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Binimetinib

Brand and Other Names: MEKTOVI
Mechanism of Action:

Binimetinib is a reversible inhibitor of MEK1 and MEK2, key kinases in the MAPK/ERK pathway. It reduces ERK phosphorylation and downstream tumor cell proliferation, particularly in BRAF V600-mutant tumors.

Indications:

In combination with encorafenib for:

  • Unresectable or metastatic melanoma with BRAF V600E/K mutation

  • Metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation

Route: oral
Dose:

Recommended Dose: 45 mg orally twice daily (approximately 12 hours apart), in combination with encorafenib

Hepatic Impairment: 30 mg twice daily for moderate/severe hepatic impairment

Adverse Reactions:

Common (≥25%): Fatigue, nausea, diarrhea, vomiting, abdominal pain, visual impairment, rash

Serious: Cardiomyopathy, venous thromboembolism, ocular toxicities (retinopathy, RVO, uveitis), ILD, hepatotoxicity, rhabdomyolysis, hemorrhage

Contraindication:

None

Warnings and Precautions:

  • New primary malignancies (cutaneous and non-cutaneous)

  • Cardiomyopathy: Monitor LVEF regularly

  • Ocular events: Regular ophthalmologic exams required

  • ILD and pneumonitis

  • Liver toxicity: Monitor LFTs

  • Muscle toxicity: Monitor CPK and renal function

  • Hemorrhage risk: Serious or fatal bleeding events reported

  • Embryo-fetal toxicity: Avoid in pregnancy; effective contraception required

 

See package insert for full prescribing information.