Trametinib is an orally bioavailable mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 inhibitor.[A258298,A258293] It was first approved by the FDA in May 2013 for the treatment of melanoma.[A258298] It was later approved by Health Canada on July 18, 2013 [L45588] and by the European Commission on June 30, 2014.[L45583] Trametinib is currently approved to treat a variety of cancers with BRAF mutations, such as non-small cell lung cancer and thyroid cancer, as monotherapy or in combination with [dabrafenib], a BRAF inhibitor, for improved therapeutic efficacy. Originally developed by Japan Tobacco, trametinib was initially investigated for treating inflammation, but further studies for this indication were not pursued.[A258298]
Synonyms
Tramétinib
Trametinibum
Trametinib dimethyl sulfoxide
Trametinib
Brand Names
Mekinist
Indication
Trametinib is indicated as monotherapy for the treatment of BRAF-inhibitor treatment-naïve patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations.[L2727,L45583] It is used in combination with [dabrafenib] for the: - treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations.[L45558] - adjuvant treatment of patients with melanoma with BRAF V600E or V600K mutations and involvement of lymph node(s), following complete resection.[L45558,L45583] - treatment of patients with metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation.[L45558] In Europe, it is indicated for the treatment of adults with advanced non-small cell lung cancer with a BRAF V600 mutation.[L45583] - treatment of patients with locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation and with no satisfactory locoregional treatment options.[L45558] - the treatment of adult and pediatric patients six years of age and older with unresectable or metastatic solid tumours with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options. In the US, this indication is approved under accelerated approval based on the overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).[L45558] - the treatment of pediatric patients one year of age and older with low-grade glioma (LGG) with a BRAF V600E mutation who require systemic therapy.[L45558] In the US, BRAF V600E or V600K mutations must be detected by an FDA-approved test. Trametinib is not indicated for the treatment of patients with colorectal cancer because of known intrinsic resistance to BRAF inhibition.[L45558]
Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison
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