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Inhibition of Mutated, Activated BRAF in Metastatic Melanoma
Refractory Metastatic BRAF-Mutated Melanoma Responds to PLX4032
KT Flaherty, I Puzanov, KB Kim, A Ribas, GA McArthur, JA Sosman, PJ O'Dwyer, RJ Lee, JF Grippo, K Nolop, PB Chapman
Yes
20100726
2010 Aug 26
N Engl J Med
Inhibition of Mutated, Activated BRAF in Metastatic Melanoma
N Engl J Med. 2010 Aug 26;363809-819, KT Flaherty, I Puzanov, KB Kim, A Ribas, GA McArthur, JA Sosman, PJ O'Dwyer, RJ Lee, JF Grippo, K Nolop, PB Chapman
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Abstract
SUMMARY
OncologySTAT Editorial Team
Metastatic melanoma, an aggressive disease with few therapeutic options, carries a median overall survival of less than 8 months in patients treated with dacarbazine. A large percentage of melanomas are associated with an activating mutation of the serine/threonine kinase, BRAF. Most BRAF mutations (90%) cause a substitution of glutamic acid for valine at residue 600 (V600E), resulting in constitutive activation of the MAP kinase pathway. PLX4032 is a potent, orally administered BRAF inhibitor shown...