Difference between revisions of "Trametinib (Mekinist)"
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*1/10/2014: [http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm381159.htm FDA approved] in combination with [[Dabrafenib (Tafinlar)]] "for the treatment of patients with unresectable or metastatic [[Melanoma, BRAF-mutated|melanoma with BRAF V600E or V600K mutations]] as detected by an FDA-approved test."<ref name="insert"></ref> | *1/10/2014: [http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm381159.htm FDA approved] in combination with [[Dabrafenib (Tafinlar)]] "for the treatment of patients with unresectable or metastatic [[Melanoma, BRAF-mutated|melanoma with BRAF V600E or V600K mutations]] as detected by an FDA-approved test."<ref name="insert"></ref> | ||
*6/22/2017: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm564331.htm FDA approved] in combination with [[Dabrafenib (Tafinlar)]] "for patients with metastatic [[Non-small_cell_lung_cancer,_BRAF-mutated|non-small cell lung cancer (NSCLC) with BRAF V600E mutation]] as detected by an FDA-approved test." | *6/22/2017: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm564331.htm FDA approved] in combination with [[Dabrafenib (Tafinlar)]] "for patients with metastatic [[Non-small_cell_lung_cancer,_BRAF-mutated|non-small cell lung cancer (NSCLC) with BRAF V600E mutation]] as detected by an FDA-approved test." | ||
| + | *4/30/2018: Regular FDA approval with [[Dabrafenib (Tafinlar)]] "in combination for the adjuvant treatment of patients with [[Melanoma,_BRAF-mutated|melanoma with BRAF V600E or V600K mutations]], as detected by an FDA-approved test, and involvement of lymph node(s), following complete resection." | ||
==Also known as== | ==Also known as== | ||
Revision as of 02:24, 1 May 2018
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]
- 1/10/2014: FDA approved in combination with Dabrafenib (Tafinlar) "for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test."[1]
- 6/22/2017: FDA approved in combination with Dabrafenib (Tafinlar) "for patients with metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation as detected by an FDA-approved test."
- 4/30/2018: Regular FDA approval with Dabrafenib (Tafinlar) "in combination for the adjuvant treatment of patients with melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test, and involvement of lymph node(s), following complete resection."
Also known as
- Code names: GSK-1120212, GSK1120212, JTP-74057
- Generic name: trametinib dimethyl sulfoxide
- Brand name: Mekinist