Difference between revisions of "Trametinib (Mekinist)"

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(FDA approval)
 
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==History of changes in FDA indication==
 
==History of changes in FDA indication==
*5/29/2013: [http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm354199.htm FDA approved] "to treat patients whose tumors express the BRAF V600E or V600K gene mutations."
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*5/29/2013: [http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm354199.htm 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."<ref name="insert"></ref>
  
 
==Also known as==
 
==Also known as==

Revision as of 06:23, 30 May 2013

FDA approved 5/29/2013.

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]
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

acetamide, N-[3-[3-cyclopropyl-5-[(2-fluoro-4- iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl- 2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-, compound with 1,1’-sulfinylbis[methane] (1:1), C26H23FIN5O4•C2H6OS, GSK-1120212, GSK1120212, JTP-74057, Trametinib dimethyl sulfoxide.

References