Mekinist

Generic name: trametinib [ tra-ME-ti-nib ]
Drug class: Multikinase inhibitors

Medically reviewed by Judith Stewart, BPharm. Last updated on Jul 6, 2022.

What is Mekinist?

Mekinist is a cancer medicine that interferes with the growth and spread of cancer cells in the body.

Mekinist is used alone or in combination with a medicine called dabrafenib (Tafinlar) to treat a type of skin cancer called melanoma that has spread to other parts of the body or cannot be removed by surgery, and has a certain type of abnormal “BRAF” gene.

Mekinist is used in combination with dabrafenib:

• to help prevent melanoma that has a certain type of abnormal “BRAF” gene from coming back after the cancer has been removed by surgery.
• to treat a type of lung cancer called non-small cell lung cancer (NSCLC) that has spread to other parts of the body, and that has a certain type of abnormal “BRAF” gene.
• to treat a type of thyroid cancer called anaplastic thyroid cancer (ATC) that has spread to other parts of the body and that has no satisfactory treatment options, and that has a certain type of abnormal “BRAF” gene.
• to treat solid tumors in adults and children 6 years and older that cannot be removed by surgery or that has spread to other parts of the body, and that has gotten worse (progressed) and that has no satisfactory treatment options, and that has a certain type of abnormal “BRAF” gene.

Mekinist is not for use in treating people with colorectal cancer.

Your healthcare provider will perform a test to make sure that Mekinist is right for you.

It is not known if Mekinist used in combination with dabrafenib is safe and effective in children younger than 6 years of age.

It is not known if Mekinist used alone is safe and effective in children.

Warnings

Using Mekinist with dabrafenib may increase your risk of developing a certain type of skin cancer. Ask your doctor about your specific risk. Tell your doctor if you notice new skin symptoms such as redness, warts, sores that will not heal, or a mole that has changed in size or color.

Follow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use.

Before taking this medicine

To make sure you can safely take Mekinist, tell your doctor if you have ever had:

• heart disease, high blood pressure;

• diabetes;

• lung disease;

• liver or kidney disease;

• a stomach or intestinal disorder;

• eye problems (especially a problem with your retina); or

• bleeding problems, or a blood clot.

Using Mekinist with dabrafenib may increase your risk of developing new skin cancer. Ask your doctor about the risk. Tell your doctor if you notice new skin symptoms such as redness, warts, sores that will not heal, or a mole that has changed in size or color.

Trametinib can harm an unborn baby if the mother or the father is using this medicine.

• If you are a woman, you may need a pregnancy test to make sure you are not pregnant. Use birth control while using Mekinist and for at least 4 months after your last dose.

• It may be harder for you get pregnant while using Mekinist. You should still use birth control to prevent pregnancy because the medicine can harm an unborn baby.

• If you are a man, use condoms if your sex partner is pregnant or is able to get pregnant, even if you've had a vasectomy. Keep using condoms for at least 4 months after your last dose.

• Tell your doctor right away if a pregnancy occurs.

Do not breastfeed while using Mekinist, and for at least 4 months after your last dose.

How should I take Mekinist?

Take Mekinist exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets.

Your doctor will make sure you have the correct tumor type to be treated with Mekinist.

Take Mekinist on an empty stomach, at least 1 hour before or 2 hours after a meal.

Your doctor will need to check your skin every 2 months while you are using Mekinist, and for up to 6 months after your last dose.

Your blood pressure and heart function will need to be checked often. You may also need regular vision examinations.

You may be given steroid medication if you have a fever and severe chills for 3 days or longer. Use the steroid for as long as your doctor has prescribed.

Store in the refrigerator and protect from light. Keep the tablets in their original container, along with the packet or canister of moisture-absorbing preservative. Do not store Mekinist tablets in a pill box.

Dosing information

Usual Adult Dose of Mekinist for Melanoma -- Metastatic:

Unresectable or Metastatic Melanoma:
-Single agent: 2 mg orally once a day
-Combination therapy: 2 mg orally once a day with dabrafenib (refer to the dabrafenib prescribing information for recommended dabrafenib dosing information)
-Duration of therapy: Until disease progression or unacceptable toxicity occurs.

