Monoclonal antibodies: what are the pharmacokinetic and pharmacodynamic considerations for drug development?

Expert Opin Drug Metab Toxicol. 2012 Feb;8(2):141-60. doi: 10.1517/17425255.2012.643868. Epub 2012 Jan 17.

Abstract

Introduction: The number of monoclonal antibodies available for clinical use and under development has dramatically increased in the last 10 years. Understanding their pharmacokinetics and pharmacodynamics is essential for selecting the right clinical candidate, correct dose and regimen for a target indication.

Areas covered: This article reviews the existing literature and knowledge of monoclonal antibodies. Specifically, the authors discuss monoclonal antibodies with respect to their pharmacokinetics (including absorption, distribution and elimination) and their pharmacodynamics. The authors also look at the pharmacokinetic/pharmacodynamic relationship, scaling from preclinical to clinical studies and selection of the first-in-human dose.

Expert opinion: Monoclonal antibodies have complex pharmacokinetic and pharmacodynamic characteristics that are dependent on several factors. Therefore, it is important to improve our understanding of the pharmacokinetics and pharmacodynamics of monoclonal antibodies from a basic research standpoint. It is also equally important to apply mechanistic pharmacokinetic/pharmacodynamic models to interpret the experimental results and facilitate efforts to predict the safety and efficacy of monoclonal antibodies.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal / immunology
  • Antibodies, Monoclonal / pharmacokinetics*
  • Antibodies, Monoclonal / pharmacology*
  • Drug Discovery*
  • Humans

Substances

  • Antibodies, Monoclonal