Dabrafenib for the treatment of melanoma

Bibliography

• Jemal A, Saraiya M, Patel P, et al. Recent trends in cutaneous melanoma incidence and death rates in the United States, 1992-2006. J Am Acad Dermatol 2011;65(5 Suppl 1):S17-25. e3
   PubMed Web of Science ®Google Scholar
• Davies H, Bignell GR, Cox C, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417:949-54
   PubMed Web of Science ®Google Scholar
• Jakob JA, Bucheit AD, Syklawer E, et al. Clinical characteristics and outcomes with specific BRAF and NRAS mutations in metastatic melanoma patients. Cancer 2013;119(21):3821-9
   PubMedGoogle Scholar
• Long GV, Menzies AM, Nagrial AM, et al. Prognostic and clinicopathologic associations of oncogenic BRAF in metastatic melanoma. J Clin Oncol 2011;29(10):1239-46
   PubMed Web of Science ®Google Scholar
• Bauer J, Buttner P, Murali R, Westra WH. BRAF mutations in cutaneous melanoma are independently associated with age, anatomic site of the primary tumor and the degree of solar elastosis at the primary tumor site. Pigment Cell Melanoma Res 2011;24:345-51
   PubMed Web of Science ®Google Scholar
• Falchook GS, Long GV, Kurzrock R, et al. Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial. Lancet 2012;379:1893-901
   PubMed Web of Science ®Google Scholar
• Long GV, Trefzer U, Davies MA, et al. Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MD): a multicenter, open-label, phase 2 trial. Lancet Oncol 2012;13:1087-95
   PubMed Web of Science ®Google Scholar
• Hingorani SR, Jacobetz MA, Robertson GP, et al. Suppression of BRAF(V599E) in human melanoma abrogates transformation. Cancer Res 2003;63:5198-202
   PubMed Web of Science ®Google Scholar
• Yang H, Higgins B, Kolinsky K, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res 2010;70:5518-27
   PubMed Web of Science ®Google Scholar
• Eisen T, Ahmad T, Flaherty KT, et al. Sorafenib in advanced melanoma: a Phase II randomized discontinuation trial analysis. Br J Cancer 2006;95:581-6
   PubMed Web of Science ®Google Scholar
• Tsai J, Lee JT, Zhang J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci USA 2008;105:3041-6
   PubMed Web of Science ®Google Scholar
• King AJ, Arnone MR, Bleam MR, et al. Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions. PLoS One 2013;8(7):e67583
   PubMed Web of Science ®Google Scholar
• Dabrafenib package insert. Available from: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
   Google Scholar
• Gentilcore G, Madonna G, Mozzillo N, et al. Effect of dabrafenib on melanoma cell lines harbouring the BRAF V600D/R mutations. BMC Cancer 2013;13:17-20
   PubMed Web of Science ®Google Scholar
• Denton DL, Minthorn E, Carson SW, et al. Concomitant oral and intravenous pharmacokinetics of dabrafenib, a BRAF inhibitor, in patients with BRAF V600 mutation-positive solid tumors. J Clin Pharmacol 2013;53:955-61
   PubMed Web of Science ®Google Scholar
• Bershas DA, Ouellet D, Mamaril-Fishman DL, et al. Metabolism and disoposition of oral dabrafenib in cancer patients: proposed participation of aryl nitrogen in carbon-carbon bond cleavage via decarboxylation following enzymatic oxidation. Drug Metab Dispos 2013;41:2215-24
   PubMed Web of Science ®Google Scholar
• Ascierto PA, Minor D, Ribas A, et al. Phase II trial (BREAK-2) of the BRAF inhibitor dabrafenib (GSK2118436) in patients with metastatic melanoma. J Clin Oncol 2013;31(25):3205-11
   PubMedGoogle Scholar
• Hauschild A, Grob JJ, Demidov LV, et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicenter, open-label, phase 3 randomised controlled trial. Lancet 2012;380:358-65
   PubMed Web of Science ®Google Scholar
• Hauschild A, Grob JJ, Demidov LV, et al. An update on BREAK-3, a phase III, randomized trial: dabrafenib (DAB) versus dacarbazine (DTIC) in patients with BRAF V600E-positive mutation metastatic melanoma (MM). J Clin Oncol 2013;31(Suppl 15):9013
   Google Scholar
• Chapman PB, Hauschild A, Robert C, et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 2011;264:2507-16
   Google Scholar
• Chapman PB, Hauschild A, Robert C, et al. Updated overall survival (OS) results for BRIM-3, a phase III randomized, open-label, multicenter trial comparing BRAF inhibitor vemurafenib (vem) with dacarbazine (DTIC) in previously untreated patients with BRAFV660E-mutated melanoma [abstract 8502]. Presented at: ASCO Annual Meeting; 31–May 4 June 2012; Chicago, IL
   Google Scholar
• Carlino MS, Fogarty GB, Long GV. Treatment of melanoma brain metastases. Cancer J 2012;18:208-12
   PubMedGoogle Scholar
• Davies MA, Liu P, McIntyre S, et al. Prognostic factors for survival in melanoma patients with brain metastases. Cancer 2011;117:1687-96
   PubMed Web of Science ®Google Scholar
• Johannessen CM, Boehm JS, Kim SY, et al. COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 2010;468:968-72
   PubMed Web of Science ®Google Scholar
• Nazarian R, Shi H, Wang Q, et al. Melanomas acquire resistance to B-RAF (V600E) inhibition by RTK or N-RAS upregulation. Nature 2010;468:973-9
   PubMed Web of Science ®Google Scholar
• Poulikakos PI, Persaud Y, Janakiraman M, et al. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature 2011;480:387-90
   PubMed Web of Science ®Google Scholar
• Flaherty KT, Infante JR, Daud A, et al. Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations. N Engl J Med 2012;367:1694-703
   PubMed Web of Science ®Google Scholar
• Flaherty KT, Puzanov I, Kim KB, et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med 2010;363:809-19
   PubMed Web of Science ®Google Scholar
• Su F, Viros A, Milagre C, et al. RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors. N Engl J Med 2012;366:207-15
   PubMed Web of Science ®Google Scholar
• Heidorn SJ, Milagre C, Whittaker S, et al. Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF. Cell 2010;140:209-21
   PubMed Web of Science ®Google Scholar
• Hatzivassiliou G, Song K, Yen I, et al. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 2010;464:431-5
   PubMed Web of Science ®Google Scholar
• Poulikakos PI, Zhang C, Bollag G, et al. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 2010;464:427-30
   PubMed Web of Science ®Google Scholar
• Topalian SL, Hodi FS, Brahmer JR, et al. Safety, activity, and immune correlates of anti–PD-1 antibody in cancer. N Engl J Med 2012;366:2443-54
   PubMed Web of Science ®Google Scholar
• Brahmer JR, Tykodi SS, Chow LQM, et al. Safety and activity of anti–PD-L1 antibody in patients with advanced cancer. N Engl J Med 2012;366:2455-65
   PubMed Web of Science ®Google Scholar
• Hamid O, Robert C, Daud A, et al. Safety and tumor responses with lambrolizumab (Anti–PD-1) in melanoma. N Engl J Med 2013;369:134-44
   PubMed Web of Science ®Google Scholar