Vemurafenib and BRAF inhibition: A new class of treatment for metastatic melanoma

Clinical Cancer Research

Volumn 18, Issue 1, 2012, Pages 9-14

  Luke, Jason J ^a   Hodi, F Stephen ^b  

^a WEILL CORNELL MEDICAL COLLEGE   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

B RAF KINASE; DACARBAZINE; IPILIMUMAB; VEMURAFENIB;

ALOPECIA; ARTHRALGIA; CANCER SURVIVAL; CLINICAL TRIAL (TOPIC); DRUG APPROVAL; DRUG DOSE ESCALATION; DRUG DOSE INCREASE; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG ERUPTION; DRUG TARGETING; DRUG TOLERABILITY; ENZYME INHIBITION; FATIGUE; HUMAN; KERATOACANTHOMA; LIVER FUNCTION; MELANOMA; MUTATION; NONHUMAN; OVERALL SURVIVAL; PHOTOSENSITIVITY; PRIORITY JOURNAL; PRURITUS; QUALITY OF LIFE; RECOMMENDED DRUG DOSE; REVIEW; SIDE EFFECT; SKIN PAPILLOMA; SQUAMOUS CELL CARCINOMA; TREATMENT DURATION; TREATMENT RESPONSE;

ANIMALS; HUMANS; INDOLES; MELANOMA; PROTO-ONCOGENE PROTEINS B-RAF; SULFONAMIDES;

EID: 84855472280     PISSN: 10780432     EISSN: 15573265     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-11-2197     Document Type: Review

References (29)

1. Chapman PB, Einhorn LH, Meyers ML, Saxman S, Destro AN, Panageas KS, et al. Phase III multicenter randomized trial of the Dartmouth regimen versus dacarbazine in patients with metastatic melanoma. J Clin Oncol 1999;17:2745-51. (Pubitemid 29415231)
2. Hodi FS, O'Day SJ, McDermott DF, Weber RW, Sosman JA, Haanen JB, et al. Improved survival with ipilimumab in patients with metastatic melanoma. N Engl J Med 2010;363:711-23.
3. Lopez-Bergami P. The role of mitogen- and stress-activated protein kinase pathways in melanoma. Pigment Cell Melanoma Res 2011;24:902-21.
4. Davies H, Bignell GR, Cox C, Stephens P, Edkins S, Clegg S, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417:949-54. (Pubitemid 34716871)
5. Curtin JA, Fridlyand J, Kageshita T, Patel HN, Busam KJ, Kutzner H, et al. Distinct sets of genetic alterations in melanoma. N Engl J Med 2005;353:2135-47. (Pubitemid 41653105)
6. Matallanas D, Crespo P. New druggable targets in the Ras pathway? Curr Opin Mol Ther 2010;12:674-83.
7. Van Cutsem E, van de Velde H, Karasek P, Oettle H, Vervenne WL, Szawlowski A, et al. Phase III trial of gemcitabine plus tipifarnib compared with gemcitabine plus placebo in advanced pancreatic cancer. J Clin Oncol 2004;22:1430-8. (Pubitemid 41103625)
8. Hauschild A, Agarwala SS, Trefzer U, Hogg D, Robert C, Hersey P, et al. 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 2009;27:2823-30.
9. Eisen T, Ahmad T, Flaherty KT, Gore M, Kaye S, Marais R, et al. Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis. Br J Cancer 2006;95:581-6. (Pubitemid 44325897)
10. Bollag G, Hirth P, Tsai J, Zhang J, Ibrahim PN, Cho H, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 2010;467:596-9.
11. Joseph EW, Pratilas CA, Poulikakos PI, Tadi M, Wang W, Taylor BS, et al. The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci U S A 2010;107:14903-8.
12. Poulikakos PI, Zhang C, Bollag G, Shokat KM, Rosen N. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 2010;464:427-30.
13. Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, et al. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 2010;464:431-5.
14. Heidorn SJ, Milagre C, Whittaker S, Nourry A, Niculescu-Duvas I, Dhomen N, et al. Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF. Cell 2010;140:209-21.
15. Robert C, Arnault JP, Mateus C. RAF inhibition and induction of cutaneous squamous cell carcinoma. Curr Opin Oncol 2011;23:177-82.
16. Tsai J, Lee JT, Wang W, Zhang J, Cho H, Mamo S, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A 2008;105:3041-6. (Pubitemid 351723664)
17. Yang H, Higgins B, Kolinsky K, Packman K, Go Z, Iyer R, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res 2010;70:5518-27.
18. Flaherty KT, Puzanov I, Kim KB, Ribas A, McArthur GA, Sosman JA, et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med 2010;363:809-19.
19. Ribas A, Kim KB, Schuchter LM, Gonzalez R, Pavlick AC, Weber JS, et al. BRIM-2: An open-label, multicenter phase II study of vemurafenib in previously treated patients with BRAF V600E mutation-positive metastatic melanoma. J Clin Oncol 2011;29:8509.
20. Chapman PB, Hauschild A, Robert C, Haanen JB, Ascierto P, Larkin J, et al. BRIM-3 Study Group. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 2011;364:2507-16.
21. Wolchok JD, Hoos A, O'Day S, Weber JS, Hamid O, Lebbe C, et al. Guidelines for the evaluation of immune therapy activity in solid tumors: immune-related response criteria. Clin Cancer Res 2009;15:7412-20.
22. Robert C, Thomas L, Bondarenko I, O'Day S, M D JW, Garbe C, et al. Ipilimumab plus dacarbazine for previously untreated metastatic melanoma. N Engl J Med 2011;364:2517-26.
23. Boni A, Cogdill AP, Dang P, Udayakumar D, Njauw CN, Sloss CM, et al. Selective BRAFV600E inhibition enhances T-cell recognition of melanoma without affecting lymphocyte function. Cancer Res 2010;70:5213-9.
24. Roche Molecular Systems, Inc.; Branchburg (NJ). cobas® 4800 BRAF V600 Mutation Test. Doc Rev 1.0. 2011 [cited 09/04/2011]. Available from: http://1roche.mylabonline.com/rs/roche/images/BRAF-USIVDpackage-insert.pdf
25. Long GV, Menzies AM, Nagrial AM, Haydu LE, Hamilton AL, Mann GJ, et al. Prognostic and clinicopathologic associations of oncogenic BRAF in metastatic melanoma. J Clin Oncol 2011;29:1239-46.
26. Menzies AM, Visintin L, Chatfield MD, Carlino MS, Howle JR, Scolyer RA, et al. BRAF mutation by age-decade and body mass index in metastatic melanoma. J Clin Oncol 2011;29:8507.
27. Nazarian R, Shi H, Wang Q, Kong X, Koya RC, Lee H, et al. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 2010;468:973-7.
28. Johannessen CM, Boehm JS, Kim SY, Thomas SR, Wardwell L, Johnson LA, et al. COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 2010;468:968-72.
29. Wagle N, Emery C, Berger MF, Davis MJ, Sawyer A, Pochanard P, et al. Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J Clin Oncol 2011;29:3085-96.