Pronunciation:

tra-ME-ti-nib

Brand Names:

• Mekinist

Dosage Forms:

• Powder for Solution
• Tablet

Classifications:

Therapeutic—

Antineoplastic Agent

Uses of This Medicine:

Trametinib is used alone or in combination with dabrafenib to treat melanoma (skin cancer) that has spread or that cannot be removed by surgery. It is also used together with dabrafenib to help prevent melanoma from coming back after surgery. It is only used if the melanoma cells have the BRAF V600E or V600K mutations. Trametinib is also used together with dabrafenib to treat non-small cell lung cancer (NSCLC) that has spread, and anaplastic thyroid cancer (ATC) that has spread and has no satisfactory treatment options. It is only used if the NSCLC cells and ATC cells have the BRAF V600E mutation. Trametinib is also used in combination with dabrafenib to treat solid tumors that has spread, that cannot be removed by surgery, or that have gotten worse (progressed) and has no satisfactory treatment options. It is only used if the solid tumors have the BRAF V600E mutations. Trametinib is also used in combination with dabrafenib to treat low-grade glioma (LGG) in patients who require other treatments. It is only used if the brain tumor has the BRAF V600E mutations. Your doctor will use a special test to look for these mutations. Trametinib belongs to the group of medicines, called antineoplastics (cancer medicines).

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of trametinib to treat melanoma, non-small cell lung cancer, and anaplastic thyroid cancer in children and to treat glioma and solid tumors in children younger than 1 year of age. Safety and efficacy have not been established.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of trametinib in the elderly.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Bleeding problems or
• Blood clots (eg, deep vein thrombosis, pulmonary embolism) or
• Diabetes, or history of or
• Eye or vision problems or
• Heart disease (eg, cardiomyopathy, heart failure) or
• Hyperglycemia (high blood sugar) or
• Hypertension (high blood pressure) or
• Lung disease or other breathing problems or
• Stomach or bowel problems (eg, colitis, perforation)—Use with caution. May make these conditions worse.

• Dehydration or
• Hypotension (low blood pressure) or
• Kidney failure—Use with caution. May cause side effects to become worse.

Proper Use of This Medicine:

Medicines used to treat cancer are very strong and can have many side effects. Before using this medicine, make sure you understand all the risks and benefits. It is important for you to work closely with your doctor during your treatment.

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

This medicine usually comes with a patient information leaflet and patient instructions. Read and follow the instructions carefully. Ask your doctor or pharmacist if you have any questions.

Take the tablet at least 1 hour before or 2 hours after a meal.

A nurse or other trained health professional will give you or your child the oral liquid. This medicine can be given using an oral dosing syringe or feeding tube.

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  • For melanoma, non-small cell lung cancer, anaplastic thyroid cancer, solid tumors, and glioma:
    • Adults—2 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated.
    • Children 1 year of age and older—Dose is based on body weight and must be determined by your doctor.
      • Weighing 51 kilograms (kg) or more—2 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated.
      • Weighing 38 to 50 kg—1.5 mg once a day. Your doctor may adjust your dose as needed and tolerated.
      • Weighing 26 to 37 kg—1 mg once a day. Your doctor may adjust your dose as needed and tolerated.
      • Weighing less than 26 kg—Use of oral solution is recommended.
    • Children younger than 1 year of age—Use and dose must be determined by your doctor.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you miss a dose and it is less than 12 hours until your next regular dose, skip the missed dose and take your next dose at the regular time. If you miss a dose and it is more than 12 hours until your next dose, take it as soon as possible and go back to your regular dosing schedule.

Storage—

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the tablets in the refrigerator and the oral liquid at room temperature. Keep the medicine in its original bottle. Do not freeze. Protect from moisture and light.

Throw away unused oral liquid after 35 days.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it. Blood and urine tests will be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. If you are a woman who can get pregnant, your doctor may do tests to make sure you are not pregnant before starting treatment. Use an effective form of birth control to keep from getting pregnant during treatment with this medicine and for at least 4 months after the last dose. If you think you have become pregnant while using the medicine, tell your doctor right away.

Some women who use this medicine have become infertile (unable to have children). Talk to your doctor before using this medicine if you plan to have children.

This medicine may increase your risk of having cutaneous squamous cell carcinoma (cuSCC) or other skin cancers. Check with your doctor right away if you develop any skin changes, including a new wart, change in size or color of a mole, or a skin sore or reddish bump that does not heal. Your doctor may want your skin be checked for new skin lesions before treatment, every 2 months during treatment, and for up to 6 months after the last dose.

