Trametinib (Mekinist®)

Cancer specialists have found new ways to fight melanoma with drugs that target certain abnormal molecules within cancer cells. Targeted therapy helps control the growth of melanoma tumors by blocking the activity of abnormal molecules. 

The drugs are systemic because they reach parts of the body through the bloodstream. As a systemic treatment, targeted therapy is effective in fighting metastatic cancer, which has spread from the original tumor to other areas.

Trametinib (Mekinist) shrinks tumors and helps patients with advanced melanoma live longer.

What Is Trametinib (Mekinist)?

Trametinib is a MEK inhibitor, which:

  • Is a type of targeted therapy known as a signal transduction inhibitor
  • Helps slow or stop the growth and spread of melanoma cells

How Does Trametinib (Mekinist) Work?

Trametinib blocks the activity of a protein called MEK, a molecule that helps regulate cell growth. MEK is part of a signaling pathway that includes BRAF, another protein. A BRAF mutation signals cells, via MEK, to develop abnormally and divide out of control. These cells grow into a melanoma tumor.

About half of all melanomas have a BRAF mutation. Trametinib acts on melanomas that have the V600E or V600K mutations in the BRAF protein. The drug interferes with abnormal BRAF signals to slow or stop the out-of-control cell growth.

Which Patients May Benefit from Trametinib (Mekinist)?

In 2013, the U.S. Food and Drug Administration (FDA) approved trametinib to treat patients who have advanced stages of melanoma:

  • Stage III that is unresectable (unable to be completely removed by surgery)
  • Stage IV, also known as metastatic (melanoma cells that have spread to organs and other parts of the body)

If you have advanced melanoma, your physician will test your melanoma for specific genetic mutations before prescribing trametinib. The physician will send a biopsy (sample of cancer tissue removed from your body) to a special lab for analysis. Trametinib:

  • Works only in patients who have tested positive for the BRAF V600E or V600K mutation
  • Cannot be used to treat patients who have already tried another BRAF inhibitor

How Is Trametinib (Mekinist) Given?

Patients take trametinib orally (swallowing by mouth).

  • The recommended dose is 2 mg once each day, via 0.5, 1 or 2 mg tablets.
  • Depending on how you respond to treatment, your physician may adjust your dose.
  • Patients usually continue to take trametinib until their melanoma worsens or they experience unacceptable side effects.

What Are the Goals of Trametinib (Mekinist)?

The goals of using trametinib include:

  • Slowing the growth or spread of melanoma
  • Shrinking melanoma tumors
  • Helping patients live longer

Results from a large Phase III clinical trial showed that trametinib provided better outcomes for patients than chemotherapy. However, melanoma experts consider trametinib to be less effective by itself than either BRAF inhibitor (vemurafenib or dabrafenib).

Melanoma treatments, like trametinib, have side effects, which can sometimes be serious. Patients should talk with their physician to learn more about the side effects of trametinib and other melanoma treatment options.

What Should I Ask My Doctor About Trametinib (Mekinist)?

It’s important to keep in mind that not all treatments work for all patients. If you are interested in learning more about trametinib, here are some questions you should ask your physicians:

  • Will I be tested for BRAF genetic mutations?
  • Am I eligible for trametinib?
  • What is your experience with trametinib?
  • Is trametinib a good option for my melanoma treatment?
  • Is there an alternative to trametinib for me?
  • How successful has trametinib been for patients like me?
  • What are the side effects of trametinib?
  • Are there any clinical trials for trametinib that I should consider?
  • What other treatments are FDA-approved for treating advanced melanoma?
  • What are the risks and benefits of the available treatment options?
  • What are the goals for my treatment?

Latest Treatments for Advanced Melanoma

Since 2011, the FDA has approved several effective treatments for patients who have advanced melanoma. Learn more about:

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Melanoma Research

Since its founding in 2007, the Melanoma Research Alliance has awarded over $88 million to research aimed at better preventing, diagnosing and treating melanoma. Learn more about our funded research.

Last reviewed: May 2016

Reviewers: Paul Chapman, Antoni Ribas, Louise Perkins

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