Drugs of interest to pathologists
Drugs related to surgical pathology
Trametinib

Author: Him G. Kwee, M.D. (see Authors page)

Revised: 6 December 2017, last major update February 2014

Copyright: (c) 2002-2017, PathologyOutlines.com, Inc.

PubMed Search: Trametinib [title] "loattrfree full text"[sb]

Cite this page: Kwee, H.G. Trametinib. PathologyOutlines.com website. http://www.pathologyoutlines.com/topic/drugstrametinib.html. Accessed June 25th, 2018.
Definition / general
  • Trametinib is a kinase inhibitor that inhibits MEK1 and MEK2
  • It blocks the activity of V600E or V600K mutated forms of BRAF
Trade name
  • Mekinist®
Clinical information
  • Approved by the U.S. Food and Drug Administration in May 2013 as a single drug for unresectable or metastatic malignant melanoma that has the V600E or V600K BRAF mutation
  • It is not indicated for patients who have received prior BRAF inhibitor therapy
  • In January 2014, the FDA approved the combination therapy of Trametinib and Dabrafenib (Tafinlar) for unresectable or metastatic malignant melanoma
  • The FDA has also approved the test Thx ID-BRAF (bioMerieux S.A.) to detect BRAF V600E and BRAF V600K mutations, which can be performed on formalin fixed paraffin embedded tissue
  • About half of patients with malignant melanoma have BRAF mutations, of which 85% are V600E mutations, and 10% are V600K mutations
  • Cost: $8,700 per month
  • Side effects: cardiomyopathy, retinal pigment epithelial detachment, retinal vein occlusion, increase in blood pressure; also skin rash (in 87% of patients), interstitial lung disease / pneumonitis, diarrhea, lymphedema, fetal malformation