Current State of Target Treatment in BRAF Mutated Melanoma

Ascierto, 2020, Update on tolerability and overall survival in COLUMBUS: landmark analysis of a randomised phase 3 trial of encorafenib plus binimetinib vs vemurafenib or encorafenib in patients with BRAF V600-mutant melanoma., Eur. J. Cancer, 126, 33, 10.1016/j.ejca.2019.11.016

Atkinson, 2020, Dabrafenib plus trametinib is effective in the treatment of BRAF V600-mutated metastatic melanoma patients: analysis of patients from the dabrafenib plus trametinib Named Patient Program (DESCRIBE II)., Melanoma Res., 30, 261, 10.1097/CMR.0000000000000654

Boni, 2010, Selective BRAFV600E inhibition enhances T-cell recognition of melanoma without affecting lymphocyte function., Cancer Res., 70, 5213, 10.1158/0008-5472.CAN-10-0118

Callahan, 2012, Progression of RAS-mutant leukemia during RAF inhibitor treatment., N. Engl. J. Med., 367, 2316, 10.1056/NEJMoa1208958

Carlino, 2014, Differential activity of MEK and ERK inhibitors in BRAF inhibitor resistant melanoma., Mol. Oncol., 8, 544, 10.1016/j.molonc.2014.01.003

Chan, 2014, The nature and management of metastatic melanoma after progression on BRAF inhibitors: effects of extended BRAF inhibition., Cancer, 120, 3142, 10.1002/cncr.28851

Chapman, 2011, Improved survival with vemurafenib in melanoma with BRAF V600E mutation., N. Engl. J. Med., 364, 2507, 10.1056/NEJMoa1103782

Chapman, 2017, Vemurafenib in patients with BRAFV600 mutation-positive metastatic melanoma: final overall survival results of the randomized BRIM-3 study., Ann. Oncol., 28, 2581, 10.1093/annonc/mdx339

2020

Dalle, 2013, Second primary melanomas on treatment with vemurafenib., Br. J. Dermatol., 168, 887, 10.1111/bjd.12093

Davies, 2011, Prognostic factors for survival in melanoma patients with brain metastases., Cancer, 117, 1687, 10.1002/cncr.25634

Davies, 2017, Dabrafenib plus trametinib in patients with BRAFV600-mutant melanoma brain metastases (COMBI-MB): a multicentre, multicohort, open-label, phase 2 trial., Lancet Oncol., 18, 863, 10.1016/S1470-2045(17)30429-1

Dréno, 2018, Health-related quality of life impact of cobimetinib in combination with vemurafenib in patients with advanced or metastatic BRAFV600 mutation-positive melanoma., Br. J. Cancer, 118, 777, 10.1038/bjc.2017.488

Dummer, 2017, Results of COLUMBUS Part 2: a phase 3 trial of encorafenib (ENCO) plus binimetinib (BINI) versus ENCO in BRAF-mutant melanoma., Ann. Oncol., 28, v428, 10.1093/annonc/mdx377.002

Dummer, 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol., 19, 603, 10.1016/S1470-2045(18)30142-6

Eisen, 2006, Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis., Br. J. Cancer, 95, 581, 10.1038/sj.bjc.6603291

Flaherty, 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med., 367, 1694, 10.1056/NEJMoa1210093

Frederick, 2013, BRAF inhibition is associated with enhanced melanoma antigen expression and a more favorable tumor microenvironment in patients with metastatic melanoma., Clin. Cancer Res., 19, 1225, 10.1158/1078-0432.CCR-12-1630

Gaestel, 2006, MAPKAP kinases - MKs - two’s company, three’s a crowd. Nature reviews., Mol. Cell Biol., 7, 120, 10.1038/nrm1834

2015, Genomic classification of cutaneous melanoma., Cell, 161, 1681, 10.1016/j.cell.2015.05.044

Gibney, 2013, Paradoxical oncogenesis–the long-term effects of BRAF inhibition in melanoma., Nat. Rev. Clin. Oncol., 10, 390, 10.1038/nrclinonc.2013.83

2019

González-Cao, 2015, Other targeted drugs in melanoma., Ann. Transl. Med., 3, 10.3978/j.issn.2305-5839.2015.08.12

Grob, 2015, Comparison of dabrafenib and trametinib combination therapy with vemurafenib monotherapy on health-related quality of life in patients with unresectable or metastatic cutaneous BRAF Val600-mutation-positive melanoma (COMBI-v): results of a phase 3, open-label, randomised trial., Lancet Oncol., 16, 1389, 10.1016/S1470-2045(15)00087-X

Hauschild, 2009, Results of a phase III, randomized, placebo-controlled study of sorafenib in combination with carboplatin and paclitaxel as second-line treatment in patients with unresectable stage III or stage IV melanoma., J. Clin. Oncol., 27, 2823, 10.1200/JCO.2007.15.7636

Hauschild, 2018, Longer Follow-Up Confirms Relapse-Free Survival Benefit With Adjuvant Dabrafenib Plus Trametinib in Patients With Resected BRAF V600-Mutant Stage III Melanoma., J. Clin. Oncol., 36, 3441, 10.1200/JCO.18.01219

