Trametinib

Name: Trametinib

Why is this medication prescribed?

Trametinib is used alone or in combination with another medication (dabrafenib [Tafinlar]) to treat a certain type of melanoma (a type of skin cancer) that cannot be treated with surgery or that has spread to other parts of the body. Trametinib is also used in combination with dabrafenib to treat a certain type of non-small-cell lung cancer (NSCLC) that has spread to nearby tissues or to other parts of the body. Trametinib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps stop the spread of cancer cells.

In case of emergency/overdose

In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

Trametinib Brand Names

Trametinib may be found in some form under the following brand names:

  • Mekinist

Other Requirements

  • Store trametinib in the refrigerator between 36°F to 46°F (2°C to 8°C). Do not freeze.
  • Keep trametinib dry and away from moisture.
  • The bottle of trametinib contains a desiccant packet to help keep your medicine dry. Do not throw away the desiccant packet.
  • Keep trametinib in its original bottle. Do not place tablets in a pill box.
  • Safely throw away trametinib that is out of date or no longer needed.
  • Keep trametinib and all medicine out of the reach of children.

Precautions While Using trametinib

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 trametinib while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant during therapy 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.

trametinib may cause fertility (ability to have children) problems in women. Talk to your doctor before using trametinib if you plan to have children.

trametinib 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, during treatment, and for up to 6 months after the last dose.

trametinib may cause bleeding problems. Tell your doctor if you have any of the following symptoms: bleeding gums, coughing up blood, difficulty in 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.

trametinib 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.

trametinib 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, troubled breathing, or rapid weight gain while using trametinib.

Check with your doctor right away if blurred vision, loss of vision, or any change in vision occurs during treatment. These could be symptoms 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 trametinib. These could be symptoms of a serious lung problem.

trametinib 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 trametinib.

Check with your doctor right away if you have a severe skin rash, acne, or redness, swelling, peeling, or tenderness of the hands or feet. These may be symptoms of a serious skin problem.

trametinib may raise your blood sugar. You should check your blood sugar more often during the first month you take trametinib, and then on a regular basis if you have diabetes or a history of high blood sugar.

You will also need to have your blood pressure measured before starting trametinib 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.

Uses of Trametinib

  • It is used to treat skin cancer.
  • It is used to treat lung cancer.

Pharmacologic Category

  • Antineoplastic Agent, MEK Inhibitor

Monitoring Parameters

BRAF V600K or V600E mutation status (prior to treatment); CBC and liver function tests at baseline and periodically; assess LVEF (by echocardiogram or MUGA scan) at baseline, 1 month after therapy initiation, and then at 2- to 3-month intervals; ophthalmological evaluation periodically during treatment and with visual disturbances; monitor for signs/symptoms of pulmonary toxicity (eg, cough dyspnea, hypoxia, pleural effusion, or infiltrates); monitor for dermatologic toxicity and secondary skin infections; blood pressure; diarrhea; signs/symptoms of bleeding, colitis, and GI perforations.

For patients receiving combination therapy with dabrafenib: Blood glucose (baseline and periodically in patients with preexisting diabetes or hyperglycemia); dermatologic exams should be performed prior to treatment initiation, every 2 months while receiving combination treatment, and for up to 6 months following therapy discontinuation. Monitor for signs/symptoms of cutaneous and noncutaneous malignancies and uveitis/iritis.

Monitor adherence.

For Healthcare Professionals

Applies to trametinib: oral tablet

General

Rash and decreased LVEF were the most common reasons cited for dose reductions of trametinib.

The most common adverse reactions resulting in permanent discontinuation of trametinib were decreased left ventricular ejection fraction (LVEF), pneumonitis, renal failure, diarrhea, and rash.[Ref]

Cardiovascular

Very common (10% or more): Lymphedema (43%), hypertension (15%), hemorrhage (13%)
Frequency not reported: Bradycardia[Ref]

Dermatologic

Very common (10% or more): rash (57%), dermatitis acneiform (19%), dry skin (11%), pruritus (10%), paronychia (10%)
Frequency not reported: Folliculitis, rash pustular, cellulitis[Ref]

Gastrointestinal

Very common (10% or more): Diarrhea (43%), stomatitis (15%), abdominal pain (13%)
Frequency not reported: Xerostomia[Ref]

Hematologic

Very common (10% or more): Anemia (38%)[Ref]

Hepatic

Very common (10% or more): Increased aspartate aminotransferase (AST) (60%), Increased alanine aminotransferase (ALT) (39%)[Ref]

Metabolic

Very common (10% or more): Hypoalbuminemia (42%), increased alkaline phosphatase (24%)[Ref]

Musculoskeletal

Frequency not reported: Rhabdomyolysis[Ref]

Nervous system

Frequency not reported: Dizziness, dysgeusia[Ref]

Ocular

Frequency not reported: Vision blurred, dry eye[Ref]

Some side effects of trametinib may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Liver Dose Adjustments

Mild Liver Dysfunction: No adjustment recommended
Moderate to Severe Liver Dysfunction: An appropriate dose has not been established.

Trametinib Side Effects

More common side effects

rash

  • diarrhea

  • swelling of your arms and legs

More common side effects

The more common side effects of trametinib with dabrafenib can include:

  • fever

  • nausea

  • vomiting

  • rash

  • chills

  • diarrhea

  • high blood pressure

  • swelling in your feet, ankles, or legs

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.

Serious side effects

Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

  • Increased bleeding. Symptoms can include:

    • headaches, dizziness, or weakness
    • coughing up blood or blood clots
    • vomit that contains blood or looks like coffee grounds
    • red or black stools that look like tar
    • nosebleeds
    • bleeding from your gums
    • red or pink urine
  • Blood clots. Symptoms can include:

    • chest pain
    • sudden shortness of breath or breathing trouble
    • swelling in your arms or legs
    • a cool and pale arm or leg
    • pain in your legs with or without swelling
  • Heart problems. Symptoms can include:

    • feeling like your heart is pounding or racing
    • shortness of breath
    • swelling in your ankles and feet
    • lightheadedness
  • Eye problems. Symptoms can include:

    • blurry vision
    • vision loss
    • seeing colored dots
    • seeing halos (blurred outline around objects)
    • eye pain, swelling, or redness
  • Lung or breathing problems. Symptoms can include:

    • shortness of breath
    • cough
  • Fever. Symptoms can include:

    • chills
    • dehydration, which can cause:
      • extreme thirst
      • dry mouth
      • dry skin
      • decreased urination
    • low blood pressure
    • dizziness
  • Skin reactions. Symptoms can include:

    • a rash that bothers you or doesn’t go away
    • acne
    • skin redness
    • redness, swelling, peeling, or tenderness of your hands or feet
  • Colitis or perforation of the GI tract. Symptoms can include:

    • abdominal pain or cramping
    • bloating in your abdomen
    • weight loss
    • diarrhea with or without blood
    • blood in your stool
    • urgent need for a bowel movement
    • chills or fever
    • vomiting
    • nausea
Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.
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