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Class: Biological Therapy
**Generic Name:**Trametinib
**Trade Name:**MEKINIST®

For which conditions is MEKINIST approved for? MEKINIST is indicated for the treatment of patients with unresectable (unable to be removed with surgery) or metastatic melanoma with a specific type of BRAF mutation (BRAF V600E or V600K), as detected by an FDA-approved test.

What is the mechanism of action? MEKINIST is a kinase inhibitor. These drugs work by blocking the action of enzymes called kinases, which are involved in many cell functions, including cell signaling, growth, and division. These enzymes may be too active or found at high levels in some types of cancer cells and blocking them may help keep cancer cells from growing. Specifically, MEKINIST targets kinases called mitogen-activated extracellular signal-regulated kinase 1 and 2 (MEK1 and MEK2), which are involved in cell growth in metastatic melanoma with BRAF V600E or V600K mutations.

How is **MEKINIST typically given (administered)?**MEKINIST is approved to be given as a single agent and in combination with the drug TAFINLAR® (dabrafenib), also a kinase inhibitor. As a single agent, the recommended dosage of MEKINIST is 2 mg orally once daily. In combination with TAFINLAR, the recommended dosage is 150 mg orally twice daily. Take MEKINIST at least 1 hour before or at least 2 hours after a meal.

How are patients typically monitored?

Because MEKINIST can cause new or worsening high blood pressure (hypertension), your healthcare provider should check your blood pressure regularly during treatment with MEKINIST. Some people may develop high blood sugar or worsening diabetes during treatment with MEKINIST in combination with TAFINLAR. If you are diabetic and receiving MEKINIST plus TAFINLAR, your healthcare provider should check your blood sugar levels closely during treatment.

What are the common (occur in 20% or more of patients) side effects of treatment withMEKINIST as a single agent?

  • Rash
  • Diarrhea
  • Lymphedema

What are the common (occur in 20% or more of patients) side effects of treatment withMEKINISTin combination with TAFINLAR?

  • Fever
  • Chills
  • Fatigue
  • Rash
  • Nausea
  • Vomiting
  • Diarrhea
  • Abdominal pain
  • Peripheral edema
  • Cough
  • Headache
  • Joint pain
  • Night sweats
  • Decreased appetite
  • Constipation
  • Pain in a muscle or group of muscles

This is not a complete list of side effects. Some patients may experience other side effects that are not listed here. Patients may wish to discuss with their physician the other less common side effects of this drug, some of which may be serious.

Some side effects may require medical attention. Other side effects do not require medical attention and may go away during treatment. Patients should check with their physician about any side effects that continue or are bothersome.

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What can patients do to help alleviate or prevent discomfort and side effects?

Tell your doctor if you have or have had any medical condition, with special attention to the following:

  • Bleeding problems or blood clots
  • Heart problems
  • Eye problems
  • Lung or breathing problems
  • High blood pressure (hypertension)
  • Liver or kidney problems

Also tell your doctor is you are pregnant or plan to become pregnant. MEKINIST can harm your unborn baby, and women who are able to become pregnant should use effective birth control during treatment and for four months after stopping treatment. If you’re taking MEKINIST with TAFINLAR, be aware that birth control using hormones (such as birth control pills, injections, or patches) may not work as well with this combination, so use another effective method of birth control. Tell you doctor if you are breastfeeding or plan to breastfeed; it is not known if MEKINIST passes into your breast milk, so you should not take this drug while breastfeeding.

Take MEKINIST one time a day exactly as your healthcare provider tells you to take it. Do not change your dose or stop MEKINIST unless your healthcare provider tells you. If you miss a dose, take it as soon as you remember. If it is within 12 hours of your next scheduled dose, skip the missed dose and take the next dose at your regular time. If you take too much MEKINIST, call your healthcare provider or go to the nearest hospital emergency room right away.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Are there any special precautions patients should be aware of before starting treatment?

Because MEKINIST can cause fetal harm if taken during pregnancy, female patients should use highly effective contraception during treatment and for four months after treatment. Patients take MEKINIST in combination with TAFINLAR should use a highly effective non-hormonal method of contraception. If you do become pregnant during treatment with MEKINIST, contact your healthcare provider immediately.

When should patients notify their physician?

Tell your doctor if you experience any side effects that bother you or don’t go away. Also call your healthcare provider right away if:

  • You develop high blood pressure, your blood pressure worsens, or you have severe headache, lightheadedness, or dizziness.
  • You have symptoms of severe high blood sugar, such as increased thirst urinating more often than normal, or urinating an increased amount of urine.
  • You have symptoms of a heart problem, including feeling like your heart is pounding or racing, shortness of breath, swelling of your ankles and feet, or feeling lightheaded.
  • You have signs of a blood clot, including chest pain, sudden shortness of breath or trouble breathing, pain in your legs with or without swelling, swelling in your arms or legs, a cool or pale arm or leg
  • You have unusual signs of bleeding, such as: headaches or dizziness; if you feel weak, cough up blood or blood clots, vomit blood; your vomit looks like coffee grounds; or your stools red or black stools and look like tar
  • You any new lesions, changes to existing lesions on their skin, or other signs and symptoms of malignancies
  • You develop rash or fever

What is a package insert?

A package insert is required by the FDA and contains a summary of the essential scientific information needed for the safe and effective use of the drug for healthcare providers and consumers. A package insert typically includes information regarding specific indications, administration schedules, dosing, side effects, contraindications, results from some clinical trials, chemical structure, pharmacokinetics and metabolism of the specific drug. By carefully reviewing the package insert, you will get the most complete and current information about how to safely use this drug. If you do not have the package insert for the drug you are using, your pharmacist or physician may be able to provide you with a copy.