2. ADME Strategies in Lead Optimization

  1. Mitchell N. Cayen
  1. Amin A. Nomeir

Published Online: 3 AUG 2010

DOI: 10.1002/9780470613191.ch2

Early Drug Development

Early Drug Development

How to Cite

Nomeir, A. A. (2010) ADME Strategies in Lead Optimization, in Early Drug Development (ed M. N. Cayen), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9780470613191.ch2

Editor Information

  1. Cayen Pharmaceutical Consulting, LLC, Bedminster, New Jersey, USA

Author Information

  1. Schering-Plough Research Institute, Kenilworth, New Jersey, USA

Publication History

  1. Published Online: 3 AUG 2010
  2. Published Print: 23 JUL 2010

ISBN Information

Print ISBN: 9780470170861

Online ISBN: 9780470613191



  • absorption, distribution, metabolism, and excretion (ADME) strategies in lead optimization;
  • metabolism (biotransformation) - most important of ADME variables affecting totality of oral bioavailability;
  • in silico ADME screening


This chapter contains sections titled:

  • Introduction

  • Absorption

  • Distribution

  • Metabolism

  • Excretion

  • Pharmacokinetics

  • Prioritizing ADME Screens

  • In Silico ADME Screening

  • The Promise of Metabolomics

  • Conclusions

  • References