Adjuvant Treatment of Melanoma:
-Combination therapy: 2 mg orally once a day with dabrafenib (refer to the dabrafenib prescribing information for recommended dabrafenib dosing information)
-Duration of therapy: Until disease progression or unacceptable toxicity occurs for up to one year.

Comments:
-Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to initiation.

Uses:
-As a single agent for the treatment of BRAF-inhibitor treatment-naive patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test
-In combination with dabrafenib for patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test
-In combination with dabrafenib for patients with melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test, and involvement of lymph node(s), following complete resection

Usual Adult Dose of Mekinist for Non-Small Cell Lung Cancer:

2 mg orally once a day with dabrafenib (refer to the dabrafenib prescribing information for recommended dabrafenib dosing information)
Duration of therapy: Until disease progression or unacceptable toxicity occurs.

Comments:
-Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of therapy with this drug and dabrafenib.

Use: In combination with dabrafenib for patients with metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation as detected by an FDA-approved test

Usual Adult Dose of Mekinist for Thyroid Cancer:

2 mg orally once a day with dabrafenib (refer to the dabrafenib prescribing information for recommended dabrafenib dosing information)
Duration of therapy: Until disease progression or unacceptable toxicity occurs.

Comments:
-Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of therapy with this drug and dabrafenib.

Use: In combination with dabrafenib for patients with locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation and with no satisfactory locoregional treatment options

Usual Adult Dose of Mekinist for Solid Tumors:

2 mg orally once a day with dabrafenib (refer to the dabrafenib prescribing information for recommended dabrafenib dosing information)
Duration of therapy: Until disease progression or unacceptable toxicity occurs.

Comments:
-Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of therapy with this drug and dabrafenib.

Use: In combination with dabrafenib the treatment of patients with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options. This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).

Usual Pediatric Dose of Mekinist for Solid Tumors:

The recommended dosage for Mekinist in pediatric patients who weigh at least 26 kg is based on body weight. A recommended dose has not been established in patients who weigh less than 26 kg.

Dosing in Pediatric Patients from 6 to 17 Years Old (Weight-Adjusted Dose)

Body Weight	Recommended Dose
26 kg to 37 kg	1 mg (two 0.5 mg tablets) orally once daily
38 to 50 kg	1.5 mg (three 0.5 mg tablets) orally once daily
51 kg or greater	2 mg orally once daily

Duration of therapy: Until disease progression or unacceptable toxicity occurs.

Comments:
-Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of therapy with this drug and dabrafenib.

Use: In combination with dabrafenib for the treatment of pediatric patients 6 years of age and older with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options. This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).

What happens if I miss a dose?

Take your dose of Mekinist as soon as you can, but skip the missed dose if your next dose is due in less than 12 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 should I avoid while taking Mekinist?

Trametinib can pass into body fluids (urine, feces, 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.

Mekinist side effects

Get emergency medical help if you have signs of an allergic reaction to Mekinist: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Some side effects are more likely to occur if you take Mekinist and dabrafenib together. Call your doctor at once if you have:

• cough, feeling short of breath;

• fever, chills, feeling light-headed;

• little or no urination;

• severe headache, blurred vision, and dizziness;

• nausea, stomach pain, severe diarrhea;

• increased thirst or urination;

• eye pain or swelling, vision changes, seeing halos around lights, seeing color "dots" in your vision;

• severe skin rash, skin pain or swelling, redness and peeling skin on your hands or feet;

• signs of bleeding - weakness, dizziness, headache, bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;

• signs of a blood clot - chest pain, sudden cough or trouble breathing, pain or swelling in an arm or leg, pale skin, cold feeling in an arm or leg; or

• signs of a heart problem - shortness of breath (even with mild exertion), pounding heartbeats, swelling in your feet or ankles.

Your cancer treatments may be delayed or permanently discontinued if you have certain side effects.

Common Mekinist side effects may include:

• nausea, vomiting, diarrhea, loss of appetite;

• fever, chills, tiredness;

• headache;

• bleeding;

• increased blood pressure;

• muscle or joint pain;

• cough, shortness of breath;

• swelling in your arms, face, and legs; or

• rash, dry skin.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Mekinist?

Other drugs may interact with trametinib, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all other medicines you use.

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Mekinist only for the indication prescribed.

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

Medical Disclaimer

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