Products
Encorafenib was approved in capsule form in the United States and EU in 2018 and in many countries in 2019 (Braftovi).
Structure and properties
Encorafenib (C22H27ClFN7O4S, Mr = 540.0 g/mol) exists as a white powder that is somewhat soluble in water only at low pH.
Effects
Encorafenib (ATC L01XE46) has antitumor and antiproliferative properties. The effects are due to inhibition of BRAF kinase (wild-type) and mutant BRAF kinase (V600E).
Indications
In combination with the MEK inhibitor binimetinib is indicated for the treatment of adult patients with nonresectable or metastatic melanoma with a BRAF V600 mutation.
Dosage
According to the SmPC. Capsules are taken once daily, independent of meals. Do not take with grapefruit juice.
Contraindications
- Hypersensitivity
- Pregnancy, lactation
Full precautions can be found in the drug label.
Interactions
Encorafenib is a substrate of CYP3A4 and, to a lesser extent, CYP2C19 and CYP2D6.
Adverse effects
The most common possible adverse effects include fatigue, nausea, diarrhea, detachment of the retinal pigment epithelium, vomiting, abdominal pain, joint pain, and muscle disorders or muscle pain.
