Mektovi (Binimetinib)

Mektovi targets the MAPK/ERK signaling pathway, which is frequently dysregulated in solid tumours.

• Melanoma: helps control disease progression in patients with BRAF‑mutated advanced melanoma.
• Non‑small cell lung cancer: used in combination therapy to improve outcomes in patients with KRAS‑mutated NSCLC.

• Binimetinib selectively inhibits the kinases MEK1 and MEK2, key components of the MAPK/ERK cascade. By blocking MEK activity, the drug reduces phosphorylation of ERK, leading to decreased transcription of genes that drive tumor cell proliferation and survival, thereby limiting cancer growth.

Adverse reactions may occur with any antineoplastic therapy.

Common Side Effects

• Diarrhea: frequent loose stools that may require supportive care.
• Rash: skin eruptions ranging from mild to moderate severity.
• Nausea: feeling of sickness often managed with anti‑emetics.
• Fatigue: persistent tiredness affecting daily activities.

Serious or Rare Side Effects

• Interstitial lung disease: inflammation of lung tissue that can be life‑threatening.
• Cardiac dysfunction: reduced left‑ventricular ejection fraction or heart failure.
• Retinal disorders: visual disturbances including serous retinal detachment.
• Severe hypertension: markedly elevated blood pressure requiring immediate treatment.
• Hepatic toxicity: significant elevation of liver enzymes or liver failure.
• Febrile neutropenia: fever with low neutrophil count, increasing infection risk.

Patients should be monitored closely for safety concerns before and during treatment.

• Cardiac monitoring: assess baseline and periodic ejection fraction.
• Liver function: check transaminases and bilirubin regularly.
• Ocular assessment: perform baseline eye exam and monitor for visual changes.
• Renal impairment: evaluate kidney function and adjust use if severe.
• Contraception: advise effective birth control during therapy and for a defined period after discontinuation.
• Store at room temperature: keep in the original packaging, protect from moisture and direct sunlight.

Binimetinib may interact with other medicines, altering efficacy or safety.

Major Interactions (Avoid)

• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): may reduce exposure.
• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may increase exposure.
• QT‑prolonging agents: combined use can heighten risk of cardiac arrhythmia.

Moderate Interactions (Monitor Closely)

• Antacids containing aluminum or magnesium: may affect absorption; separate dosing.
• Warfarin: monitor INR as binimetinib can influence anticoagulant effect.