Chapter 8. Road to PD0325901 and beyond: The MEK Inhibitor Quest

  1. Rongshi Li and
  2. Jeffrey A. Stafford
  1. Judith S. Sebolt-Leopold and
  2. Alexander J. Bridges

Published Online: 28 SEP 2009

DOI: 10.1002/9780470524961.ch8

Kinase Inhibitor Drugs

Kinase Inhibitor Drugs

How to Cite

Sebolt-Leopold, J. S. and Bridges, A. J. (2009) Road to PD0325901 and beyond: The MEK Inhibitor Quest, in Kinase Inhibitor Drugs (eds R. Li and J. A. Stafford), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9780470524961.ch8

Editor Information

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

Author Information

  1. Oncovera Therapeutics, Inc., Ann Arbor, MI 48103, 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



  • RAS/RAF/MEK/ERK signaling module and dysregulated RAS signaling;
  • road to PD0325901 and beyond-MEK inhibitor quest;
  • CI-1040 and lessons learnt


This chapter contains sections titled:

  • Introduction

  • Genesis of the MEK Inhibitor Program at Parke-Davis

  • Role of PD 98059 in Teaching US the Importance of the MAP Kinase Pathway

  • Structure-Activity Relationship (SAR) Studies with PD 0045443

  • Lessons Learned from CI-1040

  • Evolution of PD 0325901

  • Clinical Trials of PD 0325901

  • Legacy of PD 0325901

  • Looking to the Future

  • Acknowledgments

  • Dedication

  • References