clearance. Human clearance was predicted by scaling for 10 example drugs for which animal clearance values were available in the literature. The predicted human clearance values were then used to select the estimated starting dose in humans. These doses were then compared with the actual doses given to humans during clinical trials. All four approaches used to estimate the first-time dose in humans provided values that were within the dose range given to humans from Phases I to III. This work demonstrates that animal pharmacokinetic data can be used to estimate a suitable human starting dose, provided the data have been obtained from a dose that produces no adverse effects.

Publication types

  • Comparative Study

MeSH terms

  • Algorithms
  • Animals
  • Body Weight
  • Clinical Trials as Topic
  • Dose-Response Relationship, Drug
  • Drugs, Investigational / administration & dosage*
  • Drugs, Investigational / adverse effects
  • Drugs, Investigational / pharmacokinetics*
  • Humans
  • Metabolic Clearance Rate
  • Organ Size
  • Species Specificity

Substances

  • Drugs, Investigational