Last reviewed 2026-04-20 · How we verify

Mekinist (trametinib)

Mekinist works by blocking a specific enzyme called BRAF V600E, which is involved in the growth and spread of cancer cells.

Mekinist (trametinib) is a small molecule kinase inhibitor developed by Novartis, targeting the dual specificity mitogen-activated protein kinase kinase 2. It is used to treat various cancers, including anaplastic thyroid cancer, malignant melanoma, and non-small cell lung cancer, with BRAF V600E or V600K mutations. Mekinist is patented and has a long half-life of 229 hours. It is available as a branded product, with a single generic manufacturer. Key safety considerations include potential side effects such as rash, diarrhea, and fatigue.

At a glance

Mechanism of action

Trametinib is reversible inhibitor of mitogen-activated extracellular signal-regulated kinase (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. BRAF V600E mutations result in constitutive activation of the BRAF pathway which includes MEK1 and MEK2. Trametinib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.Trametinib and dabrafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Use of trametinib and dabrafenib in combination resulted in greater growth inhibition of BRAF V600 mutation-positive tumor cell lines in vitro and prolonged inhibition of tumor growth in BRAF V600 mutation positive tumor xenografts compared with either drug alone.

Approved indications

• Locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation
• Malignant Melanoma with BRAF V600E Mutation
• Malignant Melanoma with BRAF V600K Mutation
• Metastatic malignant melanoma
• Metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation
• Unresectable or metastatic solid tumors with BRAF V600E mutation

Common side effects

• Rash
• Diarrhea
• Pyrexia
• Fatigue
• Nausea
• Vomiting
• Hypertension
• Peripheral edema
• Lymphedema
• Chills
• Headache
• Arthralgia

Key clinical trials

• Study of Selective BRAF Kinase Inhibitor Dabrafenib Monotherapy Twice Daily and in Combination With Dabrafenib Twice Daily and Trametinib Once Daily in Combination Therapy in Subjects With BRAF V600E Mutation Positive Metastatic (Stage IV) Non-small Cell Lung Cancer. (PHASE2)
• A Study Comparing Trametinib and Dabrafenib Combination Therapy to Dabrafenib Monotherapy in Subjects With BRAF-mutant Melanoma (PHASE3)
• Efficacy and Safety of the Combination Therapy of Dabrafenib and Trametinib in Subjects With BRAF V600E- Mutated Rare Cancers (PHASE2)
• GSK1120212 vs Chemotherapy in Advanced or Metastatic BRAF V600E/K Mutation-positive Melanoma (PHASE3)
• Study to Evaluate Treatment of Dabrafenib Plus Trametinib in Subjects With BRAF Mutation-Positive Melanoma That Has Metastasized to the Brain (PHASE2)
• Dabrafenib With Trametinib in the Adjuvant Treatment of High-risk BRAF V600 Mutation-positive Melanoma (COMBI-AD). (PHASE3)
• Trametinib With or Without GSK2141795 in Treating Patients With Metastatic Uveal Melanoma (PHASE2)
• Testing Trametinib as a Potential Targeted Treatment in Cancers With GNAQ or GNA11 Genetic Changes (MATCH-Subprotocol S2) (PHASE2)

Patents

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Mekinist CI brief — competitive landscape report
• Mekinist updates RSS · CI watch RSS
• Novartis portfolio CI