MEKTOVI 15MG ( BINIMETINIB )

📘 Introduction & Drug Class

• Generic (Salt): Binimetinib

• Brand Name: Mektovi

• Drug Class: Orally active MEK‑1/2 inhibitor (blocks MAPK pathway signaling)

• Combined Use: Always taken with encorafenib (Braftovi®) for synergistic action

        Indications:

• Unresectable or metastatic melanoma harboring BRAF V600E or V600K mutations

• BRAF V600E‑mutant metastatic non‑small cell lung cancer (NSCLC)

🧪 Dosage & Administration

• Standard Dose: 45 mg twice daily (~12 hours apart), taken with or without food, alongside encorafenib

• Missed Dose: If more than 6 hours late, skip and continue with next scheduled dose

• Dose Reduction:

  • First dose reduction to 30 mg twice daily if intolerant

  • Discontinue if 30 mg is still not tolerated

• Hepatic Impairment: Reduce to 30 mg BID in moderate/severe hepatic dysfunction

⚠️ Side Effects

     Common 

• Fatigue (43%)

• Nausea (41%), diarrhea (36%), vomiting (30%)

• Abdominal pain (28%), constipation (22%)

• Rash (22%), peripheral edema (13%), headache, dizziness

• Visual disturbances (20%), serous retinopathy (~20%), hypertension (11%)

• Elevated liver enzymes, increased creatine phosphokinase, blood count changes

Serious Adverse Events

• Cardiac issues: Reduced LVEF in ~9.4%, occasionally requiring discontinuation

• Ocular toxicity: Retinopathy, uveitis, retinal vein occlusion—severe cases need drug pause or stop

• Bleeding/clots: Hemorrhage in ~19%, including serious events

• Pulmonary: Pulmonary embolism, ILD risk

• Muscle toxicity: Rhabdomyolysis possible (CPK elevation ~58%)

• Hepatotoxicity: ~6% grade 3–4 ALT increase; monitor monthly

🛡️ Warnings & Precautions

• Skin cancers: Risk of secondary malignancies—regular dermatologic exams

• Cardiotoxicity: Evaluate LVEF at baseline, 1 month, then every 2–3 months

• Ocular screening: Monitor for vision changes; consider ophthalmology referrals

• Pulmonary & GI: Watch for symptoms of ILD or colitis; withhold dose if suspected

• Bleeding & metabolic issues: RBC/platelet counts, liver function, CPK levels should be monitored regularly

• Reproductive safety: Teratogenic risk—use adequate contraception during treatment and for ≥30 days after stopping

These experiences highlight visual sensitivity, fatigue, nausea, and the importance of hydration.

✅ Conclusion

Mektovi (45 mg BID) plus encorafenib represents a potent targeted therapy for BRAF-mutant melanoma and NSCLC, with substantial efficacy. However, it requires meticulous monitoring for cardiac, ocular, skin, liver, and muscle toxicities, alongside patient education on hydration, eye protection, and symptom awareness.