The Medical Letter on Drugs and Therapeutics
Vemurafenib (Zelboraf) for Metastatic Melanoma
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Revised 10/14/11: In the Dosage and Cost section, the minimum dose of vemurafenib was changed from 420 mg twice daily to 480 mg twice daily.

The FDA has approved vemurafenib (Zelboraf – Genentech), a kinase inhibitor, for treatment of unresectable or metastatic melanoma with the BRAF V600E mutation, which is found in 30-60% of melanomas. An FDA-approved test can detect the mutation in DNA from melanoma tissue.

MECHANISM OF ACTION — BRAF V600E is a mutated kinase that results in activation of BRAF proteins, which can cause cell proliferation even in the absence of growth factors.1 Vemurafenib inhibits BRAF V600E and some other mutated forms of BRAF serinethreonine kinase.

STANDARD TREATMENT — Treatment options for unresectable or metastatic melanoma are limited. Dacarbazine (DTIC) is generally used, but has not shown a survival benefit. High-dose interleukin-2 (aldesleukin – Proleukin) produced responses in 16% of patients and a complete response in 6%, including some ... more      

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Title: Vemurafenib (Zelboraf) for Metastatic Melanoma
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