What is Zelboraf (vemurafenib)?

Zelboraf (vemurafenib) is a targeted therapy used to treat metastatic or unresectable melanoma with the BRAF V600E mutation. By inhibiting the abnormal activity of the mutated BRAF protein, Zelboraf helps suppress the growth of cancer cells. Taken orally, it requires strict adherence to the prescribed dosage. Common side effects include fatigue, joint pain, rash, photosensitivity, and hair loss. Serious reactions, such as severe skin issues, liver problems, or heart rhythm disturbances, may occur. Zelboraf’s effectiveness is limited to melanomas with the specific mutation mentioned. Regular monitoring by a healthcare provider is crucial to assess progress and manage potential side effects.

Zelboraf (Vemurafenib)
Zelboraf
Vemurafenib
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What is Zelboraf?

Zelboraf is a BRAF kinase inhibitor, antineoplastic medication that is used in the treatment of malignant melanoma and Erdheim-Chester disease cases that involve BRAF mutations. It may be used alongside other medications or by itself. It is not used in cases of melanoma that involve a normal BRAF gene.

How is Zelboraf Used?

Zelboraf is typically taken twice daily, with 12 hours between each dose. Most patients take a standard dose of four tablets (960 mg) twice per day. This medication may be taken with or without food, but patients should remain consistent regarding the manner in which they take Zelboraf (i.e., if you take it with food, it should be taken with food each time a dose is consumed). The tablets should not be chewed or crushed, and this medication should not be taken with grapefruit juice.

If a patient has vomited after taking a dose, they should not take an additional dose of the medication and should simply proceed with taking their next scheduled dose.

Patients should take Zelboraf exactly as prescribed by their physician to ensure maximum safety and efficacy and minimize the potential for side effects.

Storage

Zelboraf should be stored at room temperature within the range of 68°F (20°C) and 77°F (25°C). This medication may temporarily be allowed to reach a low temperature of 59°F (15°C) or a high temperature of 86°F (30°C).

Keep this medication out of the reach of children at all times.

Zelboraf should be stored in its original container, and patients should ensure that the lid remains tightly closed when not in use.

Uses

Zelboraf is prescribed for the treatment of:

  • melanoma (with BRAF gene mutation)
  • Erdheim-Chester disease (with BRAF gene mutation)

How Does Zelboraf Work?

Zelboraf is an antineoplastic medication that is, more specifically, a BRAF inhibitor. In patients that have melanoma or ECD with certain BRAF mutations, Zelboraf functions by inhibiting the activity of the mutated BRAF gene. By stopping the action of this abnormal gene, Zelboraf is able to stop the cell division leading to the conditions spreading, and it may also shrink melanoma tumors.

Dosage

Zelboraf is available in tablet form with only one strength of 240 mg.

The most common dosage is four of the 240 mg tablets (960 mg) taken twice daily.

Patients using Zelboraf should be sure to take the medication exactly as instructed by their prescribing physician.

Overdose

Patients should avoid taking more than instructed by their doctor. If an overdose has occurred or is suspected, patients should contact their local Poison Control Center or doctor for further advice.

Side Effects

Zelboraf is associated with a variety of common as well as serious side effects.

The most common side effects include:

  • fatigue
  • hair loss
  • increased risk of sunburn occurring
  • itchiness
  • joint pain
  • mild rash
  • nausea
  • skin growths
  • sun sensitivity

Some of the following serious side effects may occur when taking Zelboraf and should be reported to your prescribing physician as soon as possible:

  • breathing difficulties
  • burning sensation in the eyes
  • clay-colored stools
  • dark-colored urine
  • eye swelling or pain
  • fever
  • fluttering sensation in the chest
  • fingers bending inward
  • hives
  • jaundice (yellowing of the eyes or skin)
  • mole changes (color or size)
  • muscles aches
  • nausea
  • new lesions or warts
  • pain in the upper right side of your stomach
  • purple or red skin rash that blisters, peels, and spreads
  • rapid or pounding heartbeat
  • red bump that doesn’t heal or that bleeds
  • severe redness of the eyes
  • severe weakness
  • shortness of breath
  • skin pain
  • skin sore that bleeds or doesn’t heal
  • small yellow or white patches on the eye’s surface
  • sore throat
  • sudden dizziness
  • swollen glands
  • swelling of the throat, tongue, lips, or face
  • tightness of the fingers
  • unusual bruising
  • unusual thickening of the tissues underneath the skin of the soles of your feet or your palms
  • vision changes
  • vomiting

Warnings & Precautions

Zelboraf is associated with a number of different risks. Patients should be sure to discuss their medical history and any other medication use before beginning treatment with this medication.

