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ZELBORAF (vemurafenib)

 

Purpose: Zelboraf blocks a cellular pathway to stop the growth of melanoma tumors.

 

How it works:  Zelboraf is a kinase inhibitor that blocks the activity of the V600E-mutated form of BRAF, a key protein that helps cancer cells grow. About half of patients with melanoma have this mutated form of the protein in their tumors.

 

Which patients: Zelboraf is FDA-approved for patients who carry the BRAF V600E mutation and who have unresectable Stage III melanoma (melanoma that cannot be removed surgically) or Stage IV melanoma. Before receiving Zelboraf, patients must test positive for the BRAF mutation.

 

How it is given: Zelboraf is an oral drug. Patients receive 960 mg orally twice daily.

 

Effectiveness: In a large clinical trial, comparing Zelboraf to DTIC, almost 50% of all patients treated with Zelboraf experienced tumor shrinkage compared to 5% who received DTIC. It is not yet clear how long Zelboraf can increase overall survival, but at the time the trial was studied 77% of the people taking Zelboraf were still alive, compared to 64% of those taking DTIC.

 

In the phase III clinical trial, progression-free survival (the time a patient lives without cancer growing or spreading) was 5.3 months for patients on Zelboraf versus 1.6 months for patients on standard chemotherapy.

 

Side effects: Several side effects are common early in the course of treatment. Most of these side effects are mild or moderate in severity and, when severe, can be managed with either a decrease in the dosage or by briefly stopping the drug and then resuming its use.

 

  • Cutaneous Squamous Cell Carcinoma, occurs in approximately 24% of patients and is by far the most common side effect.
    • These usually appear in the first 7 to 8 weeks of treatment.
    • Squamous cell carcinoma is seen most often in older patients, those with a history of skin cancer, and those who have experienced chronic sun exposure.
    • If these lesions appear they should be removed, but typically you can continue taking the drug without changing the dosage.

 

Important: You should have a dermatologic examination before you start Zelboraf and every two months while you are on the drug.

 

  • Severe Allergic Reaction May cause:
    • Blisters on the skin and blisters or sores in the mouth
    • Peeling of the skin
    • Fever
    • Swelling of the face, hands, or soles of the feet

 

  • Skin Rash is also very common. The rash usually appears on the arms and legs but can also appear on the chest and back.
    • It often appears over the course of several days and may cause itching.
    • This is usually a reversible side effect, and once the drug is temporarily stopped the rash generally improves very quickly, and often does not return when the medication is restarted. 
    • In severe cases a patient may need to discontinue use of the drug.

 

Important.  If the rash is uncomfortable and if it covers more than half of the body, you should call your doctor.  The doctor will decide whether it is necessary to temporarily stop the therapy and also when to resume and at what dosage. 

 

  • Increased Sensitivity to the Sun (photosensitivity) is also common. You should avoid going out in the sun as much as possible.

 

Important. When you do go outside, cover up with clothing that protects your skin, including head, face, hands, arms and lips. Use a sunscreen with an SPF of 30 or higher and use a lip balm. 

 

  • Joint Discomfort is another relatively common side effect that usually occurs early in the course of treatment. Joint discomfort may involve one or multiple joints. The hands and feet are often painful, but the knees or shoulders can also be affected. On occasion swelling and redness around the joints will occur.

 

Important. Nonsteroidal antiinflammatories (aspirin-like medications) can be used to control the discomfort. In severe cases a dose interruption or reduction may be necessary.

 

Other Side Effects: These may include:

 

  • Changes in the electrical activity of the heart (QT prolongation) that can cause irregular heartbeats that are potentially life- threatening. Symptoms include feeling faint, lightheaded, dizzy or irregular or fast heartbeat.
  • Liver problems: symptoms include skin or the whites of the eyes turning yellow, feeling tired, dark or brown urine, nausea or vomiting, pain on the right side of the stomach,
  • Eye problems such as uveitis. Symptoms include eye pain, swelling or redness, blurred vision or other vision changes
  • New primary malignant melanomas
  • Hair loss
  • Tiredness,
  • Nausea
  • Warts

 

Additional information/resources:


Financial assistance. Zelboraf Access Solutions: 1-888-249-4918

Support: Patient Partners: 1-885-ZELBORAF (1-855-935-2672)

 



IMPORTANT!

  • When you go outside, cover up with clothing that protects your skin, including head, face, hands, arms and lips.
  • Use sunscreen with a
    SPF of 30 or higher.
  • Use lip balm.

FAST FACTS

  • Financial assistance. Zelboraf Access Solutions: 1-888-249-4918
  • Support: Patient Partners: 1-885-ZELBORAF (1-855-935-2672)