Drug Information



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Brand Name
Mekinist
Common Name
trametinib
How does this medication work? What will it do for me?

Trametinib belongs to the group of cancer-fighting medications known as antineoplastics, and specifically to the family of medications called protein kinase inhibitors. It is used alone or with the medication dabrafenib to treat a specific type of melanoma (skin cancer) that cannot be surgically removed or has metastasized (spread to other parts of the body). It is also used after surgery to remove melanoma and to help prevent the melanoma from coming back. Trametinib is also used in combination with dabrafenib to treat non-small cell lung cancer that has metastasized.

Trametinib is not appropriate for all types of melanoma or non-small cell lung cancer. It will only interfere with the growth of skin cancer cells that have a particular genetic mutation, called BRAF. Your doctor will check for this mutation before prescribing trametinib.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

How should I use this medication?

The recommended adult dose of trametinib is 2 mg taken once a day. This medication should be taken at the same time every day and should be swallowed with a full glass of water.

Food can affect the way trametinib is absorbed into the body. Take this medication on an empty stomach one hour before or two hours after eating.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor. If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication in its original bottle with the desiccant in the refrigerator. Protect it from light and moisture, and keep it out of the reach of children.

What form(s) does this medication come in?

0.5 mg
Each yellow, modified oval, biconvex, film-coated tablet with "GS" debossed on one face and "TFC" on the other contains 0.5 mg of trametinib. Nonmedicinal ingredients: croscarmellose sodium, hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, silicon dioxide (colloidal), and sodium lauryl sulphate; coating: hypromellose, polyethylene glycol, iron oxide yellow, and titanium dioxide.

0.5 mg tablets may also appear as yellow, ovaloid, biconvex, unscored, film-coated, bevelled-edge tablets with the Novartis logo on one side and "TT" on the other side.

2 mg
Each pink, round, biconvex, film-coated tablet with "GS" debossed on one face and "HMJ" on the other contains 2 mg of trametinib. Nonmedicinal ingredients: croscarmellose sodium, hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, silicon dioxide (colloidal), and sodium lauryl sulphate; coating: hypromellose, polyethylene glycol, iron oxide red, polysorbate 80, and titanium dioxide.

2 mg tablets may also appear as pink, round, biconvex, unscored, film-coated, bevelled-edge tablets with the Novartis logo debossed on one side and "LL" on the other side.

Who should NOT take this medication?

Do not take this medication if you are allergic to trametinib or any ingredients of the medication.

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • constipation
  • cough
  • decreased appetite
  • diarrhea
  • dry mouth
  • hair loss or thinning
  • headache
  • increased sensitivity of the skin to light
  • lack of energy
  • mouth sores
  • nausea
  • nosebleeds
  • pain or peeling skin of the hands or feet
  • stomach ache
  • sweating
  • swelling hands or feet
  • vomiting
  • weakness/tiredness
  • weight changes

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • acne-like rash
  • changes in blood pressure
  • changes to fingernails and toenails (e.g., pain, infection, swelling)
  • dehydration (e.g., decreased urine, dry skin, dry and sticky mouth, sleepiness, dizziness, headache, thirst, confusion)
  • dry, chapped, and cracked or itching skin
  • facial swelling
  • fast, slow, or pounding heartbeat
  • flu-like symptoms (e.g., tiredness, chills, sore throat, joint or muscle aches)
  • signs of anemia (low red blood cells; e.g., dizziness, pale skin, unusual tiredness or weakness, shortness of breath)
  • signs of bleeding (e.g., bloody nose, blood in urine, coughing blood, bleeding gums, cuts that don't stop bleeding)
  • signs of decreased levels of sodium in the body (e.g., tiredness, confusion, muscle twitching, seizures)
  • signs of heart failure (e.g., fast, irregular heartbeat or pulse, dizziness, difficulty breathing, swollen legs, feet)
  • signs of infection (symptoms may include fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness)
  • signs of inflammation of the lungs (e.g., shortness of breath and cough)
  • signs of muscle damage (e.g., muscle pain, tenderness or weakness, or brown or discoloured urine), especially if you also have a fever or a general feeling of being unwell
  • skin changes (e.g., rash, discolouration, thickening, infection, warts, pus-filled blisters)
  • skin sore, wart, or bump that does not heal
  • skin rash
  • symptoms of high blood sugar (excessive thirst or hunger, excessive urination, weight loss, tiredness)
  • symptoms of immune system problems (HLH; fever, swollen glands, bruising, rash, enlarged liver or spleen, kidney or heart problems)
  • symptoms of kidney problems (e.g., rash, itchiness, confusion, puffiness or swelling in feet, ankles, face, or hands, decreased urination, weight gain)
  • symptoms of sarcoidosis (inflammatory disease caused by overproduction of white blood cells; cough, shortness of breath, swollen lymph nodes, vision changes, fever, fatigue, joint pain or swelling, tender bumps under the skin)
  • urinary tract infection (e.g., pain when urinating, urinating more often than usual, low back or flank pain)
  • vision changes (coloured dots, halos around objects, blurred or reduced vision)

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • signs of bleeding in the stomach (e.g., bloody, black, or tarry stools; spitting up of blood; vomiting blood or material that looks like coffee grounds)
  • signs of a blood clot in the arm or leg (tenderness, pain, swelling, warmth, or redness in the arm or leg) or lungs (difficulty breathing, sharp chest pain that is worst when breathing in, coughing, coughing up blood, sweating, or passing out)
  • signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
  • signs of pancreatitis (e.g., abdominal pain on the upper left side, back pain, nausea, fever, chills, rapid heartbeat, swollen abdomen)
  • symptoms of kidney inflammation (e.g., changed urine output, drowsiness, confusion, nausea)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Birth control: Women taking this medication who could become pregnant must use effective birth control while taking trametinib and for 16 weeks after the last dose. When trametinib is taken along with the medication dabrafenib, birth control pills, patches, and injections are not as effective and other birth control methods must be used. Men taking this medication who have partners who are or may become pregnant should use condoms with spermicide as birth control while taking this medication and for 16 weeks after taking the last dose.

