Novel Targeted Therapies for Metastatic Melanoma

Cancer Journal (United States)

Volumn 23, Issue 1, 2017, Pages 54-58

  Iams, Wade T ^a   Sosman, Jeffrey A ^a   Chandra, Sunandana ^a  

^a NORTHWESTERN UNIVERSITY   (United States)

Author keywords

BRAF inhibition; MEK inhibition; melanoma; novel targeted therapy; oncogene targeted therapy

Indexed keywords

B RAF KINASE; B RAF KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE; NEUROFIBROMIN; BRAF PROTEIN, HUMAN; MITOGEN ACTIVATED PROTEIN KINASE KINASE KINASE; MTOR PROTEIN, HUMAN; PROTEIN KINASE INHIBITOR; TARGET OF RAPAMYCIN KINASE;

ENZYME INHIBITION; GENETICS; HUMAN; METASTATIC MELANOMA; MOLECULARLY TARGETED THERAPY; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; REVIEW; UVEA MELANOMA; ANTAGONISTS AND INHIBITORS; ENZYMOLOGY; MELANOMA; RANDOMIZED CONTROLLED TRIAL (TOPIC);

HUMANS; MAP KINASE KINASE KINASES; MELANOMA; MOLECULAR TARGETED THERAPY; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS B-RAF; RANDOMIZED CONTROLLED TRIALS AS TOPIC; TOR SERINE-THREONINE KINASES;

EID: 85011554570     PISSN: 15289117     EISSN: 1540336X     Source Type: Journal    
DOI: 10.1097/PPO.0000000000000242     Document Type: Review

References (51)

