Abstract
Oral vemurafenib (Zelboraf®) is a first-in-class, small molecule BRAFV600E inhibitor indicated for the treatment of unresectable or metastatic melanoma in BRAF V600 mutation-positive patients (EU) or BRAF V600E mutation-positive patients (USA). Compared with intravenous dacarbazine, vemurafenib significantly improved overall survival and progression-free survival in patients with unresectable, previously untreated, BRAF V600E mutation-positive, stage IIIC or IV melanoma. Oral vemurafenib was generally well tolerated, with cutaneous adverse events among the most commonly occurring adverse events.
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References
Lemech C, Arkenau H-T. Novel treatments for metastatic cutaneous melanoma and the management of emergent toxicities. Clin Med Insights Oncol. 2012;6:53–66.
National Comprehensive Cancer Network (NCCN). Clinical practice guidelines in oncology (NCCN guidelines®): melanoma. Version 1.2013. Fort Washington: National Comprehensive Cancer Network; 2012.
Keating GM. Vemurafenib in unresectable or metastatic melanoma. Biodrugs. 2012;26(5):325–34.
Zelboraf (vemurafenib) 240 mg film-coated tablets: EU summary of product characteristics. London: European Medicines Agency; 2012.
Zelboraf® (vemurafenib) tablet, oral: US prescribing information. San Francisco: Genentech USA, Inc.; 2011.
Chapman PB, Hauschild A, Robert C, et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med. 2011;364(26):2507–16.
McArthur G, Hauschild A, Robert C, et al. Vemurafenib improves overall survival compared to dacarbazine in advanced BRAFV600E-mutated melanoma: updated survival results from a phase III randomized, open-label, multicentre trial [abstract]. Stockholm: European Multidisciplinary Cancer Congress; 2011.
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 BRAFV600E-mutated melanoma [abstract no. 8502 plus oral presentation]. 48th Annual Meeting of the American Society of Clinical Oncology. Chicago (IL); 2012.
Sosman JA, Kim KB, Schuchter L, et al. Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med. 2012;366(8):707–14.
Schucter LM, Flaherty LE, Hamid O, et al. A single-arm, open-label, U.S. expanded access study of vemurafenib in patients with metastatic melanoma [abstract no. 8567]. 48th Annual Meeting of the American Society of Clinical Oncology. Chicago (IL); 2012.
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(18):1694–703.
Larkin JMG, Queirolo P, Arance AM, et al. An open-label, multicenter safety study of vemurafenib (PLX4032, RO5185426) in patients with metastatic melanoma [abstract no. 8517]. 48th Annual Meeting of the American Society of Clinical Oncology. Chicago (IL); 2012.
Manousaridis I, Mavridou S, Goerdt S, et al. Cutaneous side effects of inhibitors of the RAS/RAF/MEK/ERK signalling pathway and their management. J Eur Acad Dermatol Venereol. 2012. doi:10.1111/j.1468-3083.2012.04546.x. (Epub ahead of print).
Dummer R, Rinderknecht J, Goldinger SM, et al. An open-label pilot study of vemurafenib in previously treated metastatic melanoma patients with brain metastases [abstract no. 8548]. 47th Annual Meeting of the American Society of Clinical Oncology. Chicago (IL); 2012.
Disclosure
This article was adapted from BioDrugs 2012;26(5);325–34 [3]. The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on the articles. Changes results from comments received were made by the authors on the basis of scientific and editorial merit.
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The manuscript was reviewed by: K.S.M. Smalley, The Moffitt Cancer Center, Programs of Molecular Oncology and Cutaneous Oncology, Tampa, FL, USA.
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Keating, G.M., Lyseng-Williamson, K.A. Vemurafenib. Am J Clin Dermatol 14, 65–69 (2013). https://doi.org/10.1007/s40257-012-0007-3
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DOI: https://doi.org/10.1007/s40257-012-0007-3