Hauschild, 2012, Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial., Lancet, 380, 358, 10.1016/S0140-6736(12)60868-X

Heidorn, 2010, Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF., Cell, 140, 209, 10.1016/j.cell.2009.12.040

Kakavand, 2015, PD-L1 Expression and Tumor-Infiltrating Lymphocytes Define Different Subsets of MAPK Inhibitor-Treated Melanoma Patients., Clin. Cancer Res., 21, 3140, 10.1158/1078-0432.CCR-14-2023

Khalili, 2012, Oncogenic BRAF(V600E) promotes stromal cell-mediated immunosuppression via induction of interleukin-1 in melanoma., Clin. Cancer Res., 18, 5329, 10.1158/1078-0432.CCR-12-1632

King, 2013, Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions., PLoS One, 8, 10.1371/journal.pone.0067583

Korn, 2008, Meta-Analysis of Phase II Cooperative Group Trials in Metastatic Stage IV Melanoma to Determine Progression-Free and Overall Survival Benchmarks for Future Phase II Trials., JCO, 26, 527, 10.1200/JCO.2007.12.7837

Koya, 2012, BRAF inhibitor vemurafenib improves the antitumor activity of adoptive cell immunotherapy., Cancer Res., 72, 3928, 10.1158/0008-5472.CAN-11-2837

Kuczynski, 2013, Drug rechallenge and treatment beyond progression—implications for drug resistance., Nat. Rev. Clin. Oncol., 10, 571, 10.1038/nrclinonc.2013.158

Larkin, 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med., 371, 1867, 10.1056/NEJMoa1408868

Latimer, 2015, Adjusting for the Confounding Effects of Treatment Switching-The BREAK-3 Trial: dabrafenib Versus Dacarbazine., Oncologist, 20, 798, 10.1634/theoncologist.2014-0429

Long, , Dabrafenib plus trametinib versus dabrafenib monotherapy in patients with metastatic BRAF V600E/K-mutant melanoma: long-term survival and safety analysis of a phase 3 study., Ann. Oncol., 28, 1631, 10.1093/annonc/mdx176

Long, , Adjuvant Dabrafenib plus Trametinib in Stage III BRAF-Mutated Melanoma., N. Engl. J. Med., 377, 1813, 10.1056/NEJMoa1708539

Long, 2020, Multidisciplinary approach to brain metastasis from melanoma: the emerging role of systemic therapies., Am. Soc. Clin. Oncol. Educ. Book, 2013, 393

Long, 2014, Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma., N. Engl. J. Med., 371, 1877, 10.1056/NEJMoa1406037

Long, 2015, Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trial., Lancet, 386, 444, 10.1016/S0140-6736(15)60898-4

Long, 2012, Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial., Lancet Oncol., 13, 1087, 10.1016/S1470-2045(12)70431-X

Long, 2016, Overall Survival and Durable Responses in Patients With BRAF V600-Mutant Metastatic Melanoma Receiving Dabrafenib Combined With Trametinib., J. Clin. Oncol., 34, 871, 10.1200/JCO.2015.62.9345

Lovly, 2012, Routine multiplex mutational profiling of melanomas enables enrollment in genotype-driven therapeutic trials., PLoS One, 7, 10.1371/journal.pone.0035309

Maio, 2018, Adjuvant vemurafenib in resected, BRAFV600 mutation-positive melanoma (BRIM8): a randomised, double-blind, placebo-controlled, multicentre, phase 3 trial., Lancet Oncol., 19, 510, 10.1016/S1470-2045(18)30106-2

Manzano, 2016, Resistant mechanisms to BRAF inhibitors in melanoma., Ann. Transl. Med., 4, 10.21037/atm.2016.06.07

Mcarthur, 2016, Vemurafenib in Metastatic melanoma patients with brain metastases: an Open-Label, Single-Arm, Phase 2, Multicentre Study., Ann. Oncol., 28, 634, 10.1093/annonc/mdw641

McArthur, 2014, Safety and efficacy of vemurafenib in BRAFV600E and BRAFV600K mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study., Lancet Oncol., 15, 323, 10.1016/S1470-2045(14)70012-9

Menzies, 2012, Distinguishing Clinicopathologic Features of Patients with V600E and V600K BRAF-Mutant Metastatic Melanoma., Clin. Cancer Res., 18, 3242, 10.1158/1078-0432.CCR-12-0052

Michielin, 2019, Electronic address: [email protected]. Cutaneous melanoma: ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up†., Ann. Oncol., 30, 1884, 10.1093/annonc/mdz411

Minor, 2015, Severe gastrointestinal toxicity with administration of trametinib in combination with dabrafenib and ipilimumab., Pigment Cell Melanoma Res., 28, 611, 10.1111/pcmr.12383

Morris, 2013, Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors., Cancer Discov., 3, 742, 10.1158/2159-8290.CD-13-0070

Nazarian, 2010, Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation., Nature, 468, 973, 10.1038/nature09626

Nissan, 2013, ERK pathway inhibitors: how low should we go?, Cancer Discov., 3, 719, 10.1158/2159-8290.CD-13-0245

