ISSUE 1374
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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
... more1. MS Ernstoff. Been there, not done that – melanoma in the age of molecular therapy. N Engl J Med 2011; 364:2547.
2. S Bhatia et al. Treatment of metastatic melanoma: an overview. Oncology 2009; 23:488.
4. Ipilimumab (Yervoy) for metastatic melanoma. Med Lett Drugs Ther 2011; 53:51.
6. A Ribas et al. BRIM-2: An open-label, multicenter phase II study of vemurafenib in previously treated patients with BRAF V600E mutation-positive metastatic melanoma. J Clin Oncol 2011; 29 suppl:528S, abstract 8509.
7. Cost according to the manufacturer.
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Article code: 1374b
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