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

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