Difference between revisions of "Trametinib (Mekinist)"
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==General information== | ==General information== | ||
| − | Class/mechanism: Reversible [http://en.wikipedia.org/wiki/MAP2K1 MEK1 (mitogen-activated extracellular signal regulated kinase 1)] and [http://en.wikipedia.org/wiki/MAP2K2 MEK2] kinase inhibitor. MEK proteins are upstream and affect cellular proliferation by modulating the activity of the ERK (extracellular signal-related kinase) pathway. BRAF V600E mutations constitutively activate the BRAF pathway, which includes MEK1 and MEK2. By inhibiting MEK1 and MEK2, trametinib inhibits tumor cell growth that would otherwise be stimulated by constitutive activation from certain BRAF mutations.<ref name="insert">[http://us. | + | Class/mechanism: Reversible [http://en.wikipedia.org/wiki/MAP2K1 MEK1 (mitogen-activated extracellular signal regulated kinase 1)] and [http://en.wikipedia.org/wiki/MAP2K2 MEK2] kinase inhibitor. MEK proteins are upstream and affect cellular proliferation by modulating the activity of the ERK (extracellular signal-related kinase) pathway. BRAF V600E mutations constitutively activate the BRAF pathway, which includes MEK1 and MEK2. By inhibiting MEK1 and MEK2, trametinib inhibits tumor cell growth that would otherwise be stimulated by constitutive activation from certain BRAF mutations.<ref name="insert">[http://www.pharma.us.novartis.com/product/pi/pdf/mekinist.pdf Trametinib (Mekinist) package insert]</ref><ref>[[Media:Trametinib.pdf|Trametinib (Mekinist) package insert (locally hosted backup)]]</ref><ref>[http://mekinist.com/ Mekinist 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://us. | + | *[http://www.pharma.us.novartis.com/product/pi/pdf/mekinist.pdf Trametinib (Mekinist) package insert]<ref name="insert"></ref> |
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==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
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==Also known as== | ==Also known as== | ||
| − | GSK-1120212, GSK1120212, JTP-74057, Trametinib dimethyl sulfoxide. | + | *GSK-1120212, GSK1120212, JTP-74057, Trametinib dimethyl sulfoxide. |
==References== | ==References== | ||
Revision as of 06:55, 11 November 2015
General information
Class/mechanism: Reversible MEK1 (mitogen-activated extracellular signal regulated kinase 1) and MEK2 kinase inhibitor. MEK proteins are upstream and affect cellular proliferation by modulating the activity of the ERK (extracellular signal-related kinase) pathway. BRAF V600E mutations constitutively activate the BRAF pathway, which includes MEK1 and MEK2. By inhibiting MEK1 and MEK2, trametinib inhibits tumor cell growth that would otherwise be stimulated by constitutive activation from certain BRAF mutations.[1][2][3]
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 prescribing information.[1]
Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 5/29/2013: FDA approved "for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test."[1]
Also known as
- GSK-1120212, GSK1120212, JTP-74057, Trametinib dimethyl sulfoxide.