Mekinist is a targeted cancer drug that works by interfering with the growth and spread of cancer cells in the body.

Mekinist is only used for the treatment of certain cancers that have a mutation in the BRAF gene.

Mekinist works by blocking an enzyme called MEK from working, which slows the growth of cancer cells.

What is Mekinist used to treat?

Mekinist is used alone or in combination with another medicine called dabrafenib (Tafinlar) to treat certain types of cancer in people who have a BRAF gene mutation.

Mekinist is for use in treating:

• melanoma (skin cancer) that cannot be treated with surgery or has spread to other parts of the body, or to prevent melanoma from coming back after surgery; or

• non-small cell lung cancer that has spread to other parts of the body; or

• thyroid cancer (anaplastic thyroid cancer) that has spread to other parts of the body, and for which there are no other treatment options; or

• solid tumors (in adults and children 6 years and older) that cannot be removed with surgery, or have spread to other parts of the body, and that have gotten worse (progressed) and there are no other treatment options; or

• low-grade glioma (in children 1 year and older) that requires treatment with a medicine by mouth or injection (systemic therapy).

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 1 year of age.

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

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.

Your healthcare provider should check your skin before you start treatment, and every two months while taking this medicine to look for any new skin cancers.

Your healthcare provider may continue to check your skin for six months after you stop treatment.

Mekinist is usually taken one time each day. Follow all directions on your prescription label and read all medication guides or instruction sheets.

Your doctor will perform blood tests to 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.

Mekinist should be taken at evenly spaced intervals, about every 24 hours.

Tablets

Swallow the tablets whole. Do not open, crush, or break the tablets. 

If Mekinist tablets are prescribed for your child 6 years of age or older, your child’s healthcare provider will adjust their dose as your child grows.

Tell your healthcare provider if you or your child is not able to swallow the tablets whole.

Oral Solution

The oral solution is reconstituted from powder form by your pharmacist prior to dispensing. The prepared oral solution can be used for 35 days. Throw away (dispose of) any remaining oral solution after 35 days.

The oral solution should only be given by a caregiver.

If Mekinist oral solution is prescribed for your child 1 year of age or older, your child’s healthcare provider will adjust their dose as your child grows.

See the detailed Instructions for Use leaflet that comes with the medicine for instructions on how to correctly prepare and take or give a dose of the oral solution.

The oral solution can be given using an oral dosing syringe or feeding tube.

If at any time the oral solution gets on your or your child’s skin, wash the area well with soap and water.

If at any time the oral solution gets in your or your child’s eyes, rinse the eyes well with cool water.

Additional Information

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.

How should I store Mekinist?

Keep all medicines out of the reach of children and pets.

Tablets

Store the tablets in a refrigerator between 36°F to 46°F (2°C to 8°C).

Keep the tablets dry and away from moisture.

The tablet bottle contains a drying agent (desiccant packet) to help keep your medicine dry. Do not throw away the desiccant packet.

Keep the tablets in the original bottle. Do not place tablets in a pill box.

Safely throw away any tablets that are out of date or no longer needed.

Oral Solution

Store the oral solution in the original bottle at room temperature below 77°F (25°C).

Do not freeze the oral solution.

Throw away (dispose of) unused oral solution after the "discard after" date written on the bottle label.

Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to treatment initiation with FDA-approved tests: http://www.fda.gov/CompanionDiagnostics.

Usual Adult Dose for Melanoma, Non-Small Cell Lung Cancer, Thyroid Cancer, and Solid Tumors

2 mg orally once daily.

Uses:

as a single agent for the treatment of BRAF-inhibitor treatment-naïve patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations

in combination with dabrafenib:
- for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations.
- for the adjuvant treatment of patients with melanoma with BRAF V600E or V600K mutations, and involvement of lymph node(s), following complete resection.
- for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation.
- for the treatment of patients with locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation and with no satisfactory locoregional treatment options.
- for the treatment of adult 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).

Recommended duration of treatment:
- for patients with unresectable or metastatic melanoma or solid tumors, metastatic NSCLC, or locally advanced or metastatic anaplastic thyroid cancer is until disease progression or unacceptable toxicity.
- for patients in the adjuvant melanoma setting is until disease recurrence or unacceptable toxicity for up to 1 year.

Usual Pediatric Dose for Solid Tumors and Low-Grade Glioma

The recommended dosage for Mekinist in pediatric patients is based on body weight.

Tablets

Mekinist tablets for oral use are supplied as 0.5 mg and 2 mg tablets for oral administration. 

Oral Solution

Mekinist for oral solution is a white or almost white powder which produces a clear colorless solution when reconstituted with water. Each mL of reconstituted strawberry flavored oral solution contains trametinib 0.05 mg.

Uses:

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).
- for the treatment of pediatric patients 1 year of age and older with low-grade glioma (LGG) with a BRAF V600E mutation who require systemic therapy.

Recommended duration of treatment:
- for pediatric patients with solid tumors is until disease progression or unacceptable toxicity.
- for pediatric patients with LGG is until disease progression or until unacceptable toxicity. 

You should not use Mekinist if you are allergic to trametinib.

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

• heart problems;

• bleeding problems, or a blood clot;

• stomach problems;

• inflammation of the colon;

• liver or kidney disease;

• diabetes;

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

• lung or breathing problems; or

• high blood pressure (hypertension).

Using Mekinist with dabrafenib may increase your risk of developing new 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.

Pregnancy

You may need to have a negative pregnancy test before starting this treatment.

Both men and women using this medicine should use effective birth control to prevent pregnancy.
Trametinib can harm an unborn baby or cause birth defects if the mother or father is using this medicine.

Females who are able to become pregnant should use effective birth control while using Mekinist and for at least 4 months after your last dose.

Talk to your healthcare provider about birth control methods that may be right for you during this time.

Tell your healthcare provider right away if you become pregnant or think you might be pregnant during treatment .

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.

Males (including those who have had a vasectomy) with a female partner who is able to become pregnant should use condoms during treatment and for at least 4 months after your last dose.

Tell your doctor right away if a pregnancy occurs.

Breastfeeding

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

Talk to your healthcare provider about the best way to feed your baby during this time.

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.

If you vomit after taking a dose, do not take an additional dose. Take the next dose at your regular time.

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

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.

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 blood sugar, increased thirst or urination;

• eye pain or swelling, redness, vision changes, loss of vision, 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 in adults 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, acne.

Common Mekinist side effects in children may include:

• nausea, vomiting, diarrhea;

• fever, tiredness;

• headache;

• stomach-area (abdomen) pain;

• bleeding;

• constipation;

• skin infection around fingernails or toenails;

• muscle or bone pain;

• cough;

• 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.

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.