Daily Medication Pearl: Trametinib (Mekinist)

Trametinib (Mekinist) is a kinase inhibitor indicated as a single agent for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test.

Medication Pearl of the Day: Trametinib (Mekinist)

Indication: Trametinib (Mekinist) is a kinase inhibitor indicated as a single agent for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test. It is also used in combination with dabrafenib to help prevent melanoma from recurring after surgery.

Insight:

  • Dosing: The recommended dosage regimen of trametinib is 2 mg orally once daily. Take trametinib at least 1 hour before or at least 2 hours after a meal.
  • Dosage forms: Tablets: 0.5 mg and 2 mg.
  • Adverse events: Most common adverse reactions (≥20%) for trametinib as a single agent include rash, diarrhea, and lymphedema. (6.1) Most common adverse reactions (≥20%) for trametinib with dabrafenib include pyrexia, nausea, rash, chills, diarrhea, and vomiting.
  • Mechanism of action: Trametinib is a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (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.
  • Manufacturer: Novartis Pharmaceuticals

Source:

label (fda.gov)