Difference between revisions of "Everolimus (Afinitor)"

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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 [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert"></ref>  
 
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 [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert"></ref>  
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==History of changes in FDA indication==
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*3/30/2009: Initial FDA approval for the treatment of patients with advanced [[Renal cancer | renal cell carcinoma]] after failure of treatment with [[Sunitinib (Sutent) | sunitinib]] or [[Sorafenib (Nexavar) | sorafenib]].
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*10/29/2010: Approval expanded to include [[Central nervous system (CNS) cancer | subependymal giant cell astrocytoma (SEGA)]] associated with tuberous sclerosis (TS) who require therapeutic intervention but are not candidates for curative surgical resection.
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*5/5/2011: Approval expanded to include progressive [[Neuroendocrine tumors | neuroendocrine tumors of pancreatic origin (PNET)]] that is unresectable, locally advanced or metastatic.
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*4/26/2012: Approval expanded to include adults with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery.
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*7/20/2012: Approval expanded to include postmenopausal women with advanced hormone receptor-positive, [[Breast cancer | HER2-negative breast cancer (advanced HR+ BC)]] in combination with [[Exemestane (Aromasin) | exemestane]] after failure of treatment with [[Letrozole (Femara) | letrozole]] or [[Anastrozole (Arimidex) | anastrozole]].
  
 
==Patient drug information==
 
==Patient drug information==
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[[Category:Drug index]]
 
[[Category:Drug index]]
 
[[Category:Chemotherapy]]
 
[[Category:Chemotherapy]]
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[[Category:Kinase inhibitors]]
 
[[Category:Kinase inhibitors]]
 
[[Category:mTOR inhibitors]]
 
[[Category:mTOR inhibitors]]
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[[Category:Aggressive Non-Hodgkin lymphoma medications]]
 
[[Category:Aggressive Non-Hodgkin lymphoma medications]]
 
[[Category:Breast cancer medications]]
 
[[Category:Breast cancer medications]]
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[[Category:Central nervous system (CNS) cancer medications]]
 
[[Category:Hodgkin lymphoma medications]]
 
[[Category:Hodgkin lymphoma medications]]
 
[[Category:Mantle cell lymphoma medications]]
 
[[Category:Mantle cell lymphoma medications]]
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[[Category:Renal cancer medications]]
 
[[Category:Renal cancer medications]]
 
[[Category:Waldenström macroglobulinemia medications]]
 
[[Category:Waldenström macroglobulinemia medications]]
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[[Category:Drugs FDA approved in 2009]]

Revision as of 02:09, 30 June 2014

Also known as Afinitor Disperz (everolimus tablets for oral suspension), Certican, RAD-001, Zortress.

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]

History of changes in FDA indication

Patient drug information

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)
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