Vandetanib (Caprelsa)

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General information

Class/mechanism: from the NCI Drug Dictionary: "An orally bioavailable 4-anilinoquinazoline. Vandetanib selectively inhibits the tyrosine kinase activity of vascular endothelial growth factor receptor 2 (VEGFR2), thereby blocking VEGF-stimulated endothelial cell proliferation and migration and reducing tumor vessel permeability. This agent also blocks the tyrosine kinase activity of epidermal growth factor receptor (EGFR), a receptor tyrosine kinase that mediates tumor cell proliferation and migration and angiogenesis." Also a tyrosine kinase inhibitor of RET (rearranged during transfection), BRK (breast tumor kinase/protein tyrosine kinase 6), TIE2, EPH, Src. Inhibits angiogenesis, endothelial cell migration, and tumor growth.[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, 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, or the prescribing information.[1]

Toxicity management

Diseases for which it is established (work in progress)

Diseases for which it is used

Patient drug information

History of changes in FDA indication

  • 2011-04-06: Initial approval for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. (Based on ZETA)

History of changes in EMA indication

  • 2012-02-16: Initial marketing authorization as Caprelsa.

History of changes in Health Canada indication

  • 2012-01-12: Initial notice of compliance

History of changes in PMDA indication

Also known as

  • Code names: AZD-6474
  • Brand names: Caprelsa, Lucivand, Zactima