Pronunciation: mek-TOE-vee
Generic name: binimetinib
Dosage form: oral tablet
Drug class: Multikinase inhibitors

Medically reviewed by Carmen Pope, BPharm. Last updated on Mar 26, 2024.

What is Mektovi?

Mektovi (binimetinib) is an oral kinase inhibitor that may be used in combination with encorafenib for the treatment of adults with:

• unresectable or metastatic melanoma with a confirmed BRAF V600E or V600K mutation
• metastatic non-small cell lung cancer (NSCLC) with a confirmed BRAF V600E mutation.

Mektovi is a reversible inhibitor of two proteins, mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2. These are upstream regulators of the extracellular signal-related kinase (ERK) pathway and blocking them results in an inhibition of extracellular signal-related kinase (ERK) phosphorylation as well as the viability and MEK-dependent phosphorylation of BRAF-mutations. A BRAF mutation is a spontaneous change in the BRAF gene that makes it work incorrectly, turning on the protein and keeping it on. This means certain cells get ongoing signals to keep dividing and no instructions on when to stop, leading to the development of a tumor. It is given together with encorafenib which targets a different kinase in the RAS/RAF/MEK/ERK pathway.

Roughly 50% of patients diagnosed with metastatic melanoma test positive for the BRAF mutation, and it is the most common genetic mutation in metastatic melanoma. BRAF mutations are rare in non-small cell lung cancer (NSCLC), occurring in 2% to 5% of cases.

Mektovi was FDA-approved on 27 June 2018.

Warnings

Although Mektovi is used to treat melanoma, it may increase your risk of developing other types of cancer including skin cancer when used in combination with encorafenib. Ask your doctor about your specific risk. Tell your doctor if you notice any new skin or other symptoms. Your healthcare provider should check your skin before treatment, every 2 months during treatment, and for up to 6 months after you stop treatment to look for any new skin or other cancers.

Mektovi can harm an unborn baby. Do not use it if you are pregnant. Your doctor may conduct a pregnancy test before you start treatment if you are a woman of childbearing age. Use a non-hormonal form of birth control to prevent pregnancy while using Mektovi and for at least 30 days after your last dose.

May not be suitable for patients with cardiomyopathy. Your healthcare provider will assess your left ventricular ejection fraction (LVEF) before initiating treatment, then after one month of treatment, and then every 2 to 3 months thereafter.

May cause liver toxicity when used in combination with encorafenib. Your healthcare provider will conduct liver function tests before treatment, and then monitor your liver function during treatment.

There is also a risk of major bleeding events, venous thromboembolism, interstitial lung disease, muscle toxicity, and eye toxicity such as uveitis (inflammation inside the eye), and retinopathy (disease of the retina). Your doctor may perform certain tests before starting treatment, and then monitor you throughout treatment.

It is not known if Mektovi is safe and effective in children.

Mektovi is not recommended to be used as a single agent.

Before taking this medicine

You should not use Mektovi if you are allergic to binimetinib or any of the other components in the tablets.

Tell your doctor if you have ever had:

• heart disease, high blood pressure
• lung disease
• a muscle disorder
• liver or kidney disease
• eye problems (especially a problem with your retina) or
• bleeding problems, or a blood clot
• are pregnant or plan to become pregnant.

Pregnancy

Do not use Mektovi if you are pregnant. It could harm the unborn baby or cause birth defects. Use effective birth control to prevent pregnancy while you are using this medicine and for at least 30 days after your last dose.

Tell your doctor if you think you may be pregnant. You may need to have a negative pregnancy test before starting this treatment.

Breastfeeding

You should not breastfeed while using this medicine, and for at least 3 days after your last dose.

How should I take Mektovi?

Take Mektovi exactly as it was prescribed for you. Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.

• Mektovi is usually taken twice per day (every 12 hours), with or without food.
• The recommended dose for melanoma and NSCLC is 45mg twice daily, taken in combination with encorafenib.
• The dosage may need to be reduced in those with liver disease.
• Do not change your dose or dosing schedule without your doctor's advice.
• If you vomit shortly after taking Mektovi, do not take another dose. Wait until your next scheduled dose time to take the medicine again.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if your next dose is due in less than 6 hours. Do not use two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What to avoid

Mektovi can pass into body fluids such as urine, feces, or vomit. Caregivers should wear rubber gloves while cleaning up a patient's body fluids, handling contaminated trash or laundry, or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.

What are the side effects of Mektovi?

Get emergency medical help if you have signs of an allergic reaction to Mektovi such as hives; difficulty breathing; or swelling of your face, lips, tongue, or throat.

Mektovi may cause serious side effects, such as:

• Heart problems, including heart failure. Call your healthcare provider right away if you have any of the following signs and symptoms:
  • feeling like your heart is pounding or racing
  • shortness of breath
  • swelling of your ankles and feet
  • feeling lightheaded.
• Blood clots. Get medical help right away if you have the following symptoms:
  • chest pain
  • sudden shortness of breath or trouble breathing
  • pain in your legs with or without swelling
  • swelling in your arms and legs
  • a cool pale arm or leg.
• Eye problems. Tell your healthcare provider right away if you develop any new or worsening symptoms of eye problems, including:
  • blurred vision, loss of vision, or other vision changes
  • see colored dots
  • see halos (blurred outlines around objects)
  • eye pain, swelling, or redness.
• Lung or breathing problems. Tell your healthcare provider if you have any new or worsening symptoms of lung or breathing problems, including:
  • shortness of breath
  • cough.
• Liver problems. Tell your healthcare provider if you have any of the following signs and symptoms of a liver problem:
  • yellowing of your skin or your eyes o tiredness
  • dark or brown (tea-colored) urine o bruising
  • nausea or vomiting o bleeding
  • loss of appetite.
• Muscle problems (rhabdomyolysis). Treatment with Mektovi may increase the level of an enzyme in your blood called creatine phosphokinase (CPK) and can be a sign of muscle damage. Tell your healthcare provider right away if you develop:
  • weakness
  • muscle aches or pain
  • dark, reddish urine.
• Bleeding problems. Tell your healthcare provider and get medical help right away if you develop any signs of bleeding, including:
  • headaches, dizziness, or feeling weak
  • cough up blood or blood clots
  • vomit blood or your vomit looks like “coffee grounds”
  • red or black stool that looks like tar.

The most common side effects of Mektovi affecting more than 25% of people who are taking it with encorafenib (depending on the condition) include:

• fatigue
• vomiting
• nausea
• stomach-area (abdominal) pain
• diarrhea or constipation
• blurred vision, loss of vision, or other vision changes
• shortness of breath
• muscle or joint pain
• rash
• cough.

These are not all of the possible side effects of Mektovi. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects to Pfizer Inc. at 1-800-438-1985.

Related/similar drugs

What other drugs will affect Mektovi?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

While no clinically important drug interactions have been observed with Mektovi, several interactions have been reported with encorafenib.

Know the medicines you take. Keep a list of them to show to your healthcare provider and pharmacist when you get a new medicine. See the prescribing information for a full list of interactions.

Storage

Store at room temperature, 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F).

Keep the container tightly closed and out of reach of children.

Ingredients

Oral tablets

Active: binimetinib 15mg

Inactive: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate (vegetable source), and colloidal silicon dioxide.

Coating: polyvinyl alcohol, polyethylene glycol, titanium dioxide, talc, ferric oxide yellow, and ferrosoferric oxide.

Manufacturer

Array BioPharma Inc., a wholly owned subsidiary of Pfizer Inc.

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