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Zelboraf (vemurafenib)

Zelboraf® (vemurafenib) is used to treat 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 unresectable or metastatic melanoma.

Vemurafenib can be used alone, or it may be used together with a drug called Cotellic® (cobimetinib).

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 10% of melanomas that develop on sun-exposed skin.2 BRAF mutations are found in 50% of melanomas that occur in skin that rarely has sun exposure.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.

Cotellic is a drug that inhibits a protein called MEK. Vemurafenib and Cotellic 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

How do I take 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.1 Do not crush or chew the tablet. Take Vemurafenib twice a day, 12 hours apart. You can take it with or without food.

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 another type of skin cancer called squamous cell carcinoma. 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.

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 a complete list of adverse effects

Who should not take Vemurafenib?

Pregnant women should not take Vemurafenib.1 Women who could become pregnant should use birth control during treatment and for at least 2 weeks after the last dose. Do not breastfeed while taking Vemurafenib or for 2 weeks after the last dose.

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 makes 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.

During treatment and for at least 2 weeks after the last dose of Vemurafenib:1

  • Women who can become pregnant should use birth control.
  • Women should not breastfeed.
Written by: Sarah O'Brien | Last reviewed: June 2019.
  1. Zelboraf® [prescribing information]. South San Francisco, CA: Genentech; September 2016.
  2. Lovly C, Pao W, Sosman J. 2016. Molecular Profiling of Melanoma. My Cancer Genome https://www.mycancergenome.org/content/disease/melanoma/ (Updated January 26).
  3. Lo JA, Fisher DE. The melanoma revolution: from UV carcinogenesis to a new era in therapeutics. Science. 2014;346:945-949.
  4. NCCN Clinical Practice Guidelines in Oncology. Melanoma. Version 1.2017. Published November 10, 2016. https://www.nccn.org/professionals/physician_gls/pdf/melanoma.pdf
  5. Sosman JA, Kim KB, Schuchter L, et al. Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med. 2012;366:707-714.
  6. Chapman PB, Hauschild A, Robert C, et al; BRIM-3 Study Group. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med. 2011;364:2507-2516.
  7. McArthur GA, Maio M, Arance A, et al. Vemurafenib in metastatic melanoma patients with brain metastases: An open-label, single-arm, phase 2, multicentre study. Ann Oncol. 2016 Dec 19.