Bleeding: Trametinib may increase your risk of bleeding. If you have a history of coughing up blood, brain bleeds, or bleeding from the stomach, discuss with your doctor how this medication may affect your medical condition. If you notice signs of serious bleeding, such as vomiting blood or a coffee grounds-like substance, or bleeding from the rectum, get immediate medical attention.

Blood clots: This medication appears to increase the risk of developing blood clots. These blood clots may form anywhere in the body, but are more noticeable when they occur in the large muscles, lung, brain (stroke), or heart (heart attack). If you experience pain in the chest or leg, unexplained shortness of breath, fast and irregular heartbeat, severe headache, blurred vision, or slurred speech, get immediate medical attention.

Diabetes: Trametinib may cause increases in blood sugar levels. If you have diabetes, monitor your blood sugar frequently as recommended by your doctor. If you experience symptoms of high blood sugar (e.g., increased urination, increased thirst, increased eating, and weakness) while taking this medication, contact your doctor.

Eye problems: There have been rare reports of retinal detachment and retinal vein occlusion (blockage of the vein draining the eye) from people taking trametinib. If you notice any changes in your vision such as coloured dots, halos, or blurred vision, contact your doctor immediately.

Gastrointestinal problems: Rarely, trametinib can cause inflammation of the digestive tract (colitis) or perforation of the stomach or intestines. If you experience severe abdominal pain, fever, vomiting, nausea, or black and tarry stools, contact your doctor immediately.

Heart problems: Trametinib may cause the heart to become less effective in pumping blood out into the body. It may also cause severely decreased heart rate. If you have a history of heart disease or are at risk of developing heart disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

If you experience signs of decreased heart function, like a change in heartbeat or pulse, chest pain, difficulty breathing, unusual tiredness, or swelling in the legs, feet, or hands, contact your doctor as soon as possible.

High blood pressure: Trametinib may increase your blood pressure. Your doctor will monitor your blood pressure while you are taking this medication.

Immune system: There have been reports of trametinib causing the immune system to overreact, causing increased numbers of certain white blood cells to be produced. This can cause collections of these cells in certain areas of the body, such as the lymph nodes, or damage to organs in the body. Your doctor will monitor the number of blood cells in the body, but if you notice any unusual swelling or lumps, talk to your doctor as soon as possible.

Infection: As with other medications used to treat cancer, trametinib can cause a decrease in the number of white blood cells, the cells responsible for fighting infection in the body. Your doctor will have you go for regular blood work to monitor your white blood cells, however if you notice that you are getting infections more often, talk to your doctor as soon as possible.

Lungs: This medication is known to cause serious lung and breathing problems. The resulting damage to the lungs can be fatal. If you experience any new or worsening cough or shortness of breath while using this medication, contact your doctor immediately. Your doctor may order a chest X-ray before you start using this medication to use as a baseline in case you develop breathing problems.

Muscle effects:  Muscle damage has been associated with the use of trametinib. Report any unexplained muscle pain, tenderness, weakness or cramps, or any brown or discoloured urine to your doctor immediately, particularly if you are also experiencing malaise (a general feeling of being unwell) or fever.

Skin problems: This medication can cause additional skin problems such as rash, skin ulcers that may become infected, and other skin redness and irritation. These reactions can lead to serious problems. Let your doctor know as soon as possible if you develop any skin reactions while you are taking trametinib.

Vision changes: This medication may cause changes to the sharpness of your vision and possibly cause vision loss. Vision loss can occur slowly or suddenly. People with high blood pressure, diabetes, high blood cholesterol, or glaucoma are at a higher risk of vision loss. Your doctor may order an eye exam before you start taking trametinib. If you notice any change in your vision such as colour dots, a blurred outline around objects (halo), or blurred vision while you are taking trametinib, contact your doctor immediately.

Pregnancy: This medication may cause harm to an unborn child and should not be used during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately. People of childbearing age who are taking trametinib should use an effective method of birth control such as condoms during treatment and for 4 months after stopping the medication.

Breast-feeding: It is not known if trametinib passes into breast milk. If you are breast-feeding and taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of using this medication have not been established for children.

What other drugs could interact with this medication?

There may be an interaction between trametinib and any of the following:

  • amiodarone
  • beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
  • dabrafenib
  • desmopressin
  • digoxin
  • diltiazem
  • HIV protease inhibitors (e.g., atazanavir, ritonavir)
  • procainamide
  • sotalol
  • sphingosine 1-phosphate (S1P) receptor inhibitors (e.g., fingolimod, ponesimod, siponimod)
  • verapamil

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

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