Everolimus (Afinitor)

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General information

Class/mechanism: mTOR kinase inhibitor; mTOR (mammalian target of rapamycin) is a serine-threonine kinase downstream of the PI3K/AKT pathway. In vitro, everolimus has been found to reduce cell proliferation, angiogenesis, and glucose uptake. Everolimus forms inhibitory complexes with mTORC1 by binding to the intracellular protein FKBP-12. Reduces activity of downstream effectors of mTOR that are involved in protein synthesis, S6 ribosomal protein kinase (S6K1) and eukaryotic elongation factor 4E binding protein (4E-BP1). Reduces expression of vascular endothelial growth factor (VEGF) and hypoxia-inducible factor (HIF-1).[1][2][3]
Route: PO
Extravasation: n/a

  • Anecdotally, taking the pill in a small amount of whipped/sour cream[4] or putting the pill in a marshmallow[5] may decrease the likelihood of developing stomatitis/mucositis.

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.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Also known as

  • Code names: RAD001, RAD-001
  • Brand names: Advacan, Afinitor, Afinitor Disperz, Certican, Everecan, EverGraf, Evermil, Evertor, Rapact, Rolimus, Votubia, Zortress

References

  1. 1.0 1.1 1.2 Everolimus (Afinitor) package insert
  2. Everolimus (Afinitor) package insert (locally hosted backup)
  3. Afinitor manufacturer's website
  4. Discussion between Sara Hurvitz, MD and Neil Love, MD, 2012
  5. Simeon Bennett, Novartis’ Afinitor gets OK of FDA, Bloomberg News (July 29, 2012). Retrieved 9/11/2012.
  6. Everolimus (Afinitor) patient drug information (Chemocare)
  7. Everolimus (Afinitor) patient drug information (UpToDate)