1. Balch CM, Gershenwald JE, Soong SJ, et al. Final version of 2009 AJCC melanoma staging and classification. J Clin Oncol. 2009;27:6199-6206.
2. Genomic Classification of Cutaneous Melanoma. Cancer Genome Atlas Network. Cell. 2015;161:1681-1696.
3. Davies H, Bignell GR, Cox C,etal. Mutations of the BRAF gene inhuman cancer. Nature. 2002;417:949-954.
4. Andersen LB, Fountain JW, Gutmann DH, et al. Mutations in the neurofi-bromatosis 1 gene in sporadic malignant melanoma cell lines. Nat Genet. 1993;3:118-121.
5. Curtin JA, Fridlyand J, Kageshita T, et al. Distinct sets of genetic alterations in melanoma. N Engl J Med. 2005;353:2135-2147.
6. Van Raamsdonk CD, Bezrookove V, Green G, et al. Frequent somatic mutations of GNAQ in uveal melanoma and blue naevi. Nature. 2009;457: 599-602.
7. Van Raamsdonk CD, Griewank KG, Crosby MB, et al. Mutations in GNA11 in uveal melanoma. N Engl J Med. 2010;363:2191-2199.
8. Alexandrov LB, Nik-Zainal S, Wedge DC, et al. Signatures of mutational processes in human cancer. Nature. 2013;500:415-421.
9. Hodis E, Watson IR, Kryukov GV, et al. A landscape of driver mutations in melanoma. Cell. 2012;150:251-263.
10. Krauthammer M, Kong Y, Ha BH, et al. Exome sequencing identifies recurrent somatic RAC1 mutations in melanoma. Nat Genet. 2012;44: 1006-1014.
11. Chapman PB, Hauschild A, Robert C, et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med. 2011;364:2507-2516.
12. Sosman JA, Kim KB, Schuchter L, et al. Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med. 2012;366: 707-714.
13. 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;380:358-365.
14. Klein O, Clements A, Menzies AM, et al. BRAF inhibitor activity in V600R metastatic melanoma. Eur J Cancer. 2013;49:1073-1079.
15. Zhang C, Spevak W, Zhang Y, et al. RAF inhibitors that evade paradoxical MAPK pathway activation. Nature. 2015;526:583-586.
16. Li Z, Jiang K, Zhu X, et al. Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells. Cancer Lett. 2016;370:332-344.
17. Robert C, Karaszewska B, Schachter J, et al. Improved overall survival in melanoma with combined dabrafenib and trametinib. N Engl J Med. 2015;372:30-39.
18. Long GV, Stroyakovskiy D, Gogas H, et al. Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trial. Lancet. 2015;386:444-451.
19. Larkin J, Ascierto PA, Dréno B, et al. Combined vemurafenib and cobimetinib in BRAF-mutated melanoma. N Engl J Med. 2014;371: 1867-1876.
20. Rizos H, Menzies AM, Pupo GM, et al. BRAF inhibitor resistance mechanisms in metastatic melanoma: spectrum and clinical impact. Clin Cancer Res. 2014;20:1965-1977.
21. Shi H, Hugo W, Kong X, et al. Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy. Cancer Discov. 2014;4: 80-93.
22. Caporali S, Alvino E, Lacal PM, et al. Targeting the PI3K/AKT/mTOR pathway overcomes the stimulating effect of dabrafenib on the invasive behavior of melanoma cells with acquired resistance to the BRAF inhibitor. Int J Oncol. 2016;49:1164-1174.
23. Van Allen EM, Wagle N, Sucker A, et al. The genetic landscape of clinical resistance toRAF inhibition in metastatic melanoma. Cancer Discov. 2014; 4:94-109.
24. Jha S, Morris EJ, Hruza A, et al. Dissecting therapeutic resistance to ERK inhibition. Mol Cancer Ther. 2016;15:548-559.
25. Greger JG, Eastman SD, Zhang V, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012;11:909-920.
26. Carlino MS, Todd JR, Gowrishankar K, et al. Differential activity of MEK and ERK inhibitors in BRAF inhibitor resistant melanoma. Mol Oncol. 2014;8:544-554.
27. Smyth T, Paraiso KH, Hearn K, et al. Inhibition of HSP90 by AT13387 delays the emergence of resistance to BRAF inhibitors and overcomes resistance to dual BRAF and MEK inhibition in melanoma models. Mol Cancer Ther. 2014;13:2793-2804.
28. Vilgelm AE, Pawlikowski JS, Liu Y, et al. Mdm2 and aurora kinasea inhibitors synergize to block melanoma growth by driving apoptosis and immune clearance of tumor cells. Cancer Res. 2015;75:181-193.
29. Wang W, Kang H, Zhao Y, et al. Targeting autophagy sensitizes BRAF-mutant thyroid cancer to vemurafenib. J Clin Endocrinol Metab. 2016;jc20161999.
30. Das Thakur M, Salangsang F, Landman AS, et al. Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance. Nature. 2013;494:251-255.
31. Stephen AG, Esposito D, Bagni RK, et al. Dragging ras back in the ring. Cancer Cell. 2014;25:272-281.
32. Asati V, Mahapatra DK, Bharti SK. PI3K/Akt/mTOR and Ras/Raf/MEK/ ERK signaling pathways inhibitors as anticancer agents: structural and pharmacological perspectives. Eur J Med Chem. 2016;109:314-341.
33. Ascierto PA, Schadendorf D, Berking C, et al. MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study. Lancet Oncol. 2013;14: 249-256.
34. Dummer RSD, Ascierto PA, et al. Results of NEMO: a phase III trial of binimetinib (BINI) vs dacarbazine (DTIC) in NRAS-mutant cutaneous melanoma. J Clin Oncol. 2016;34: abstr 95002016.
35. Sosman JA, Kittaneh M, Lolkema MPJ, et al. A phase 1b/2 study of LEE011 in combination with binimetinib (MEK162) in patients with NRAS-mutant melanoma: early encouraging clinical activity. J Clin Oncol. 2014;9009.
36. Atefi M, Titz B, Avramis E, et al. Combination of pan-RAF and MEK inhibitors in NRAS mutant melanoma. Mol Cancer. 2015;14:27.
37. Conrad WH, Swift RD, Biechele TL, et al. Regulating the response to targeted MEK inhibition in melanoma: enhancing apoptosis in NRAS- and BRAF-mutant melanoma cells with Wnt/β-catenin activation. Cell Cycle. 2012;11:3724-3730.
38. Whittaker SR, Theurillat JP, Van Allen E,et al. A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition. Cancer Discov. 2013;3:350-362.
39. Nissan MH, Pratilas CA, Jones AM, et al. Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence. Cancer Res. 2014;74:2340-2350.
40. Peng SB, Henry JR, Kaufman MD, et al. Inhibition of RAF isoforms and active dimers by LY3009120 leadstoanti-tumor activitiesin RAS or BRAF mutant cancers. Cancer Cell. 2015;28:384-398.
41. Robertson KA, Nalepa G, Yang FC, et al. Imatinib mesylate for plexiform neurofibromas in patients with neurofibromatosis type 1: a phase 2 trial. Lancet Oncol. 2012;13:1218-1224.
42. +/-- and c-KIT-dependent bone marrow. Cell. 2008;135:437-448.
43. Carvajal RD, Antonescu CR, Wolchok JD, et al. KITas a therapeutic target in metastatic melanoma. JAMA. 2011;305:2327-2334.
44. Guo J, Si L, Kong Y, et al. Phase II, open-label, single-arm trial of imatinib mesylate in patients with metastatic melanoma harboring c-KIT mutation or amplification. J Clin Oncol. 2011;29:2904-2909.
45. Hodi FS, Corless CL, Giobbie-HurderA,etal. Imatinib for melanomas harboring mutationally activated or amplified KIT arising on mucosal, acral, and chronically sun-damaged skin. J Clin Oncol. 2013;31:3182-3190.
46. Carvajal RD, Sosman JA, Quevedo JF, et al. Effect of selumetinib vs chemotherapy on progression-free survival in uveal melanoma: a randomized clinical trial. JAMA. 2014;311:2397-2405.
47. Carvajal RD, Piperno-Neumann SEK. SUMIT: phase III, randomized, placebo-controlled, double-blind trial of selumetinib in combination with dacarbazine in patients with metastatic uveal melanoma. Presented at the Society for Melanoma Research Congress, November 18-21, 2015 San Francisco, CA.
48. Tse KF, Jeffers M, Pollack VA, et al. CR011, a fully human monoclonal antibody-auristatin E conjugate, for the treatment of melanoma. Clin Cancer Res. 2006;12:1373-1382.
49. Qian X, Mills E, Torgov M, et al. Pharmacologically enhanced expression of GPNMB increases the sensitivity of melanoma cells to the CR011-vcMMAE antibody-drug conjugate. Mol Oncol. 2008;2:81-93.
50. Williams MD, Esmaeli B, Soheili A, et al. GPNMB expression in uveal melanoma: a potential for targeted therapy. Melanoma Res. 2010;20:184-190.
51. Naumovski L, Junutula JR. Glembatumumab vedotin, a conjugate of an anti-glycoprotein non-metastatic melanoma protein B mAb and monomethyl auristatin E for the treatment of melanoma and breast cancer. Curr Opin Mol Ther. 2010;12:248-257.