Zelboraf
Zelboraf (vemurafenib) is a targeted therapy that’s used to treat a type of skin cancer called melanoma and a rare blood cancer called Erdheim-Chester disease (ECD). These cancers must have a certain mutation called a BRAF mutation in order for you to use Zelboraf (vemurafenib) as treatment. This medication is a tablet that you take by mouth, but some side effects can include tiredness, joint pain, and rash.
What is Zelboraf (vemurafenib)?
What is Zelboraf (vemurafenib) used for?
Melanoma with a certain BRAF mutation that has spread (metastatic) or can’t be removed by surgery
Erdheim-Chester disease (ECD) with a certain BRAF mutation
How Zelboraf (vemurafenib) works
Zelboraf (vemurafenib) is a kinase inhibitor known as a BRAF inhibitor. The BRAF protein helps cells (including cancer cells) grow. And when the BRAF protein is mutated, the cancer can grow uncontrollably and spread more quickly. By blocking BRAF, Zelboraf (vemurafenib) helps stop tumor growth.
Drug Facts
What are the side effects of Zelboraf (vemurafenib)?
Common Side Effects
- Joint pain (up to 67%)
- Tiredness (up to 54%)
- Rash (up to 52%)
- Sun sensitivity (up to 49%)
- Hair loss (up to 45%)
- Nausea (up to 37%)
- Itching (up to 30%)
- Skin papilloma (non-cancerous, wart-like skin growth; up to 30%)
- Diarrhea (up to 29%)
- Thickened skin (up to 28%)
- Headache (up to 27%)
- Vomiting (up to 26%)
Other Side Effects
- Muscle or back pain
- Pain in arms or legs
- Swelling in arms or legs
- Low appetite
- Constipation
- Fever
- Dry skin
- Sunburn
- Rash
- New skin cancers
- Changes in taste
- Cough
- Weakness
- Changes in liver enzyme levels in blood
Serious Side Effects
- Serious allergic reactions: rash, fever, trouble breathing, swelling of the face or mouth
- Serious skin reactions: painful blisters, skin wounds, peeling skin
- Serious liver problems: upper stomach pain, yellow skin, yellow around the whites of the eyes
- Changes in heart rhythm: lightheadedness, blurry vision, fainting, seizures, loss of consciousness
- Serious reaction in people who’ve received radiation therapy: see Warnings for more details
Source: DailyMed
The following side effects have also been reported
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:
More common
Blistering, peeling, or loosening of the skin
bloating or swelling of the face, arms, hands, lower legs, or feet
bloody urine
blurred vision or other change in vision
chills
decreased frequency or amount of urine
dizziness
fainting
fast or irregular heartbeat
increased sensitivity of the skin to sunlight
increased thirst
itching or skin rash
joint or muscle pain
loss of appetite
lower back or side pain
lump or growth on the skin
pain in the ankles or knees
painful, red lumps under the skin, mostly on the legs
paralysis of the nerves
rapid weight gain
rash with flat lesions or small raised lesions on the skin
red skin lesions, often with a purple center
red, irritated eyes
redness or other discoloration of the skin
redness, soreness, swelling, or itching of the skin
scaling of the skin on the hands and feet
sensitivity of the eye to light
severe sunburn
sores, ulcers, or white spots in the mouth or on the lips
sores, welts, or blisters
tearing
tingling of the hands and feet
tiredness
trouble breathing
ulceration of the skin
unusual tiredness or weakness
unusual weight gain or loss
vomiting
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
More common
Back or bone pain
burning, itching, and pain in the hairy areas, or pus at the root of the hair
change in taste
decreased appetite
decreased weight
difficulty having a bowel movement
difficulty with moving
hair loss or thinning of the hair
headache
lack or loss of strength
loss of taste
muscle stiffness
pain in the arms or legs
sunburn
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
Pros and cons of Zelboraf (vemurafenib)
Pros
Recommended for people with BRAF-mutated melanoma or Erdheim-Chester disease
Works in a more specific, targeted way than traditional chemotherapy
Can take with or without food
Cons
Not recommended for people who don’t have a BRAF mutation in their cancer
Typical dose is four tablets taken all at one time, so not ideal for people with trouble swallowing
Might cause side effects such as sun sensitivity, joint pain, and hair loss
Pharmacist tips for Zelboraf (vemurafenib)
For each dose, you’ll need to take several tablets of Zelboraf (vemurafenib) all at once (or one right after another). You can take the medication with or without food. Swallow the tablets whole; don’t crush or chew them.
