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What is it? Overview Usage Side Effects and Warnings

What is Vemurafenib?

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Vemurafenib (dots) bound to B-RAF (ribbons)

Vemurafenib is a recently approved chemotherapy available for melanoma treatment. It is an excellent demonstration of a targeted cancer therapy. It inhibits the activity of a mutated protein (BRAF) which bypasses the cell’s usual signals and leads to excessive cell growth (cancer). Vemurafenib only works in melanoma patients whose cancer has the V600E BRAF mutation (which means amino acid position number 600 on the BRAF protein, valine is replaced by glutamic acid). Approximately 60% of melanomas have this mutation. It is not known how often this mutation is present while melanoma is not detected. This new targeted chemotherapy was shown to extend survival time and shrink tumors better than dacarbazine, the standard of care choice for treating [metastatic...

Vemurafenib is taken twice a day in pill form, approximately every 12 hours. In contrast, dacarbazine is administered every three weeks by IV. Patients should inform any other doctor or dentist that you are taking Vemurafenib before they care for you. Avoid sunlight and sunlamps. They should use lip balm and a broad-spectrum sunscreen with SPF 30 or higher. It is necessary to get regularly screened for new moles (squamous cell carcinomas), that grow more frequently when using Vemurafenib, and that will need to be quickly removed.

Vemurafenib is a treatment that extends life and reduces tumors. It is not a cure. While 74% of the patients showed regression, compared with ~5% for Dacarbazine, the regression only lasted from 2-18 months. Two explanations for the recurrence have been...

Vemurafenib caused a number of side effects, including diarrhea, fatigue, nausea, hair loss, rash, joint pain and squamous cell skin cancer. About 31% of the patients grew these moles, which were monitored and removed promptly. About 45% of Vemurafenib patients had to modify their dose because of these side effects. The side effects were more frequent and significant for vemurafenib than for the dacarbazine group(1).

Possible serious side effects of Zelboraf include severe allergic reactions; severe skin reactions; changes in the electrical activity of the heart called QT prolongation, which can potentially be life-threatening; abnormal liver function tests; eye problems; or new melanoma lesions.