• Metastatic/unresectable melanoma in patients with the BRAF V600E or V600K mutation (in combination with encorafenib).
• Metastatic non-small cell lung cancer (NSCLC) in patients with the BRAF V600E mutation (in combination with encorafenib).

Contraindicated in:

• OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• Left ventricular ejection fraction <50%
• History of retinal vein occlusion
• Uncontrolled glaucoma or history of hypercoagulability (↑ risk of retinal vein occlusion)
• Moderate or severe hepatic impairment (↓ dose)
• Women of reproductive potential
• Pedi: Safety and effectiveness not established in children.

CV: cardiomyopathy, hypertension, peripheral edema, DEEP VENOUS THROMBOSIS (DVT).

Derm: rash.

EENT: retinopathy, visual impairment, macular edema, retinal detachment, retinal vein occlusion (RVO), uveitis.

F and E: hyponatremia.

GI: ↑liver enzymes, abdominal pain, constipation, diarrhea, nausea, vomiting, colitis, HEPATOTOXICITY.

GU: ↑serum creatinine.

Hemat: anemia, hemorrhage, leukopenia, lymphopenia, neutropenia.

MS: ↑creatine kinase, RHABDOMYOLYSIS.

Neuro: dizziness, fatigue.

Resp: INTERSTITIAL LUNG DISEASE (ILD), PULMONARY EMBOLISM (PE).
Misc: fever, MALIGNANCY.

Drug-Drug:

• None reported.

• Tablets: 15 mg;

• PO (Adults): 45 mg twice daily; continue until disease progression or unacceptable toxicity.

Mektovi

• Inhibits the activity of mitogen-activated extracellular kinase 1 and 2, which are enzymes that normally promote cellular proliferation.

• Decreased progression of melanoma and improved survival.
• Decreased progression of NSCLC.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: At least 50% absorbed following oral administration.

Distribution: Extensively distributed to tissues.

Protein Binding: 97%.

Metabolism/Excretion: Mostly metabolized by the liver via glucuronidation. 62% excreted in feces (32% as unchanged drug); 31% excreted in urine (6.5% as unchanged drug).

Half-life: 3.5 hr.

(plasma concentrations)

• Instruct patient to take medication as directed. Take missed doses as soon as remembered, but not closer than 6 hr to next dose. If patient vomits after dose, omit and take next dose when scheduled.
• Advise patient to notify health care professional promptly if signs and symptoms of HF, venous thromboembolism (sudden onset of difficulty breathing, leg pain, swelling), changes in vision, ILD (new or worsening cough or dyspnea), hepatotoxicity (jaundice, dark urine, nausea, vomiting, loss of appetite, fatigue, bruising, bleeding), rhabdomyolysis (unusual or new onset weakness, myalgia, darkened urine), hemorrhage, or abnormal skin changes (mole color/shape changes, new wart, unhealed skin sores) occur.
• May cause fetal harm. Advise females of reproductive potential to use effective contraception during and for at least 30 days after last dose and to avoid breastfeeding for 3 days after last dose. Advise patient to notify health care professional if pregnancy is planned or suspected.

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