Joint pain is a common side effect of Zelboraf (vemurafenib), though typically, it isn’t severe. It commonly happens in the finger, wrist, and knee joints. Most times, you won’t need treatment for the pain. But if you have joint pain that’s bothering you, your provider might recommend a nonsteroidal anti-inflammatory drug (NSAID) like ibuprofen (Advil).
Let your provider know if you feel nauseous during treatment so they can prescribe an antiemetic medication, like ondansetron (Zofran) or prochlorperazine, to help prevent or manage this side effect. The nausea is usually mild, but if it’s severe, contact your provider. They might adjust your treatment.
You might experience some diarrhea when you first start Zelboraf (vemurafenib) treatment, but this should improve over time. Your provider might suggest an over-the-counter medication like loperamide (Imodium A-D) to help manage diarrhea. If you have diarrhea, it’s important to drink a lot of fluids. But try to avoid sugary sports drinks because they can make diarrhea worse.
It’s important to wear broad-spectrum sunscreen while outdoors to protect your skin. Zelboraf (vemurafenib) makes your skin sensitive to sunlight, which can cause skin damage or sunburns.
Don't breastfeed while you're taking Zelboraf (vemurafenib). We don’t know whether Zelboraf (vemurafenib) is found in breast milk and whether it affects breastfed babies. But because of the possible risks to a baby, it’s best to avoid nursing when you’re taking Zelboraf (vemurafenib) and for 2 weeks after the last dose.
Ask your provider about the best way to handle and throw away Zelboraf (vemurafenib) safely. Anticancer medications can be harmful to people who handle or come in contact with them. You should store the medication up and away, so children and pets won’t be able to reach it.
Frequently asked questions about Zelboraf (vemurafenib)
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What are the risks and warnings for Zelboraf (vemurafenib)?
Zelboraf (vemurafenib) can cause some serious health issues. This risk may be even higher for certain groups. If this worries you, talk to your doctor or pharmacist about other options.
New cancers
Risk factors: 65 years and older | Previous skin cancer | A lot of sun exposure over time
Some people taking Zelboraf (vemurafenib) developed a new cancer. In studies, these cancers included different kinds of skin cancer and other non-skin cancers. While you’re taking Zelboraf (vemurafenib), your provider will monitor you for new signs and symptoms of cancer, especially skin cancers. If you notice a new sore on your skin or any skin changes while taking Zelboraf (vemurafenib), contact your provider.
Not for people with cancers without a BRAF mutation
Zelboraf (vemurafenib) isn’t recommended for people with conditions without a BRAF mutation. Lab studies have shown that if a BRAF inhibitor is used to treat a condition that doesn’t have a BRAF mutation, it might cause cancer cells to grow. For this reason, BRAF inhibitors like Zelboraf (vemurafenib) should only be used in people with certain BRAF mutations. Your provider will confirm that you have a BRAF mutation before you start taking Zelboraf (vemurafenib).
Allergic reaction
It’s possible for people taking Zelboraf (vemurafenib) to experience serious allergic reactions, including anaphylaxis. Severe symptoms can include rash, red and swollen skin, low blood pressure, and a serious reaction called drug reaction with eosinophilia and systemic symptoms (DRESS syndrome). If you have a new rash, fever, swollen lymph nodes, or trouble breathing, seek medical attention right away.
Changes in heart rhythm
Risk factors: Heart rhythm problems (arrhythmias) | Heart failure | Electrolyte imbalances | Taking medications that can change heart rhythm
Some people taking Zelboraf (vemurafenib) have had changes in their heart rhythm, also called QT prolongation. This lengthens the time it takes for your heart to recharge after each beat. Tell your provider about all the medical conditions you have and the medications you take. If you’re born with this heart rhythm problem (long QT syndrome) or if you take another medication that can raise your risk of this heart rhythm problem, it might not be safe for you to take Zelboraf (vemurafenib). In some cases, your provider might still prescribe Zelboraf (vemurafenib).