Allergic Reactions

Severe allergic reactions are possible in those who are taking Zelboraf. If you are taking Zelboraf and experience symptoms such as difficulty breathing, a swollen throat or face, flu-like symptoms, skin blistering or a rash, swollen glands, or jaundice, seek emergency attention immediately.

Changes in Heart Rhythm

Zelboraf is capable of impacting the electrical activity that occurs within a patient’s heart, and this may lead to abnormalities in heart rhythm. The risk of this condition, referred to as QT prolongation, is further increased in individuals also using tacrolimus, arsenic trioxide, pentamidine, mefloquine, moxifloxacin, pimozide, chlorpromazine, thioridazine, quinidine, or sotalol for treatment. The following factors place patients at a notably higher risk of QT prolongation when using Zelboraf: being over the age of 65 years, being female, having a slow heart rate, having a family history of abnormal heart rhythms or heart disease, diabetes, nutritional deficiencies, history of stroke, congenital prolongation of the QT interval, low levels of calcium, low levels of magnesium, and low levels of potassium.

Development of Other Cancers

Zelboraf comes with the risk of patients potentially developing additional cancers, as well as having the medication speed up the progression of certain pancreatic and blood cancers. Patients using Zelboraf will typically be monitored for such conditions occurring, and those with a history of cancers besides the ones for which they are using Zelboraf should inform their physician to ensure they are receiving the safest possible dosage of the medication for their current treatment.

Eye Problems

Zelboraf may cause inflammation within a patient’s eye and cause blood vessel blockages to develop. Any changes in vision or other eye-related symptoms should be reported to the patient’s prescribing physician immediately.

Grapefruit

Patients should not eat grapefruit or consume grapefruit juice while taking Zelboraf, as this fruit impacts the excretion of Zelboraf from the body. Drinking grapefruit juice or consuming the fruit itself while taking Zelboraf may result in a buildup of the medication within the body and lead to serious side effects.

Hypertension

Zelboraf is associated with increased blood pressure, and this factor will be monitored by your doctor throughout treatment. Patients with preexisting high blood pressure should discuss their history of hypertension with their physician before beginning treatment with Zelboraf.

Kidney Dysfunction

Zelboraf use may result in impaired kidney function, and it may also cause kidney failure in some individuals. Patients with a history of kidney-related health conditions should be sure to discuss this with their physician before beginning treatment with Zelboraf, as this may impact the dosage and efficacy of Zelboraf.

Liver Dysfunction

Zelboraf may impair liver function in some individuals and may even cause liver failure, which can be fatal. Patients that experience any of the following symptoms of reduced liver function should contact their prescribing physician as soon as possible: appetite loss, nausea, jaundice, feeling unwell, fatigue, itchy skin, pale stools, abdominal swelling, or abdominal pain.

Skin Issues

Zelboraf is associated with a high risk of skin changes, including some that may be serious, such as cutaneous squamous cell carcinoma and new melanoma. Any changes in the patient’s skin while using it should be reported to their prescribing physician immediately.

This medication also causes sun sensitivity, resulting in an increased risk of developing sunburns which may be severe. Protective measures, such as protective clothing and sunscreen, should be used when taking Zelboraf and going outdoors.

Radiation Treatment

Patients using it are at an increased risk of developing burns if also receiving radiation therapy. Patients currently undergoing radiation treatment are advised against using it. Additionally, patients that have received radiation treatment before may experience past treatment areas becoming inflamed in response to treatment. This is a condition referred to as radiation recall.

Pregnancy and Breastfeeding

Zelboraf is capable of harming an unborn child if used by a patient that is pregnant. This medication should not be used by pregnant individuals unless the benefits of Zelboraf have been determined to be greater than the potential risks. Patients it should avoid pregnancy during treatment and continue to take measures to avoid becoming pregnant for at least six months after stopping the medication. Patients that become pregnant during treatment should report this to their physician immediately.

The safety for breastfeeding patients has not been determined. It is advised that patients who are breastfeeding or desiring to breastfeed while using Zelboraf speak with their physician about the potential risks involved.

Drug Interactions

Speak to your doctor about any medications or herbal supplements you are currently taking before beginning treatment. Discuss any concerns you may have with your doctor or a trusted pharmacist.

