Difference between revisions of "Everolimus (Afinitor)"
(Created page with "==General information== Class/mechanism: <ref name="insert">[http://www.pharma.us.novartis.com/product/pi/pdf/afinitor.pdf Everolimus (Afinitor) package insert]</ref><ref>[http:/...") |
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==General information== | ==General information== | ||
| − | Class/mechanism: <ref name="insert">[http://www.pharma.us.novartis.com/product/pi/pdf/afinitor.pdf Everolimus (Afinitor) package insert]</ref><ref>[http://hemonc.org/docs/packageinsert/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>[http://hemonc.org/docs/packageinsert/everolimus.pdf Everolimus (Afinitor) package insert (locally hosted backup)]</ref> |
| − | <br>Route: | + | <br>Route: PO |
| − | <br>Extravasation: | + | <br>Extravasation: n/a |
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 package insert<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 package insert<ref name="insert"></ref>. | ||
Revision as of 03:57, 14 January 2012
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]
Route: PO
Extravasation: n/a
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 package insert[1].
Patient drug information
- Everolimus (Afinitor) patient drug information (Chemocare)[3]
- Everolimus (Afinitor) patient drug information (UpToDate)[4]