Drug Action
Vemurafenib is a BRAF kinase inhibitor.
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Drug reference
Vemurafenib is a BRAF kinase inhibitor.
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Monotherapy for the treatment of BRAF V600 mutation- positive unresectable or metastatic melanoma ▶BY MOUTH ▶Adult: 960 mg twice daily, for dose adjustment due to side effects—consult product literature
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Wild-type BRAF malignant melanoma
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Electrolyte disturbances. prior or concurrent cancer associated with RAS mutation—increased risk of tumour progression. susceptibility to QT-prolongation
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NICE decisions ▶Vemurafenib for treating locally advanced or metastatic BRAF V600 mutation-positive malignant melanoma (updated January 2015) NICE TA269 Vemurafenib (Zelboraf ®) is recommended as an option for the treatment of BRAF V600 mutation-positive unresectable or metastatic melanoma only if the manufacturer provides vemurafenib with the discount agreed in the patient access scheme. www.nice.org.uk/guidance/ta269 Scottish Medicines Consortium (SMC) decisions The Scottish Medicines Consortium has advised (December 2013) that vemurafenib (Zelboraf ®) is accepted for restricted use within NHS Scotland as monotherapy for the first-line treatment of BRAF V600 mutation-positive unresectable or metastatic melanoma.
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DRUG RASH WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS SYNDROME) DRESS syndrome has been reported in patients taking vemurafenib. DRESS syndrome starts with rash, fever, swollen glands, and increased white cell count, and it can affect the liver, kidneys and lungs; DRESS can also be fatal. Patients should be advised to stop taking vemurafenib and consult their doctor immediately if skin rash develops. Treatment with vemurafenib should not be restarted. MHRA/CHM ADVICE (NOVEMBER 2015): RISK OF POTENTIATION OF RADIATION TOXICITY Potentiation of radiation toxicity has been reported in patients treated with vemurafenib before, during, or after radiotherapy— use with caution. RISKS OF INCORRECT DOSING OF ORAL ANTI-CANCER MEDICINES See Cytotoxic drugs p. 938.
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→Appendix 1: vemurafenib
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▶Common or very common 7th nerve paralysis. alopecia. appetite decreased. arthralgia. arthritis. asthenia. connective tissue disorders. constipation. cough. diarrhoea. dizziness. eye inflammation. fever. folliculitis. headache. myalgia. nausea. neoplasms. pain. panniculitis. peripheral oedema. photosensitivity reaction . QT interval prolongation. radiation injuries. skin reactions. taste altered. vomiting. weight decreased ▶Uncommon Liver injury. neutropenia. pancreatitis. peripheral neuropathy. retinal occlusion. severe cutaneous adverse reactions (SCARs). vasculitis ▶Rare or very rare Acute tubular necrosis. nephritis acute interstitial ▶Frequency not known Acute kidney injury
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Effective contraception required during for at least 6 months after treatment.
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Manufacturer advises avoid unless potential benefit outweighs risk. See also Pregnancy and reproductive function in Cytotoxic drugs p. 938.
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Avoid—no information available.
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Manufacturer advises caution in moderate to severe impairment (risk of increased exposure)—monitor ECG monthly during the first 3 months of treatment, followed by at least every 3 months thereafter (if QTc interval is prolonged, consult product Immune system and malignant disease literature).
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Manufacturer advises caution in severe impairment.
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▶Monitor ECG and electrolytes before treatment, after one month and following dose adjustment (treatment not recommended if QT interval greater than 500 milliseconds at baseline). ▶Monitor liver function before treatment and periodically thereafter. ▶Monitor for uveitis, iritis and retinal vein occlusion. ▶Monitor for cutaneous and non-cutaneous squamous cell carcinoma and new primary melanoma before, during and for up to 6 months after treatment—consult product literature.
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Food may affect absorption (take at the same time with respect to food).
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There can be variation in the licensing of different medicines containing the same drug. Tablet CAUTIONARY AND ADVISORY LABELS 25 ▶Zelboraf (Roche Products Ltd) Vemurafenib 240 mg Zelboraf 240mg tablets | 56 tablet P £1,750.00 (Hospital only) ANTINEOPLASTIC DRUGS › OTHER
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Counselling advised (administration). Drug rash with eosinophilia and systemic symptoms (DRESS syndrome) Patients should be advised to stop taking vemurafenib and consult their doctor immediately if skin rash develops.
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960 mg twice daily, for dose adjustment due to
First-line fragment. Read the complete Indications and Dose section above.
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