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

  1. Rongshi Li,
  2. Jeffrey A. Stafford
  1. Connie L. Sun1,
  2. James G. Christensen2,
  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