Zelboraf (Vemurafenib) – Oral

Warning:

Zelboraf (vemurafenib) has the potential of causing new skin cancers to develop. These are called cutaneous squamous cell carcinoma, and keratocanthoma. Notify your healthcare team if you have any new skin lesions that develop, such as warts, nonhealing ulcers, or a change in any moles.

What Is Zelboraf?

Zelboraf (vemurafenib) is an oral medication used to treat melanoma (a type of skin cancer) with a BRAF V600E mutation that cannot be removed with surgery. It can also be used to treat a rare type of blood cancer called Erdheim-Chester disease, which has a BRAF V600 mutation.

A BRAF mutation is a mutation in a cancer cell that causes the cell to grow quickly and out of control. 

Zelboraf is available in tablet form.

Drug Facts

Generic Name: Vemurafenib

Brand Name: Zelboraf

Drug Availability: Prescription

Therapeutic Classification: Antineoplastic agent

Available Generically: No

Controlled Substance: N/A

Administration Route: Oral

Active Ingredient: Vemurafenib

Dosage Form: Tablet

What Is Zelboraf Used For?

The Food and Drug Administration (FDA) approved Zelboraf to treat two types of cancers: melanoma and Erdheim-Chester disease. 

For Zelboraf to be used for melanoma, the cancer has to have a BRAF V600E mutation and be too advanced to be removed by surgery. Your healthcare provider will use a special test to look for this mutation.

Zelboraf can also treat Erdheim-Chester disease if a BRAF V600 mutation is present. In this disease, a type of white blood cell (histiocytes) is overproduced. Having too many histiocytes causes inflammation in the body, which can then lead to scarring and organ damage.

Zelboraf (Vemurafenib) Drug Illustration - Illustration by Zoe Hansen

Verywell / Zoe Hansen

How to Take Zelboraf

Zelboraf needs to be taken twice a day, about 12 hours apart. It can be taken with or without food. Swallow the tablets whole. Do not crush or chew them.

Storage

Zelboraf tablets should be kept in their original packaging. Do not put them in a pill box or planner. Keep them at room temperature (between 68 and 77 degrees Fahrenheit), with the lid closed tightly.

Off-Label Uses

In some instances, Zelboraf may be used off-label, meaning it is used for a condition that it doesn’t have the initial approval for. The most common use of Zelboraf off-label is for cancer that has a BRAF V600 mutation that isn’t being treated well by current medications or other therapy.

How Long Does Zelboraf Take to Work?

Once you start taking Zelboraf, the medication will be absorbed and start working to stop the cancer growth. Imaging tests will likely be done a few months after starting Zelboraf to see if the medication is working.

What Are the Side Effects of Zelboraf?

This is not a complete list of side effects and others may occur. A medical professional can advise you on side effects. If you experience other effects, contact your pharmacist or a medical professional. You may report side effects to the FDA at www.fda.gov/medwatch or 800-FDA-1088.

Common Side Effects

Taking Zelboraf comes along with the risk of potential side effects. The most common side effects from taking Zelboraf include:

Severe Side Effects

If you’re experiencing any side effects that are severe, notify your healthcare team. Call 911 if you feel your symptoms are life-threatening or if you’re having a medical emergency. Serious side effects and their symptoms can include the following:

  • New skin cancers: Changes in moles, new warts growing, nonhealing areas on skin
  • Severe allergic reaction: Face or tongue swelling, trouble breathing, tightness in throat
  • Skin reactions: Blistering, skin peeling, redness to the skin, sores in the mouth
  • Changes to heart electrical activity: Dizziness, feeling faint, irregular heartbeat
  • Liver problems: Dark urine, yellowing to the skin or eyes, nausea, vomiting
  • Eye problems: Vision changes, blurriness, eye pain, eye swelling
  • Kidney problems

Long-Term Side Effects

If any of the above side effects become severe, they could lead to long-term side effects. There are not currently any reported long-term side effects to Zelboraf specifically.

Report Side Effects

Zelboraf may cause other side effects. Call your healthcare provider if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your provider may send a report to the FDA's MedWatch Adverse Event Reporting Program or by phone (800-332-1088).

Dosage: How Much Zelboraf Should I Take?

Drug Content Provided and Reviewed by IBM Micromedex®

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablet):
    • For melanoma or Erdheim-Chester Disease:
      • Adults—960 milligrams (mg) (four 240 mg tablets) two times a day. The first dose should be taken in the morning, and the second dose in the evening. The 2 doses should be taken 12 hours apart. Your doctor may adjust your dose as needed and tolerated.
      • Children—Use and dose must be determined by your doctor.

Modifications

The dose of Zelboraf may need to be changed or modified if any severe side effects develop.

Missed Dose

If a dose of Zelboraf is missed, it can be taken up to four hours before the next scheduled dose. It should not be taken less than four hours before the next dose.

Overdose: What Happens If I Take Too Much Zelboraf?

There is not currently any documented amount of Zelboraf to call an overdose. If you have taken too much Zelboraf, call your healthcare team for instructions.

What Happens If I Overdose on Zelboraf?

If you think you or someone else may have overdosed on Zelboraf, call a healthcare provider or the Poison Control Center (800-222-1222).

If someone collapses or isn't breathing after taking Zelboraf, call 911 immediately.

Precautions

Drug Content Provided and Reviewed by IBM Micromedex®

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly. Blood tests and an ECG (electrocardiogram) may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control during treatment with this medicine and for 2 weeks after the last dose. If you think you have become pregnant while using this medicine, tell your doctor right away.

