Mekinist

Mekinist is the brand name for trametinib, a targeted cancer therapy that inhibits MEK1 and MEK2 kinases in the MAPK/ERK signaling pathway. By blocking MEK activity, trametinib can reduce proliferation and survival of tumor cells driven by MAPK pathway activation. Mekinist is developed by Novartis.

In the United States and European Union, Mekinist is approved for the treatment of unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, typically in combination with dabrafenib, a BRAF inhibitor. The combination therapy targets tumors with BRAF mutations by dual blockade of the pathway. Additional approvals exist in other countries and for other BRAF-mutant cancers, such as non-small cell lung cancer in select patients, with regulatory status evolving over time.

Trametinib is taken orally, usually once daily, with dosing adjusted for tolerability and patient factors. It is generally continued until disease progression or unacceptable toxicity, and management of side effects may include dose interruptions or reductions.

Common adverse effects include rash, diarrhea, edema, fatigue, and nausea. Ocular toxicity requiring monitoring, including retinal changes, has been observed. Cardiomyopathy and decreased left ventricular function can occur, as can interstitial lung disease and liver enzyme elevations; patients require regular monitoring.

Beyond melanoma, trametinib has been studied in other MAPK-activated tumors and in combination regimens, contributing to the development of targeted therapies for BRAF-mutant cancers.