Chapter 7. Structure-Based Design and Characterization of Axitinib

  1. Rongshi Li and
  2. Jeffrey A. Stafford
  1. Robert S. Kania

Published Online: 28 SEP 2009

DOI: 10.1002/9780470524961.ch7

Kinase Inhibitor Drugs

Kinase Inhibitor Drugs

How to Cite

Kania, R. S. (2009) Structure-Based Design and Characterization of Axitinib, in Kinase Inhibitor Drugs (eds R. Li and J. A. Stafford), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9780470524961.ch7

Editor Information

  1. Takeda San Diego, Inc., San Diego, CA 92121, USA

Author Information

  1. Pfizer Global Research and Development, San Diego, CA 92121, USA

Publication History

  1. Published Online: 28 SEP 2009
  2. Published Print: 2 OCT 2009

Book Series:

  1. Wiley Series in Drug Discovery and Development

Book Series Editors:

  1. Binghe Wang

ISBN Information

Print ISBN: 9780470278291

Online ISBN: 9780470524961



  • structure-based design and axitinib characterization;
  • indazole series discovery;
  • deep-pocket binders - amide functional group addition


This chapter contains sections titled:

  • Introduction

  • Project Underpinning

  • Lead Selection: Structures of HITS and of Proteins

  • Discovery of the Indazole Series

  • Targeting the DFG-Out Conformation

  • Extended 6-Linker Indazoles: Capturing all Efficient Interactions

  • Deep-Pocket Binders: Addition of an Amide Functional Group

  • Refinement and Characterization of the Deep-Pocket Binder Axitinib

  • Preclinical and Clinical Development of Axitinib

  • Summary

  • Acknowledgments

  • References