Chapter 1. Discovery and Development of Sunitinib (SU11248): A Multitarget Tyrosine Kinase Inhibitor of Tumor Growth, Survival, and Angiogenesis

  1. Rongshi Li and
  2. Jeffrey A. Stafford
  1. Connie L. Sun1,
  2. James G. Christensen2 and
  3. Gerald McMahon1

Published Online: 28 SEP 2009

DOI: 10.1002/9780470524961.ch1

Kinase Inhibitor Drugs

Kinase Inhibitor Drugs

How to Cite

Sun, C. L., Christensen, J. G. and McMahon, G. (2009) Discovery and Development of Sunitinib (SU11248): A Multitarget Tyrosine Kinase Inhibitor of Tumor Growth, Survival, and Angiogenesis, in Kinase Inhibitor Drugs (eds R. Li and J. A. Stafford), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9780470524961.ch1

Editor Information

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

Author Information

  1. 1

    Poniard Pharmaceuticals, Inc., South San Francisco, CA 94080, USA

  2. 2

    Pfizer Global Research and Development, La Jolla, 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

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Keywords:

  • multitarget tyrosine kinase inhibitor of tumor growth, survival, and angiogenesis;
  • Sunitinib (SU11248, Sutent™; Pfizer Inc) - oral, multitargeted tyrosine kinase inhibitor of VEGF receptors;
  • SU 11248 in vitro protein kinase target profile

Summary

This chapter contains sections titled:

  • Sunitinib

  • Receptor Tyrosine Kinase Signaling Affects Multiple and Diverse Cancer Processes

  • Role of Receptor Tyrosine Kinases in Pathologic Tumor Angiogenesis

  • SU 5416: Discovery of First-Generation VEGFR RTK Inhibitors

  • SU 6668: Inhibitor of PDGFR and VEGFR Tyrosine Kinases

  • Design, Discovery, and Development Rationale for SU 11248

  • SU 11248 in vitro Protein Kinase Target Profile

  • Simultaneous Inhibition of VEGFR, PDGFR, and KIT (SCFR) RTKs Established a Unique Mechanism of Action for SU 11248

  • SU 11248 PKPD Studies Established the Optimal Dosing Parameters

  • SU 11248 Nonclinical Studies Supported Clinical Strategy and Tumor Indication Selection

  • SU 11248: Translational Studies Provided a Drug Registration Path

  • Summary

  • Acknowledgments

  • References