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Mutations in BRAF and KRAS characterize the development of low-grade ovarian serous carcinoma
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Tsai, J.; Lee, J.; Wang, W.; Zhang, J.; Cho, H.; Mamo, S.; Bremer, R.; Gillette, S.; Kong, J.; Haass, N.; Sproesser, K.; Li, L.; Smalley, K.; Fong, D.; Zhu, Y.-L.; Marimuthu, A.; Nguyen, H.; Lam, W.; Liu, J.; Cheung, I.; Rice, J.; Suzuki, Y.; Luu, C.; Settachatgul, C.; Shellooe, R.; Cantwell, J.; Kim, S.-H.; Schlessinger, J.; Zhang, K.; West, B.; Powell, B.; Habets, G.; Zhang, C.; Ibrahim, P.; Hirth, P.; Artis, D.; Herlyn, M.; Bollag, G. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity Proc. Natl. Acad. Sci. U.S.A. 2008, 105, 3041-3046 (Pubitemid 351723664)
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Improved survival with vemurafenib in melanoma with BRAF V600E mutation
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Chapman, P.; Hauschild, A.; Robert, C.; Haanen, J.; Ascierto, P.; Larkin, J.; Dummer, R.; Garbe, C.; Testori, A.; Maio, M.; Hogg, D.; Lorigan, P.; Lebbe, C.; Jouary, T.; Schadendorf, D.; Ribas, A.; O'Day, S.; Sosman, J.; Kirkwood, J.; Eggermont, A.; Dreno, B.; Nolop, K.; Li, J.; Nelson, B.; Hou, J.; Lee, R.; Flaherty, K. Improved survival with vemurafenib in melanoma with BRAF V600E mutation N. Engl. J. Med. 2011, 364, 2507-2516
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V600E Inhibitors Containing an Arylsulfonamide Headgroup Bioorg. Med. Chem. Lett. 2011, 21, 4436-4440
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For a thorough biological characterization of dabrafenib, see: Novel Selective BRAF Inhibitor (GSK2118436; dabrafenib) with Demonstration of Increased Efficacy and Reduced Skin Lesions by Combining BRAF and MEK Inhibitors. Manuscript in preparation.
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For a thorough biological characterization of dabrafenib, see: King, A.; Arnone, M.; Bleam, M.; Moss, K.; Yang, J.; Fisher, K.; Smitheman, K.; Erhardt, J.; Hughes-Earle, A.; Kane-Carson, L.; Sinnamon, R.; Qi, H.; Rheault, T.; Uehling, D.; Laquerre, S. Novel Selective BRAF Inhibitor (GSK2118436; dabrafenib) with Demonstration of Increased Efficacy and Reduced Skin Lesions by Combining BRAF and MEK Inhibitors. Manuscript in preparation.
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Dabrafenib in BRAF-mutated metastatic melanoma: A multicentre, open-label, phase 3 randomised controlled trial
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Hauschild, A.; Grob, J.; Demidov, L.; Jouary, T.; Gutzmer, R.; Millward, M.; Rutkowski, P.; Blank, C.; Miller, W.; Kaempgen, E.; Martín-Algarra, S.; Karaszewska, B.; Mauch, C.; Chiarion-Sileni, V.; Martin, A.; Swann, S.; Haney, P.; Mirakhur, B.; Guckert, M.; Goodman, V.; Chapman, P. Dabrafenib in BRAF-mutated metastatic melanoma: A multicentre, open-label, phase 3 randomised controlled trial Lancet 2012, 380, 358-365
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Falchook, G.; Long, G.; Kurzrock, R.; Kim, K.; Arkenau, T.; Brown, M.; Hamid, O.; Infante, J.; Millward, M.; Pavlick, A.; O'Day, S.; Blackman, S.; Curtis, C.; Lebowitz, P.; Ma, B.; Ouellet, D.; Kefford, R. Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial Lancet 2012, 379, 1893-1901
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Updated safety and efficacy results from a phase I/II study of the oral BRAF inhibitor dabrafenib (GSK2118436) combined with the oral MEK 1/2 inhibitor trametinib (GSK1120212) in patients with BRAFi-naive metastatic melanoma
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Weber, J.; Flaherty, K.; Infante, J.; Falchook, G.; Kefford, R.; Daud, A.; Hamid, O.; Gonzalez, R.; Kudchadkar, R.; Lawrence, D.; Burris, H.; Long, G.; Algazi, A.; Lewis, K.; Kim, K.; Puzanov, I.; Sun, P.; Little, S.; Patel, K.; Sosman, J. Updated safety and efficacy results from a phase I/II study of the oral BRAF inhibitor dabrafenib (GSK2118436) combined with the oral MEK 1/2 inhibitor trametinib (GSK1120212) in patients with BRAFi-naive metastatic melanoma ASCO Meeting Abstracts 2012, 30, 8510
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