During treatment, your provider will track the electrical activity of your heart using a test called an electrocardiogram (EKG). If the EKG shows that you have a heart rhythm problem and you experience symptoms, such as dizziness, chest pain, or weakness, your provider might switch you to a different medication.
Liver problems
Some people taking Zelboraf (vemurafenib) have developed liver damage, sometimes causing the liver to not work as well. Since the liver plays a role in helping your body stop any bleeding, liver damage can sometimes affect your body’s ability to clot blood when it needs to.
During treatment, your provider will track your liver health through lab tests on a regular basis, usually every month. And if your levels are concerning, you might need to pause or stop Zelboraf (vemurafenib) while your provider looks into it. Most people don’t feel any noticeable symptoms when this happens, so it’s important to keep up with your lab work regularly. If you have stomach pain, yellowish skin, or yellow around the whites of your eyes, call your provider right away, as these can be symptoms of liver problems.
Skin that’s sensitive to sun and serious skin reactions
Zelboraf (vemurafenib) might cause your skin to be more sensitive to the sun and make it easier for you to get a sunburn. This reaction can be mild or severe. If possible, avoid being in direct sunlight while taking Zelboraf (vemurafenib). If you do go outdoors, wear protective clothing and broad-spectrum UVA/UVB sunscreen with an SPF of at least 30. If you have a skin rash after being outdoors, contact your provider.
Rarely, Zelboraf (vemurafenib) can also cause severe and sometimes life-threatening skin reactions that happen with or without infections. These reactions include Stevens-Johnson syndrome (SJS) or toxic epidermal necrolysis (TEN). Tell your provider right away if you develop painful blisters, skin wounds, peeling skin, flu-like symptoms, or fever. These are signs of a serious skin reaction that need immediate medical attention.
Eye problems
Though uncommon, some people taking Zelboraf (vemurafenib) experienced vision changes. These changes included blurry vision, light sensitivity, and swelling inside their eye (also called uveitis). Contact your provider right away if you have vision changes, eye pain, or light sensitivity. You might have to pause treatment while your provider or an ophthalmologist checks your eyes for problems.
Harm to unborn baby
While unknown, it’s possible for Zelboraf (vemurafenib) to harm an unborn baby based on the way the medication works. Because of these risks, if you’re able to get pregnant, you should use birth control while taking Zelboraf (vemurafenib) and for 2 weeks after the last dose. Let your provider know right away if you become pregnant while taking Zelboraf (vemurafenib).
Serious reaction to radiation
Risk factors: Previous radiation therapy
People who take Zelboraf (vemurafenib) and receive radiation therapy for cancer treatment are at risk for having a reaction at the site where they received the radiation. This reaction is called radiation recall. It can happen if you’ve had radiation before, during, or after treatment with Zelboraf (vemurafenib). The reaction happens most commonly on the skin, but it can occur in any organ that has gotten radiation. These reactions can range from mild (e.g., rash, dry skin) to life-threatening (e.g., severe wounds, bleeding). Talk to your provider if you’re taking Zelboraf (vemurafenib) and you’ve had radiation therapy.
Kidney failure
Risk factors: Kidney problems
Some people taking Zelboraf (vemurafenib) develop higher levels of creatinine in their blood, which can suggest kidney damage. Most times, these elevations in creatinine levels are mild. But in some cases, there can be serious kidney damage, including kidney failure. You might not have any symptoms if your kidneys aren’t working as well. For this reason, your provider will check your kidney function regularly with lab tests while you’re taking Zelboraf (vemurafenib).
Serious hand and foot conditions
Though uncommon, some people taking Zelboraf (vemurafenib) have experienced changes in their hands or feet. One condition, called Dupuytren’s contracture, causes the fingers to bend toward the palm. Another condition, called plantar fibromatosis, causes tissue growth on the bottom of the foot. These conditions can be painful and lead to difficulty walking. Most cases were mild or moderate, but sometimes can be severe and affect daily life. If you notice any changes to your hands or feet, contact your provider right away.
