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:
- Fatigue
- Nausea, diarrhea, vomiting, abdominal pain.
- Retinal detachment
- Muscle and joint pain
- Increase in CK in the blood