Zelboraf - Vemurafenib

What is Zelboraf - Vemurafenib?

Zelboraf is a medicine that contains the active substance vemurafenib. It is available as tablets (240 mg).

What is Zelboraf used for - Vemurafenib?

Zelboraf is used to treat adults with melanoma (a type of skin cancer) that has spread to other parts of the body or is inoperable. It is only indicated for patients whose tumor cell genes show a BRAF V600 mutation.

The medicine can only be obtained with a prescription.

How is Zelboraf used - Vemurafenib?

Treatment with Zelboraf should be started and supervised by a specialist who is an expert in cancer therapy. Before starting, the presence of the BRAF V600 mutation in the patient's tumor cells must be ascertained.

The recommended dose is 960 mg (four tablets) twice a day. The first dose is taken in the morning and the second dose in the evening, about 12 hours later. Each dose should always be taken in the same way, with meals or between meals.

The treatment should be continued for as long as possible until the disease gets worse or the side effects become too serious.

How does Zelboraf work - Vemurafenib?

The active substance in Zelboraf, vemurafenib, is a BRAF inhibitor, a protein that stimulates cell division. In the BRAF V600 mutation melanomas there is an abnormal form of BRAF which contributes to the development of the tumor allowing the uncontrolled division of tumor cells. By blocking the action of the abnormal BRAF protein, Zelboraf helps slow the growth and spread of the tumor. Zelboraf is only given to patients with melanomas caused by a BRAF V600 mutation.

What studies have been performed on Zelboraf - Vemurafenib?

The effects of Zelboraf were first tested in experimental models before being studied in humans.

Zelboraf was compared with the anticancer medicine dacarbazine in one main study involving 675 patients with melanoma containing the widespread or inoperable BRAF V600 mutation. Patients had to receive the medicine until the disease got worse or the treatment did not develop an excessive level of toxicity. The main measures of effectiveness were overall survival and progression-free survival of the disease.

What benefits has Zelboraf shown during the studies?

Zelboraf has been shown to be effective in prolonging patients' lives and delaying the worsening of the disease. As shown in the main study, the survival of patients treated with Zelboraf was on average 13.2 months, compared with 9.6 months in patients treated with dacarbazine. As for the worsening of the disease, in the Zelboraf group it occurred on average after 5.3 months, compared with 1.6 months in the dacarbazine group.

What is the risk associated with Zelboraf?

The most common side effects of Zelboraf (seen in more than 30% of patients) include arthralgia (joint pain), fatigue, rash, photosensitive reactions (reactions similar to sunburn caused by exposure to light), nausea, alopecia (hair loss) ) and itching. Some patients treated with Zelboraf develop another type of skin cancer called "squamous cell skin cancer" which can be effectively treated with local surgery. For the full list of all side effects reported with Zelboraf, see the Package Leaflet.

Zelboraf must not be used in people who may be hypersensitive (allergic) to vemurafenib or any of the other ingredients.

Why has Zelboraf - Vemurafenib been approved?

The CHMP noted that the effectiveness of Zelboraf in improving overall survival and delaying the widespread or inoperable "BRAF V600 mutation positive" melanoma had been convincingly demonstrated. Regarding the risks, about half of patients treated with Zelboraf developed a serious side effect and about one fifth developed skin squamous cell carcinoma. The CHMP considered the side effects to be manageable and included recommendations for doctors to help reduce the risks in the product information. The Committee concluded that Zelboraf's benefits are greater than its risks and recommended that it be given marketing authorization.

More information on Zelboraf - Vemurafenib

On 17 February 2012, the European Commission issued a marketing authorization for Zelboraf, valid throughout the European Union.

For more information on Zelboraf therapy, read the package leaflet (also part of the EPAR) or contact your doctor or pharmacist.

Last update of this summary: 01-2012.