Zelboraf (vemurafenib) dosage forms
Typical dosing for Zelboraf (vemurafenib)
The usual dose is 960 mg (four 240 mg tablets) by mouth every 12 hours.
Interactions between Zelboraf (vemurafenib) and other drugs
Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
- Bepridil
- Cisapride
- Colchicine
- Dronedarone
- Fluconazole
- Ketoconazole
- Mesoridazine
- Pimozide
- Piperaquine
- Posaconazole
- Saquinavir
- Sparfloxacin
- Terfenadine
- Thioridazine
- Ziprasidone
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Afatinib
- Alfuzosin
- Amiodarone
- Amisulpride
- Amitriptyline
- Anagrelide
- Apomorphine
- Aripiprazole
- Aripiprazole Lauroxil
- Arsenic Trioxide
- Asenapine
- Astemizole
- Atazanavir
- Azithromycin
- Bedaquiline
- Berotralstat
- Betrixaban
- Boceprevir
- Buprenorphine
- Buserelin
- Carbamazepine
- Ceritinib
- Chloroquine
- Chlorpromazine
- Ciprofloxacin
- Citalopram
- Clarithromycin
- Clofazimine
- Clomipramine
- Clozapine
- Cobicistat
- Conivaptan
- Crizotinib
- Cyclobenzaprine
- Dabigatran Etexilate
- Dabrafenib
- Dasatinib
- Degarelix
- Delamanid
- Desipramine
- Deslorelin
- Deutetrabenazine
- Digoxin
- Disopyramide
- Dofetilide
- Dolasetron
- Domperidone
- Donepezil
- Doxepin
- Droperidol
- Ebastine
- Efavirenz
- Encorafenib
- Entrectinib
- Enzalutamide
- Eribulin
- Erythromycin
- Escitalopram
- Famotidine
- Felbamate
- Fingolimod
- Flecainide
- Fluoxetine
- Formoterol
- Foscarnet
- Fosphenytoin
- Fostemsavir
- Galantamine
- Gatifloxacin
- Gemifloxacin
- Glasdegib
- Gonadorelin
- Goserelin
- Granisetron
- Halofantrine
- Haloperidol
- Histrelin
- Hydroquinidine
- Hydroxychloroquine
- Hydroxyzine
- Ibutilide
- Idelalisib
- Iloperidone
- Imipramine
- Indinavir
- Inotuzumab Ozogamicin
- Itraconazole
- Ivabradine
- Ivosidenib
- Lapatinib
- Lefamulin
- Lenvatinib
- Leuprolide
- Levofloxacin
- Lofexidine
- Lopinavir
- Lumacaftor
- Lumefantrine
- Macimorelin
- Mefloquine
- Methadone
- Methotrimeprazine
- Metronidazole
- Mifepristone
- Mirtazapine
- Mitotane
- Mizolastine
- Moricizine
- Moxifloxacin
- Nafarelin
- Nefazodone
- Nelfinavir
- Nilotinib
- Norfloxacin
- Octreotide
- Ofloxacin
- Olanzapine
- Ondansetron
- Osilodrostat
- Osimertinib
- Oxaliplatin
- Ozanimod
- Paliperidone
- Panobinostat
- Papaverine
- Paroxetine
- Pasireotide
- Pazopanib
- Pentamidine
- Perphenazine
- Phenytoin
- Pimavanserin
- Pipamperone
- Pitolisant
- Ponesimod
- Probucol
- Procainamide
- Prochlorperazine
- Promethazine
- Propafenone
- Protriptyline
- Quetiapine
- Quinidine
- Quinine
- Ranolazine
- Relugolix
- Ribociclib
- Rifampin
- Rimegepant
- Risperidone
- Ritonavir
- Selpercatinib
- Sertindole
- Sertraline
- Sevoflurane
- Siponimod
- Sodium Phosphate
- Sodium Phosphate, Dibasic
- Sodium Phosphate, Monobasic
- Solifenacin
- Sorafenib
- Sotalol
- St John's Wort
- Sulpiride
- Sultopride
- Sunitinib
- Tacrolimus
- Tamoxifen
- Telaprevir
- Telavancin
- Telithromycin
- Tetrabenazine
- Theophylline
- Tizanidine
- Tolterodine
- Topotecan
- Toremifene
- Trazodone
- Triclabendazole
- Trimipramine
- Triptorelin
- Ubrogepant
- Vandetanib
- Vardenafil
- Venetoclax
- Venlafaxine
- Vilanterol
- Vincristine
- Vincristine Sulfate Liposome
- Vinflunine
- Voclosporin
- Voriconazole
- Vorinostat
- Zotepine
- Zuclopenthixol
What are alternatives to Zelboraf (vemurafenib)?