This medicine may cause bleeding problems. Tell your doctor if you have bleeding gums, coughing up blood, difficulty with breathing or swallowing, dizziness, headache, increased menstrual flow or vaginal bleeding, nosebleeds, prolonged bleeding from cuts, red or dark brown urine, or red or black, tarry stools.

This medicine may cause diarrhea, and in some cases it can be severe. Do not take any medicine to treat diarrhea without first checking with your doctor. If you have any questions about this or if mild diarrhea continues or gets worse, check with your doctor.

This medicine may cause heart problems, including heart failure. Check with your doctor right away if you have chest pain, decreased urine output, an uneven heartbeat, swelling of the face, fingers, feet, or lower legs, trouble breathing, or rapid weight gain while using this medicine.

Check with your doctor right away if eye pain or a change in vision occurs during treatment. These could be a sign of a serious eye problem. Your doctor may want your eyes be checked by an ophthalmologist (eye doctor).

Tell your doctor right away if you have a cough, trouble breathing, chest tightness, or any type of breathing problem with this medicine. These could be symptoms of a serious lung problem.

This medicine may cause fever, including severe fever reactions that can sometimes happen with low blood pressure, chills, dehydration, or kidney problems. Check with your doctor right away if you have a fever while using this medicine.

This medicine may cause serious skin reactions, including Stevens-Johnson syndrome (SJS) and drug reaction with eosinophilia and systemic symptoms (DRESS), which can be life-threatening and require immediate medical attention. Call your doctor right away if you have a rash, itching, blistering, peeling, or loosening of the skin, fever or chills, cough, sore throat, trouble breathing or swallowing, swelling of your hands, face, mouth, or throat, swollen, painful, or tender lymph glands in the neck, armpit, or groin, or yellow skin or eyes while using this medicine.

This medicine may affect your blood sugar levels. Check with your doctor right away if you have increased thirst or increased urination. If you notice a change in the results of your urine or blood sugar tests, or if you have any questions, check with your doctor.

This medicine may cause a severe inflammatory condition that could be life-threatening, including hemophagocytic lymphohistiocytosis (HLH), which is caused by an overactive immune system. Check with your doctor right away if you have a bruising, fever, skin rash, or swollen glands.

You will also need to have your blood pressure measured before starting this medicine and while you are using it. If you notice any change to your recommended blood pressure, call your doctor right away. Symptoms of high blood pressure are blurred vision, severe headache, a slow or fast heartbeat, lightheadedness, or dizziness.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

Bleeding from the rectum or bloody stools

bleeding gums

blemishes on the skin

blistering, crusting, irritation, itching, or reddening of the skin

bloating or swelling of the face, arms, hands, lower legs, or feet

bloody nose

blurred vision

chest discomfort, pain, or tightness

cracked, dry, or scaly skin

coughing up blood

decreased urine output

diarrhea

difficulty in moving

difficulty with breathing or swallowing

dilated neck veins

extreme tiredness or weakness

fast, slow, irregular, or pounding heartbeat

headache

increased menstrual flow or vaginal bleeding

irregular breathing

joint pain

lightheadedness, dizziness, or fainting

muscle aches, cramps, pain, or stiffness

nervousness

nosebleeds

paralysis

pimples

pounding in the ears

prolonged bleeding from cuts

rapid weight gain

rash

red or black, tarry stools

red or dark brown urine

redness, swelling, or pain of the skin

scaling of the skin on the hands and feet

swelling of the hands, ankles, feet, or lower legs

tingling of the hands and feet

ulceration of the skin

unusual tiredness or weakness

unusual weight gain or loss

Less common

Cough

fever

Rare

Change in vision

seeing flashes or sparks of light

seeing floating spots before the eyes, or a veil or curtain across part of your vision

stomach cramps, pain, or tenderness

watery or bloody diarrhea

Incidence not known

Blistering, peeling, loosening of the skin

chills

itching

red skin lesions, often with a purple center

sore throat

sores, ulcers, or white spots in the mouth or on lips

swollen glands

unusual bleeding or bruising

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Acne, pimples

burning, itching, and pain in hairy areas, pus at the root of the hair

canker sores

change in taste

dark urine

dry eyes

dry mouth

dry skin

itching, pain, redness, swelling, tenderness, or warmth on the skin

loosening of the fingernails

loss of taste

redness or soreness around the fingernails

sores, ulcers, or white spots on the lips or tongue or inside the mouth

swelling or inflammation of the mouth

thirst

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.