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Zelboraf (vemurafenib)

Zelboraf® (vemurafenib) is used to treat certain forms of advanced melanoma with a mutation called BRAF V600E. Your doctor will test for BRAF mutation. Vemurafenib is not used for melanoma with a normal BRAF gene.

Vemurafenib is used when the melanoma:1

  • Cannot be removed with surgery (unresectable) or
  • Has spread to distant parts of the body (metastasized)

Vemurafenib does not come in generic form. Vemurafenib is similar to Tafinlar® (dabrafenib), another drug that is approved to treat certain forms of melanoma.

Vemurafenib can be used alone, or it may be used together with a drug called Cotellic® (cobimetinib). Vemurafenib and cobimetinib targeted therapies may also be used in combination with Tecentriq® (atezolizumab) immunotherapy for metastatic or unresectable melanoma that has the BRAF V600 mutation.

How does vemurafenib work?

Vemurafenib is a type of medication called a kinase inhibitor. It works by blocking certain proteins that pass along signals for cell growth. One of the proteins is called BRAF. Mutations in the gene (instructions) for BRAF are found in approximately one third of melanoma cases.2

BRAF proteins have a role in a pathway called MAPK (also called ERK). These proteins are part of a chain of events that allow cells to grow and survive. Normally, there are mechanisms that turn each protein “on” and “off,” keeping the cell processes under control. Certain mutations cause BRAF to stay “on,” sending continuous signals for uncontrolled cell growth.3

Vemurafenib turns the BRAF protein off. It is called a targeted therapy because it targets one feature that makes cancer cells different from normal cells.

Cobimetinib is a drug that inhibits a protein called MEK. Vemurafenib and cobimetinib are sometimes used together to target the MAPK pathway at two points. Some patients have better results with combination treatment than with Vemurafenib alone.4

Receiving vemurafenib

Before taking Vemurafenib, read the Medication Guide that comes in the package. Follow your doctor’s instructions for taking Vemurafenib.

Vemurafenib comes as a tablet that you take by mouth. Based on your doctor’s instructions, you will continue taking Vemurafenib until the cancer progresses or the side effects are unacceptable.1

Patients should take their medication as prescribed by their doctor. Patients should talk to their doctor if they have any questions, or if they have questions regarding their vemurafenib regimen.

What are the side effects of Vemurafenib?

Taking Vemurafenib can cause other cancers.1 It has been linked to other types of skin cancer called cutaneous squamous cell carcinoma and keratoacanthoma. It also may cause squamous cell carcinoma in locations other than the skin. Some people have developed new melanoma lesions while taking Vemurafenib. Possible signs of new cancers include: new wart, skin sore, reddish bump, or mole that changes in size or color (patients should tell their doctor if they notice any of these skin changes).

The most common side effects of Vemurafenib include:1

  • Joint pain
  • Rash (can be severe)
  • Hair loss
  • Tiredness
  • Sensitivity to the sun and sunburn
  • Nausea
  • Itching
  • Warts

Less common but serious side effects include allergic reactions, severe skin reactions, changes in your heart rhythm, liver or kidney damage, or eye problems. This is not an exhaustive list of all potential side effects of vemurafenib. Talk to your healthcare provider or pharmacist for further information.

Who should not take Vemurafenib?

If you are pregnant, plan to become pregnant, or are breastfeeding or plan to breastfeed, talk with your doctor. Vemurafenib can cause harm to a developing fetus and should not be taken by women who are pregnant.1 While receiving Vemurafenib, females who can become pregnant should use contraceptives during treatment and for a period of time after completing treatment (patients should discuss appropriate birth control methods, and how long they need to use them, with their doctor). Females should not breastfeed during Vemurafenib treatment and for a period of time following the final dose (patients should discuss breastfeeding considerations with their doctor).

Tell your doctor about any other medical conditions you have, especially:1

  • Heart problems
  • Liver problems
  • Kidney problems
  • Low levels of potassium, calcium, or magnesium in your blood

Tell your doctor if you have had or are planning to have radiation therapy.

What precautions are needed when taking Vemurafenib?

Regular skin exams are needed while taking Vemurafenib.1 Your doctor will do a skin exam before you start this medication. You will need skin exams every 2 months while taking Vemurafenib and for up to 6 months afterward. Your doctor will also look for non-skin cancers.

Try to avoid sunlight while taking Vemurafenib.1 This medication may make your skin sensitive to sunlight and you may burn more easily. If you are outside, wear a wide-brimmed hat and long clothing. Use sunscreen and lip balm with a sun protection factor (SPF) of 30 or more.

Before starting treatment with vemurafenib, patients should tell their doctor about all medications (prescription and over-the-counter), herbal supplements, and vitamins they are taking.

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Written by: Sarah O'Brien | Last reviewed: February 2021.