Products
Cobimetinib is commercially available in the form of film-coated tablets (Cotellic). It was approved in many countries in 2015.
Structure and properties
Cobimetinib (C21H21F3IN3O2, Mr = 531.3 g/mol) is present in the drug as cobimetinib hemifumarate, a white crystalline substance whose solubility is pH-dependent.
Effects
Cobimetinib (ATC L01XE38) has antitumor and antiproliferative properties. The effects are due to inhibition of the kinase MEK1/2. The mean half-life of cobimetinib is approximately 44 hours. Cobimetinib enhances the effect of vemurafenib and may counteract adverse effects of the BRAF inhibitor (e.g., development of squamous cell carcinoma).
Indications
For the treatment of patients with nonresectable or metastatic melanoma with the BRAF V600 mutation (combination therapy with vemurafenib).
Dosage
According to the SmPC. Tablets are taken once daily, independent of meals.
Contraindications
Cobimetinib is contraindicated in the presence of hypersensitivity. Full precautions can be found in the drug label.
Interactions
Cobimetinib is metabolized by CYP3A and UGT2B7, and corresponding drug-drug interactions are possible.
Adverse effects
The most common potential adverse effects include:
- Hypertension, bleeding
- Chorioretinopathy
- Diarrhea, nausea, vomiting
- Skin rash, photosensitivity
- Fever