This medicine may increase your risk of having new skin cancers such as cutaneous squamous cell carcinoma, keratoacanthoma, and melanoma. It may also cause other cancers like noncutaneous squamous cell carcinoma of the head and neck and myeloid neoplasm. This is more likely to occur if you are more than 65 years of age, have too much sun exposure, or have a history of skin cancer. Your doctor may want to check for new skin lesions before treatment and every 2 months while you are using this medicine.

This medicine may cause serious types of allergic reactions, including anaphylaxis and drug reaction with eosinophilia and systemic symptoms (DRESS syndrome). Anaphylaxis can be life-threatening and requires immediate medical attention. Call your doctor right away if you have a rash, itching, hoarseness, lightheadedness or dizziness, trouble breathing, trouble swallowing, or any swelling of your hands, face, or mouth after using this medicine.

Serious skin reactions can occur with this medicine. Check with your doctor right away if you have blistering, peeling, or loosening of the skin, red skin lesions, severe acne or skin rash, sores or ulcers on the skin, or fever or chills with this medicine.

This medicine may cause changes to your heart rhythm, such as a condition called QT prolongation. Contact your doctor right away if you feel dizzy or faint, or have fast, pounding, or uneven heartbeats.

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, vomiting, or yellow eyes or skin. These could be symptoms of a serious liver problem.

This medicine may make your skin more sensitive to sunlight. Use sunscreen or sunblock lotions and lip balms with a sun protection factor (SPF) of at least 30 on a regular basis when you are outdoors. Wear protective clothing and hats and stay out of direct sunlight, especially between the hours of 10 AM and 3 PM. Avoid sunlamps and tanning beds.

Check with your doctor right away if blurred vision, difficulty with reading, eye pain, or any other vision change occurs with this medicine. Your doctor may want an ophthalmologist (eye doctor) to check your eyes.

Kidney failure may occur while you are using this medicine. Tell your doctor right away if you have bloody urine, decrease in how much or how often you urinate, lower back or side pain, swelling of the face, fingers, or lower legs, trouble breathing, or weight gain.

This medicine may cause muscle, bone, and connective tissue disease (eg, Dupuytren's contracture or plantar fascial fibromatosis). Check with your doctor right away if you have unusual thickening of the palms of your hands with tightening of the fingers inward or unusual thickening of the soles which may be painful.

It is important to tell your doctor if you have had or are planning to receive radiation treatment while you are taking this medicine.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

What Are Reasons I Shouldn’t Take Zelboraf?

Zelboraf should not be taken by any person who is pregnant or plans to become pregnant, as it can cause fetal harm. It should also not be used while breastfeeding.

It should also not be taken by anyone who has a heart condition called long QT syndrome, as this can increase the risk of a severe and potentially life-threatening irregular heart rhythm.

What Other Medications Interact With Zelboraf?

Medications that should be avoided when taking Zelboraf include:

  • Biaxin (clarithromycin)
  • Itrafungol, Sporanox, or Onmel (itraconazole)
  • Diflucan (fluconazole)
  • Calan or Verelan (verapamil)
  • Dilantin (phenytoin)
  • Carbatrol, Epitol or TEGretol (carbamazepine)
  • Zanaflex (tizanidine)
  • Digox or Lanoxin (digoxin)

What Medications Are Similar?

In addition to Zelboraf, there are two other BRAF inhibitor medications that can be used to treat melanoma that has a BRAF mutation: Tafinlar (dabrafenib) and Braftovi (encorafenib). These two BRAF inhibitors can be used to treat melanoma that cannot be removed surgically or has become metastatic.

Tafinlar can be used in combination with another medication to be used in BRAF-mutated stage 3 melanoma that has been removed surgically. This drug combination can help reduce the chance of the cancer coming back.

Frequently Asked Questions

  • What is Zelboraf used for?

    Zelboraf is used to treat BRAF mutated melanoma that has spread to distant areas of the body (metastatic) or cannot be removed surgically. It can also be used to treat a rare blood cancer called Erdheim-Chester disease, which has to have a BRAF mutation.

  • How does Zelboraf work?

    Zelboraf works by blocking a BRAF mutation that can be found in some cancers. This BRAF protein signals cancer cells to grow quickly and out of control. By blocking this signal, Zelboraf can stop the cancer cells from continuing to grow out of control.

  • What are the side effects of Zelboraf?

    The common side effects of Zelboraf can include:

    • Nausea
    • Rash
    • Itching
    • Joint pain
    • Hair loss
    • Skin sensitivity to the sun

    The more serious side effects of Zelboraf can include:

    • Abnormal heart rhythm
    • New skin cancers
    • Problems to the eyes, liver, kidneys
    • Severe skin reactions
  • How do I stop taking Zelboraf?

    Zelboraf should not be stopped unless first discussed with the oncologist who prescribed it.

How Can I Stay Healthy While Taking Zelboraf?

Zelboraf can be a very important medication in the treatment plan for BRAF-mutated melanoma or Erdheim-Chester disease. However, side effects can occur, which can be scary if you don’t understand how to manage them. Talk to your healthcare team about the best way to take your medication and treat any side effects that come up.

Many times, the sooner you try to treat a side effect, the sooner you will feel better, and the easier it will be to treat. Never hesitate to ask any questions you have or discuss any concerns you have with your cancer care team.

Medical Disclaimer

Verywell Health's drug information is meant for educational purposes only and is not intended as a replacement for medical advice, diagnosis, or treatment from a healthcare professional. Consult your healthcare provider before taking any new medication(s). IBM Watson Micromedex provides some of the drug content, as indicated on the page.

6 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
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