Binimetinib

Products

Binimetinib was approved in the EU and US in 2018 and in many countries in 2019 in film-coated tablet form (Mektovi).

Structure and properties

Binimetinib (C17H15BrF2N4O3, Mr = 441.2 g/mol) exists as a light yellow powder that is practically insoluble in water.

Effects

Binimetinib (ATC L01XE41) has antitumor and antiproliferative properties. The effects are due to reversible inhibition of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2.

Indications

In combination with encorafenib for the treatment of adult patients with nonresectable or metastatic melanoma with a BRAF V600 mutation.

Dosage

According to the SmPC. Tablets are taken morning and evening 12 hours apart, independent of meals. The half-life is approximately 8 hours.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Binimetinib is glucuronidated by UGT1A1. Interactions have been described with inducers of CYP1A2.

Adverse effects

The most common potential adverse effects include: