Products
Trametinib was approved in the form of film-coated tablets in the United States in 2013, in the EU in 2014, and in many countries in 2016 (Mekinist).
Structure and properties
Trametinib (C26H23FIN5O4, Mr = 615.4 g/mol) is a pyridine and a pyrimidine derivative. It is present in the drug product as trametinib dimethyl sulfoxide, a white powder that is practically insoluble in water.
Effects
Trametinib (ATC L01XE25) has antitumor and antiproliferative properties. The effects are due to inhibition of MEK kinases 1 and 2 (mitogen-activated extracellular signal-regulated kinase). MEK kinases are phospholyzed and activated by mutant V600 BRAF kinases (MAP kinase signaling pathway). Trametinib has a long half-life between 3 to 5 days.
Indications
In combination with dabrafenib for the treatment of adult patients with unresectable or metastatic melanoma with the BRAF V600 mutation (V600E/K).
Dosage
According to the SmPC. Tablets are taken fasting once daily, at least 1 hour before or two hours after a meal.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Adverse effects
The most common possible adverse effects of combination therapy include fever, fatigue, nausea, headache, chills, diarrhea, rash, joint pain, hypertension, vomiting, and cough.
