507
Views
7
CrossRef citations to date
0
Altmetric
Drug Evaluation

Future of combination therapy with dabrafenib and trametinib in metastatic melanoma

, MPH, , MS (Cutaneous Oncology Clinical Trial Coordinator) & , MD (Cutaneous Oncologist)

Bibliography

  • SEER Cancer Statistics Factsheets. Melanoma of the Skin. 2015
  • Balch CM, Gershenwald JE, Soong SJ, et al. Final version of 2009 AJCC melanoma staging and classification. J Clin Oncol 2009;27(36):6199-206
  • Wan PT, Garnett MJ, Roe SM, et al. Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell 2004;116(6):855-67
  • Baiter M, Schuler G, Hartmann A, et al. Pathogenic implications of BRAF mutation distribution in stage IV melanoma patients. Dermatology 2015;231(2):127-33
  • Tran NH, Wu X, Frost JA. B-Raf and Raf-1 are regulated by distinct autoregulatory mechanisms. J Biol Chem 2005;280(16):16244-53
  • Huang T, Karsy M, Zhuge J, et al. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol 2013;6:30
  • Wu J, Rosenbaum E, Begum S, Westra WH. Distribution of BRAF T1799A(V600E) mutations across various types of benign nevi: implications for melanocytic tumorigenesis. Am J Dermatopathol 2007;29(6):534-7
  • Pfeiffer V, Gotz R, Xiang C, et al. Ablation of BRaf impairs neuronal differentiation in the postnatal hippocampus and cerebellum. PLoS One 2013;8(3):e58259
  • Luke JJ, Ott PA. New developments in the treatment of metastatic melanoma – role of dabrafenib-trametinib combination therapy. Drug Healthc Patient Saf 2014;6:77-88
  • Menzies AM, Long GV. Dabrafenib and trametinib, alone and in combination for BRAF-mutant metastatic melanoma. Clin Cancer Res 2014;20(8):2035-43
  • Flaherty KT, Robert C, Hersey P, et al. Improved survival with MEK inhibition in BRAF-mutated melanoma. N Engl J Med 2012;367(2):107-14
  • Hauschild A, Grob JJ, Demidov LV, et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet 2012;380(9839):358-65
  • Kim KB, Kefford R, Pavlick AC, et al. Phase II study of the MEK1/MEK2 inhibitor Trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitor. J Clin Oncol 2013;31(4):482-9
  • Long GV, Fung C, Menzies AM, et al. Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma. Nat Commun 2014;5:5694
  • Federal Drug Administration. TAFINLAR (dabrafenib) full prescribing information. Silver Spring; MD: 2014
  • Federal Drug Administration. MEKINIST (trametinib) full prescribing information. Silver Spring; MD: 2014
  • 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
  • Gilmartin AG, Bleam MR, Groy A, et al. GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin Cancer Res 2011;17(5):989-1000
  • Roberts PJ, Der CJ. Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer. Oncogene 2007;6(22):3291-310
  • Nakazumi H, Sasano H, Iino K, et al. Expression of cell cycle inhibitor p27 and Ki-67 in human adrenocortical neoplasms. Mod Pathol 1998;1(12):1165-70
  • Falchook GS, Long GV, Kuzrock R, et al. Dose selection, pharmacokinetics and pharmacodynamics of BRAF inhibitor dabrafenib (GSK2118436). Clin Cancer Res 2014;20(17):4449-58
  • Infante JR, Fecher LA, Falchook GS, et al. Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial. Lancet Oncol 2012;13(8):773-81
  • Denton CL, 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(9):955-61
  • 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(26):3205-11
  • Falchook GS, Long GV, Kuzrock R, et al. Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial. Lancet 2012;379(9829):1893-901
  • Falchook GS, Lewis KD, Infante JR, et al. Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial. Lancet Oncol 2012;13(8):782-9
  • Azer MW, Menzies AM, Haydu LE, et al. Patterns of response and progression in patients with BRAF-mutant melanoma metastatic to the brain who were treated with dabrafenib. Cancer 2014;120(4):530-6
  • Flaherty KT, Infante JR, Daud A, et al. Combined BRAF and MEK inhibition in melanoma with BRAFV600 mutations. N Engl J Med 2012;367(18):1694-703
  • Ascierto PA, Marincola FM, Atkins MB. What’s new in melanoma? Combination!. J Transl Med 2015;213
  • Robert C, Karaszewska B, Schachter J, et al. Improved overall survival in melanoma with combined dabrafenib and trametinib. N Engl J Med 2015;372(1):30-9
  • Larkin J, Ascierto PA, Dreno B, et al. Combined vemurafenib and cobimetinib in BRAF-mutated melanoma. N Engl J Med 2014;371(20):1867-76
  • Long GV, Stroyakovskiy D, Gogas H, et al. Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicenter, double-blind, phase 3 randomised controlled trial. Lancet 2015;386(9992):444-51
  • Menzies AM, Ashworth MT, Swann S, et al. Characteristics of pyrexia in BRAFV600E/K metastatic melanoma patients treated with combined dabrafenib and trametinib in a phase I/II clinical trial. Ann Oncol 2015;26(2):415-21
  • Joseph EW, Pratilas CA, Poulikakos PI, et al. The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in V600E BRAF-selective manner. Proc Natl Acad Sci 2010;107(33):14903-8
  • Shi H, Moriceau G, Kong X, et al. Melanoma whole-exome sequencing identifies V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistance. Nat Commun 2012;6(3):724
  • Paraiso KH, Fedorenko IV, Cantini LP, et al. Recovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibotr therapy. Br J Cancer 2010;102(12):172-30
  • 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(3):207-15
  • Sun C, Wang L, Huang S, et al. Reversible and adaptive resistance to BRAF V600E inhibition in melanoma. Nature 2014;508(7494):118-22
  • Goldinger SM, Zimmer L, Schulz C, et al. Upstream mitogen-activated protein kinase (MAPK) pathway inhibition: MEK inhibitor followed by a BRAF inhibitor in advanced melanoma patients. Eur J Cancer 2014;50(2):406-10

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.