Chapter 2. Tykerb Discovery: A Dual EGFR and ERBB2 Tyrosine Kinase Inhibitor

  1. Rongshi Li and
  2. Jeffrey A. Stafford
  1. Karen Lackey1 and
  2. G. Stuart Cockerill2

Published Online: 28 SEP 2009

DOI: 10.1002/9780470524961.ch2

Kinase Inhibitor Drugs

Kinase Inhibitor Drugs

How to Cite

Lackey, K. and Cockerill, G. S. (2009) Tykerb Discovery: A Dual EGFR and ERBB2 Tyrosine Kinase Inhibitor, in Kinase Inhibitor Drugs (eds R. Li and J. A. Stafford), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9780470524961.ch2

Editor Information

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

Author Information

  1. 1

    Molecular Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709, USA

  2. 2

    Arrow Therapeutics, London SE1 1DB, United Kingdom

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



  • Tykerb discovery - dual EGFR and erbB2 tyrosine kinase inhibitor;
  • inhibiting erbB2 and EGFR tyrosine kinase activity;
  • drug candidate selection


This chapter contains sections titled:

  • Introduction

  • Early Efforts Established the Feasibility of Inhibiting ERBB2 and EGFR Tyrosine Kinase Activity as a Drug Intervention Approach

  • Lead Optimization Efforts Produced Two Drug Candidates with the Desired Mechanism of Action: GW 2974 and GW 0277

  • Data Reanalysis and Mix-and-Match Strategy Lead to Tykerb

  • Drug Candidate Selection

  • References