The following medications and substances are known to interact with Zelboraf:

  • aliskiren
  • amiodarone
  • amitriptyline
  • amlodipine
  • antihistamines
  • antipsychotics
  • apalutamide
  • aprepitant
  • atazanavir
  • atorvastatin
  • “-azole” antifungals
  • beta-blockers
  • beta-2 agonists (long-acting)
  • bicalutamide
  • bosentan
  • bosutinib
  • bromazepam
  • caffeine
  • carbamazepine
  • calcium channel blockers
  • carvedilol
  • cetirizine
  • chlorpromazine
  • chloroquine
  • citalopram
  • ciprofloxacin
  • clarithromycin
  • clomipramine
  • clozapine
  • cobicistat
  • colchicine
  • conivaptan
  • conjugated estrogen
  • corticosteroids
  • crizotinib
  • cyclosporine
  • dabrafenib
  • dabigatran
  • daclatasvir
  • dasatinib
  • deferasirox
  • degarelix
  • delavirdine
  • desipramine
  • dextromethorphan
  • dexamethasone
  • digoxin
  • diltiazem
  • dipyridamole
  • disopyramide
  • dofetilide
  • domperidone
  • dronedarone
  • doxorubicin
  • doxylamine
  • duloxetine
  • diphenhydramine
  • edoxaban
  • efavirenz
  • etravirine
  • elagolix
  • enzalutamide
  • erythromycin
  • estradiol
  • estrogens
  • ethinyl estradiol
  • etoposide
  • flecainide
  • flutamide
  • fluconazole
  • “-gliptin” diabetes medications
  • granisetron
  • grapefruit juice
  • haloperidol
  • hepatitis C antiviral medications
  • HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)
  • HIV protease inhibitors
  • hydrocodone
  • hydrocortisone
  • hydroxyzine
  • imatinib
  • imipramine
  • indacaterol
  • indinavir
  • ipilimumab
  • ketoconazole
  • ledipasvir
  • levofloxacin
  • lidocaine
  • linagliptin
  • loratadine
  • lovastatin
  • macrolide antibiotics
  • melatonin
  • methadone
  • methotrexate
  • mexiletine
  • midazolam
  • mifepristone
  • mirtazapine
  • mitotane
  • modafinil
  • morphine
  • moxifloxacin
  • nadolol
  • naloxegol
  • narcotic pain medications
  • nevirapine
  • nifedipine
  • nilotinib
  • olanzapine
  • ondansetron
  • other cancer medications
  • pentamidine
  • phenobarbital
  • phenytoin
  • porfimer
  • primaquine
  • primidone
  • procainamide
  • propafenone
  • propranolol
  • protein kinase inhibitors
  • prucalopride
  • quetiapine
  • quinidine
  • quinine
  • quinolone antibiotics
  • ranitidine
  • rasagiline
  • rifabutin
  • rifampin
  • risperidone
  • ritonavir
  • rivaroxaban
  • romidepsin
  • ropinirole
  • salmeterol
  • saquinavir
  • saxagliptin
  • sertraline
  • serotonin antagonists (anti-emetic medication)
  • silodosin
  • simvastatin
  • sitagliptin
  • sofosbuvir
  • sotalol
  • “-statin” anti-cholesterol medications
  • John’s wort
  • sunitinib
  • tacrolimus
  • tetrabenazine
  • theophylline
  • tamoxifen
  • tizanidine
  • tocilizumab
  • tolvaptan
  • tricyclic antidepressants
  • venetoclax
  • verapamil
  • vinblastine
  • vincristine
  • voriconazole
  • warfarin

Alternative Medications

For patients who are unable to take Zelboraf or experiencing significant adverse side effects, alternative medications may be used to treat some of the associated conditions for which this medication is commonly prescribed:

  • dabrafenib (Tafinlar)
  • ipilimumab (Yervoy)
  • nivolumab (Opdivo)
  • pembrolizumab (Keytruda)
  • trametinib (Mekinist)

Frequently Asked Questions

Zelboraf is approved for the treatment of melanoma that is metastatic or unable to be removed with surgery and also includes an abnormal BRAF gene. Zelboraf is not approved for the treatment of any types of melanomas that lack this abnormality in the BRAF gene. It is also approved for the treatment of Erdheim-Chester disease (ECD) including an abnormal BRAF gene as well.

Zelboraf may cause the development of new skin cancers in some patients. Individuals using this medication should report any new melanoma lesions that may appear, any new warts, any moles that have changes occur in their color or size, or any new red bumps or skin sores that either do not appear to heal or that bleed.

Patients using Zelboraf should be careful to avoid exposure to sunlight as this medication can result in significant skin sensitivity, especially to radiation. This increased sensitivity can result in severe sunburns, and patients should exercise caution regarding taking appropriate safety measures when outdoors. This includes using sunscreen and lip balm with sunscreen included, as well as wearing protective clothing and keeping the skin covered.

