Skip to main content

Mektovi

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

Medically reviewed by Carmen Pope, BPharm. Last updated on Oct 25, 2023.

What is Mektovi?

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

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:

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.

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:

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

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.

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.

 

Popular FAQ

Mektovi is used in combination with another medicine called encorafenib (Braftovi) to treat advanced forms of melanoma (skin cancer) and non-small cell lung cancer with certain BRAF gene mutations. Continue reading

References

  1. Product label

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.