Class/mechanism: Tyrosine kinase inhibitor, inhibits multiple tyrosine kinases, including: vascular endothelial growth factor receptor (VEGFR1, VEGFR2 and VEGFR3), platelet-derived growth factor receptors (PDGFRα and PDGFRβ), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and RET. Inhibition of these kinases disrupts angiogenesis, tumor cell signaling, and induces apoptosis.
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.
Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 1/26/2006: Initial FDA approval for the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate.
- 5/20/2011: FDA approved for treatment of progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) in patients with unresectable locally advanced or metastatic disease. (New disease entity)
- 1/26/2006: Initial accelerated FDA approval for the treatment of advanced renal cell carcinoma.
- 2/2/2007: Granted regular approval for the treatment of advanced renal cell carcinoma. (Converted to regular approval)
- 11/16/2017: FDA approved for the adjuvant treatment of adult patients at high risk of recurrent renal cell carcinoma following nephrectomy. (Approval expanded to the adjuvant setting)
Also known as
- Code names: SU11248, SU011248
- Brand names: Suninat, Sutent