Zelboraf is capable of causing severe side effects in some individuals. Patients experiencing any of the following should contact their doctor and seek medical attention immediately: severe skin reactions, severe allergic reactions, changes in liver function, changes in kidney function, eye problems, connective tissue disorders, changes or irregularities pertaining to heartbeat (QT prolongation), or worsening of any side effects associated with radiation treatment.

Patients using Zelboraf for the treatment of melanoma most commonly experience the following side effects: nausea, hair loss, itching, joint pain, rashes, sun sensitivity, an increased risk of sunburns, and warts. Those using it to treat Erdheim-Chester disease commonly experience hair loss, joint pain, QT prolongation, and fatigue.

The most important thing patients using Zelboraf should know is that this medication is associated with a variety of serious side effects and may also cause the development of new cancers to occur. Patients using this medication should be closely monitored and should report any serious side effects or skin changes to their physician immediately.

Zelboraf is a medication that is prescribed for the treatment of melanoma with an abnormal BRAF gene that is not able to be removed with surgery and that is metastatic and has spread elsewhere within the body. It may also be used in the treatment of Erdheim-Chester Disease (ECD)—a type of cancer that affects the blood cells—that has an abnormal BRAF gene as well.

Patients should take Zelboraf exactly as instructed by their prescribing physician. This medication is typically taken twice per day, with 12 hours between each dose. It may be taken with food or without, but the manner in which the patient takes the medication should remain consistent for each dose. The tablets should never be chewed or crushed. If vomiting occurs after taking one of their daily doses, an additional dose of the medication should not be taken to compensate for this. They will simply need to just take their next scheduled dose. If a dose has accidentally been missed, it may be taken once the individual remembers. However, a missed dose should not be consumed if the next upcoming dose is to occur within the next four hours.

Zelboraf should be stored at room temperature, ranging between 68°F (20°C) and 77°F (25°C). Temporary exposure to temperatures no lower than 59°F (15°C) and no higher than 86°F (30°C) are permitted. This medication should be stored in its original container and packaging, and patients that have this medication in their possession should ensure that the lid stays tightly closed when it is not currently being administered.

The active ingredient is vemurafenib. The inactive ingredients include the following: hydroxypropyl cellulose, magnesium stearate, colloidal silicon dioxide, croscarmellose sodium, and hypromellose acetate succinate. The coating of Zelboraf tablets include the following: iron oxide red, talc, polyethylene glycol 3350, titanium dioxide, and pinkish-white poly (vinyl alcohol).

Zelboraf may not be suitable for those with the following medical conditions: cancer progression involving the RAS mutation, pregnancy, those who are breastfeeding, pancreatitis, abnormal liver function tests, reduced kidney function, high levels of bilirubin within the blood, prolonged QT interval (on EKG), abnormal EKG including QT changes since birth, chronic heart failure that isn’t well-controlled with medicine, a slow heart rate, uvea inflammation, iris inflammation, low potassium levels, low magnesium levels, low calcium levels, or blood vessel blockages within the retina.

Patients using Zelboraf should be sure to avoid drinking grapefruit juice or consuming grapefruit while using the medication, as this may result in higher levels of Zelboraf remaining in the patient’s blood compared to the proper excretion taking place and keeping these levels balanced during treatment.

Zelboraf comes with significant risks for geriatric patients, and those above the age of 60 years may require special monitoring or other changes in how their condition is managed with the medication. Use in pediatric patients has not been shown to be effective nor safe in those with metastatic or unresectable melanoma with the BRAF V600 mutation. Patients that are nursing are advised against breastfeeding due to the potential risks to their child. It should not be used by pregnant women.

Zelboraf is intended to treat Erdheim-Chester disease in individuals with a BRAF V600 mutation as well as malignant melanoma in those who have a BRAF V600E mutation.

Zelboraf functions by either slowing down cell division or fully stopping the growth and spread of cancerous cells within the patient’s body. It is capable of recognizing the harmful cancer cells that are present, attaching to them, and then inhibiting their continued spread.

Zelboraf is available in tablet form with a single strength option of 240 mg.

Zelboraf is typically taken twice daily, with 12 hours between each dose. Most patients using this medication will consume four tablets (960 mg) for each twice-daily dose. Tablets should not be chewed or crushed, and they should be swallowed whole along with a full glass of water. Additionally, it may be taken with or without food. However, this medication should be taken in the same way at the exact same time of day consistently.