Overcoming metastatic melanoma with BRAF inhibitors
ABSTRACT Melanoma has the capacity to spread via the blood stream to the brain, and has been notoriously resistant to drug therapy.
An activating mutation in the gene encoding BRAF is known to be responsible for half of melanomas. This article provides a
review of GSK2118436 and PLX4032 as potential therapeutics for the treatment of melanomas by inhibiting oncogenic BRAF.
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ABSTRACT: Metastatic melanoma (MM) presents a treatment challenge to oncologists worldwide. Dacarbazine is the first line chemotherapy treatment for MM, though the overall response rates are very poor. Recently, the v-raf murine sarcoma viral oncogene homolog B1 (BRAF) V600 mutation was found to play a main role in MM. This mutation is present in 40-60% of melanoma patients. Vemurafenib is a BRAF kinase inhibitor that showed impressive results in phase I-III trials and was thus recently approved for the treatment of MM. This paper will briefly focus on vemurafenib in the treatment of MM and highlight concerns.Rare tumors 04/2012; 4(2):e31.