Difference between revisions of "Everolimus (Afinitor)"
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| − | Also known as Afinitor Disperz (everolimus tablets for oral suspension), Zortress. | + | Also known as Afinitor Disperz (everolimus tablets for oral suspension), Certican, RAD-001, Zortress. |
==General information== | ==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).<ref name="insert">[http://www.pharma.us.novartis.com/product/pi/pdf/afinitor.pdf Everolimus (Afinitor) package insert]</ref><ref>[[Media:Everolimus.pdf | Everolimus (Afinitor) package insert (locally hosted backup)]]</ref> | + | 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).<ref name="insert">[http://www.pharma.us.novartis.com/product/pi/pdf/afinitor.pdf Everolimus (Afinitor) package insert]</ref><ref>[[Media:Everolimus.pdf | Everolimus (Afinitor) package insert (locally hosted backup)]]</ref><ref>[http://www.afinitor.com Afinitor manufacturer's website]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a | ||
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==Patient drug information== | ==Patient drug information== | ||
*[http://www.pharma.us.novartis.com/product/pi/pdf/afinitor.pdf#page=40 Everolimus (Afinitor) package insert PDF pages 40-46]<ref name="insert"></ref> | *[http://www.pharma.us.novartis.com/product/pi/pdf/afinitor.pdf#page=40 Everolimus (Afinitor) package insert PDF pages 40-46]<ref name="insert"></ref> | ||
| − | *[http://chemocare.com/ | + | *[http://chemocare.com/chemotherapy/drug-info/everolimus.aspx Everolimus (Afinitor) patient drug information (Chemocare)]<ref>[http://chemocare.com/chemotherapy/drug-info/everolimus.aspx Everolimus (Afinitor) patient drug information (Chemocare)]</ref> |
*[http://www.uptodate.com/contents/everolimus-patient-drug-information Everolimus (Afinitor) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/everolimus-patient-drug-information Everolimus (Afinitor) patient drug information (UpToDate)]</ref> | *[http://www.uptodate.com/contents/everolimus-patient-drug-information Everolimus (Afinitor) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/everolimus-patient-drug-information Everolimus (Afinitor) patient drug information (UpToDate)]</ref> | ||
==References== | ==References== | ||
<references/> | <references/> | ||
| + | |||
| + | [[Category:Drug index]] | ||
| + | [[Category:Chemotherapy]] | ||
| + | [[Category:Tyrosine kinase inhibitors]] | ||
| + | [[Category:mTOR inhibitors]] | ||
| + | [[Category:Breast cancer medications]] | ||
| + | [[Category:Renal cancer medications]] | ||
Revision as of 03:47, 4 November 2012
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]
Diseases for which it is used
Patient drug information
- Everolimus (Afinitor) package insert PDF pages 40-46[1]
- Everolimus (Afinitor) patient drug information (Chemocare)[6]
- Everolimus (Afinitor) patient drug information (UpToDate)[7]
References
- ↑ 1.0 1.1 1.2 Everolimus (Afinitor) package insert
- ↑ Everolimus (Afinitor) package insert (locally hosted backup)
- ↑ Afinitor manufacturer's website
- ↑ Discussion between Sara Hurvitz, MD and Neil Love, MD, 2012
- ↑ Simeon Bennett, Novartis’ Afinitor gets OK of FDA, Bloomberg News (July 29, 2012). Retrieved 9/11/2012.
- ↑ Everolimus (Afinitor) patient drug information (Chemocare)
- ↑ Everolimus (Afinitor) patient drug information (UpToDate)