Pasquali, 2018, Systemic treatments for metastatic cutaneous melanoma., Cochrane Database. Syst. Rev., 2, 10.1002/14651858.CD011123.pub2

Poulikakos, 2010, RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF., Nature, 464, 427, 10.1038/nature08902

Queirolo, 2017, BRAF plus MEK-targeted drugs: a new standard of treatment for BRAF-mutant advanced melanoma., Cancer Metastasis Rev., 36, 35, 10.1007/s10555-017-9660-6

Reschke, 2019, Rechallenge of targeted therapy in metastatic melanoma., J. Dtsch. Dermatol. Ges., 17, 483, 10.1111/ddg.13766

Ribas, 2014, Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study., Lancet Oncol., 15, 954, 10.1016/S1470-2045(14)70301-8

Ribas, 2016, Pembrolizumab (pembro) in combination with dabrafenib (D) and trametinib (T) for BRAF -mutant advanced melanoma: Phase 1 KEYNOTE-022 study., J. Clin. Oncol., 34, 3014, 10.1200/JCO.2016.34.15_suppl.3014

Ribas, 2013, Hepatotoxicity with combination of vemurafenib and ipilimumab., N. Engl. J. Med., 368, 1365, 10.1056/NEJMc1302338

Robarge, 2014, Abstract DDT02-03: discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development., Cancer Res., 74, 10.1158/1538-7445.AM2014-DDT02-03

Robert, 2019, Five-Year Outcomes with Dabrafenib plus Trametinib in Metastatic Melanoma., N. Engl. J. Med., 381, 626, 10.1056/NEJMoa1904059

Robert, 2015, Improved overall survival in melanoma with combined dabrafenib and trametinib., N. Engl. J. Med., 372, 30, 10.1056/NEJMoa1412690

Robert, 2016, Three-year estimate of overall survival in COMBI-v, a randomized phase 3 study evaluating first-line dabrafenib (D) + trametinib (T) in patients (pts) with unresectable or metastatic BRAF V600E/K–mutant cutaneous melanoma., Ann. Oncol., 27, 1, 10.1093/annonc/mdw435.37

Rubinstein, 2010, Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032., J. Transl. Med., 8, 10.1186/1479-5876-8-67

Sanchez-Vega, 2018, Oncogenic Signaling pathways in the cancer genome atlas., Cell, 173, 321, 10.1016/j.cell.2018.03.035

Sapkota, 2013, Vemurafenib enhances MHC induction in BRAFV600E homozygous melanoma cells., Oncoimmunology, 2, 10.4161/onci.22890

Schadendorf, 2015, Health-related quality of life impact in a randomised phase III study of the combination of dabrafenib and trametinib versus dabrafenib monotherapy in patients with BRAF V600 metastatic melanoma., Eur. J. Cancer, 51, 833, 10.1016/j.ejca.2015.03.004

Scholtens, 2015, Vemurafenib for BRAF V600 mutated advanced melanoma: results of treatment beyond progression., Eur. J. Cancer, 51, 642, 10.1016/j.ejca.2015.01.009

Shi, 2014, Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy., Cancer Discov., 4, 80, 10.1158/2159-8290.CD-13-0642

2017, Pigment Cell & Melanoma Research, 76, 10.1111/pcmr.12547

2019

Spagnolo, 2019, The adjuvant treatment revolution for high-risk melanoma patients., Semin. Cancer Biol., 59, 283, 10.1016/j.semcancer.2019.08.024

Spagnolo, 2015, BRAF-mutant melanoma: treatment approaches, resistance mechanisms, and diagnostic strategies., Oncol. Targets Ther., 8, 157, 10.2147/OTT.S39096

Spagnolo, 2016, Survival of patients with metastatic melanoma and brain metastases in the era of MAP-kinase inhibitors and immunologic checkpoint blockade antibodies: a systematic review., Cancer Treat. Rev., 45, 38, 10.1016/j.ctrv.2016.03.003

Straussman, 2012, Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion., Nature, 487, 500, 10.1038/nature11183

Su, 2012, RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors., N. Engl. J. Med., 366, 207, 10.1056/NEJMoa1105358

Van Allen, 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov., 4, 94, 10.1158/2159-8290.CD-13-0617

Vanni, 2020, The current state of molecular testing in the BRAF-Mutated melanoma landscape., Front. Mol. Biosci., 7, 10.3389/fmolb.2020.00113

Villanueva, 2010, Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K., Cancer Cell, 18, 683, 10.1016/j.ccr.2010.11.023

Wilson, 2012, Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors., Nature, 487, 505, 10.1038/nature11249

Wong, 2014, Antitumor activity of the ERK inhibitor SCH772984 [corrected] against BRAF mutant. NRAS mutant and wild-type melanoma., Mol. Cancer, 13, 10.1186/1476-4598-13-194

Zimmer, 2012, Atypical melanocytic proliferations and new primary melanomas in patients with advanced melanoma undergoing selective BRAF inhibition., J. Clin. Oncol., 30, 2375, 10.1200/JCO.2011.41.1660