Melanoma with a certain BRAF mutation that has spread (metastatic) or can’t be removed by surgery
Erdheim-Chester disease (ECD) with a certain BRAF mutation
Melanoma with certain BRAF mutations that has spread (metastatic) or that can’t be removed by surgery, used with Mektovi (binimetinib)
Colorectal cancer with a certain BRAF mutation that has spread (metastatic), used with Erbitux (cetuximab)
Melanoma with certain BRAF mutations
Metastatic non-small cell lung cancer (NSCLC) with a certain BRAF mutation, used with Mekinist (trametinib)
Metastatic anaplastic thyroid cancer (ATC) with a certain BRAF mutation, used with Mekinist (trametinib)
Solid tumors with a certain BRAF mutation that have spread (metastatic) or can’t be removed by surgery, used with Mekinist (trametinib)
Low-grade glioma (LGG) with a certain BRAF mutation, used with Mekinist (trametinib)
What is the latest news about Zelboraf (vemurafenib)?
Zelboraf (vemurafenib) images
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References
Best studies we foundAl-Akchar, M., et al. (2022). Long QT syndrome. StatPearls.
Al-Khatib, S. M., et al. (2003). What clinicians should know about the QT interval. Journal of the American Medical Association.
American Cancer Society. (2019). Chemotherapy safety.
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American Kidney Fund. (n.d.). Serum creatinine test for kidney disease.
American Society for Surgery of the Hand. (2021). Dupuytren's contracture.
Boussemart, L., et al. (2013). Vemurafenib and radiosensitization. Journal of the American Medical Association Dermatology.
Burris, H. A., III., et al. (2010). Radiation recall with anticancer agents. The Oncologist.
Dika, E., et al. (2016). Hair and nail adverse events during treatment with targeted therapies for metastatic melanoma. European Journal of Dermatology.
Flores, B., et al. (2017). Hemostasis, bleeding and thrombosis in liver disease. Journal of Translational Science.
Genentech, Inc. (2023). Zelboraf- vemurafenib tablet, film coated [package insert]. DailyMed.
Goyal, G., et al. (2020). Erdheim-Chester disease: Consensus recommendations for evaluation, diagnosis, and treatment in the molecular era. Blood.
Leukemia and Lymphoma Society. (2022). Erdheim-Chester disease.
National Cancer Institute. (n.d.). BRAF V600 mutation.
National Comprehensive Cancer Network. (2023). Melanoma.
National Eye Institute. (2023). Uveitis.
National Heart, Lung, and Blood Institute. (2022). Long QT syndrome.
National Organization for Rare Disorders. (2023). Erdheim Chester disease.
Piraccini, B. M., et al. (2015). RASopathic alopecia: Hair changes associated with vemurafenib therapy. Journal of the American Academy of Dermatology.
Proietti, I., et al. (2020). BRAF inhibitors: Molecular targeting and immunomodulatory actions. Cancers.
Rossi, A., et al. (2017). Chemotherapy-induced alopecia management: Clinical experience and practical advice. Journal of Cosmetic Dermatology.
Sabry, A. O., et al. (2023). Papilloma. StatPearls.
Salzmann, M., et al. (2020). Arthralgia induced by BRAF inhibitor therapy in melanoma patients. Cancers.
Wanchoo, R., et al. (2016). Renal effects of BRAF inhibitors: A systematic review by the Cancer and the Kidney International Network. Clinical Kidney Journal.
Young, J. R., et al. (2018). The etiology, evaluation, and management of plantar fibromatosis. Orthopedic Research and Reviews.
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