Vemurafenib (Zelboraf®)

Targeted therapy is cancer treatment that focuses on specific molecules within cancer cells. The drugs work by blocking the function of abnormal molecules to slow the growth and spread of cancer, such as melanoma.

Systemic cancer treatments, including targeted therapy, reach parts of your body through the bloodstream. Such drugs fight cancer cells that have metastasized, or spread, from the original tumor to other areas.

Vemurafenib (Zelboraf) is a drug that shrinks tumors and helps patients with advanced melanoma live longer.

What Is Vemurafenib (Zelboraf)?

Vemurafenib is a BRAF (pronounced bee-raff) 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 Vemurafenib (Zelboraf) Work?

Vemurafenib blocks the activity of a mutated protein called BRAF, a molecule that helps regulate cell growth. A BRAF mutation signals cells to develop abnormally and divide out of control. These cells grow into a melanoma tumor.

About half of all melanomas have a BRAF mutation. Vemurafenib specifically targets the V600E mutated BRAF protein. The drug interferes with abnormal BRAF signals to slow or stop the out-of-control cell growth.

Which Patients May Benefit from Vemurafenib (Zelboraf)?

The U.S. Food and Drug Administration (FDA) approved vemurafenib in 2011 to treat patients in 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)

Vemurafenib works only in patients who have tested positive for the BRAF V600E mutation. If you have advanced melanoma, your physician will have your melanoma tested for the mutation before prescribing Zelboraf. The physician will send a biopsy (sample of cancer tissue removed from your body) to a special lab for analysis.

How Is Vemurafenib (Zelboraf) Given?

Patients take vemurafenib orally (swallowing by mouth).

  • The recommended dose is 960 mg twice each day, via 240 mg tablets.
  • Depending on how you respond to treatment, your physician may adjust your dose.
  • Patients usually continue to take vemurafenib until their melanoma worsens or they experience unacceptable side effects.

What Are the Goals of Vemurafenib (Zelboraf)?

Vemurafenib works to target melanoma cells with the goals of:

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

Results from a large Phase III clinical trial showed that vemurafenib improved patient outcomes better than DTIC (dacarbazine), a chemotherapy drug.

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

What Should I Ask My Doctor About Vemurafenib (Zelboraf)?

Because every patient is different, not all treatments will work for everyone. Your physician can determine whether vemurafenib may be right for you.

If you are interested in learning more about vemurafenib, here are some questions you should ask your physicians:

  • Will my melanoma tumor be tested for BRAF genetic mutations?
  • Am I eligible for vemurafenib?
  • What is your experience with vemurafenib?
  • Is vemurafenib a good option for my melanoma treatment?
  • Is there an alternative to vemurafenib for me?
  • How successful has vemurafenib been for patients like me?
  • What are the side effects of vemurafenib?
  • Are there any clinical trials for vemurafenib 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?

Need Help Paying for Vemurafenib (Zelboraf)?

Patient Assistant Programs (PAPs) are designed so that you still have access to the treatments you need, in any financial circumstance. Learn more about the manufacturer’s patient assistance program and other options here.

Manufacturer’s Patient Assistance


Latest Treatments for Advanced Melanoma

Learn more about the latest, most effective treatments that have been approved by the FDA for treating advanced melanoma:

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Melanoma Research

The Melanoma Research Alliance is the largest, non-profit funder of melanoma research worldwide. Since 2007, we have directly funded over $131 million in innovative grants to improve prevention, detection, and treatment of melanoma. We have also leveraged an additional $415 million in outside funds for research. Learn more about our funded research.

Last updated: August, 2021