Trametinib (Mekinist)

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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, 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 established (work in progress)

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Low-grade glioma, pediatric

Melanoma, BRAF-mutated

Non-small cell lung cancer, BRAF-mutated

Thyroid cancer, BRAF-mutated

History of changes in EMA indication

  • 2014-06-30: Initial marketing authorization as Mekinist

History of changes in Health Canada indication

  • 2016-03-11: Initial notice of compliance with conditions
  • 2016-05-13: Conditions were met

History of changes in PMDA indication

  • 2018-03-23: new additional indication for the treatment of unresectable advanced or recurrent BRAF mutation-positive non-small cell lung cancer.
  • 2018-07-02: new additional indication and a new dosage indicated for the treatment of BRAF mutation-positive melanoma.

Also known as

  • Code names: GSK-1120212, GSK1120212, JTP-74057
  • Generic name: trametinib dimethyl sulfoxide
  • Brand name: Mekinist, Meqsel