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Targeted Therapy for Melanoma

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Melanoma

Part of the book series: Cancer Treatment and Research ((CTAR,volume 167))

Abstract

Vemurafenib and dabrafenib, two potent tyrosine kinase inhibitors (TKIs) of the BRAFV600E kinase, are highly effective in the treatment of a BRAF V600-mutant metastatic melanoma. These are selective type I inhibitors (functional against the active conformation of the kinase) of the RAF kinases, which are key players in the mitogen-activated protein kinase (MAPK) pathway. BRAF V600 mutations are present in approximately 7 % of all cancers, including high frequencies of mutations reported in 50 % of advanced melanomas and 100 % of hairy cell leukemias. As with most targeted therapies, resistance to BRAF inhibitors is an issue, and mechanisms of resistance are varied. Combining BRAF inhibitors with MEK inhibitors such as trametinib delays the development of resistance. Rationally combining targeted therapies to address the mechanism of resistance or combining BRAF inhibitors with other effective therapies such as immunotherapy may result in further improvement in outcomes for patients.

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Author Disclosures

Deborah Wong has no conflict of interests to declare.

Antoni Ribas has served as consultant for Amgen, Genentech-Roche, GSK, Merck, and Novartis with the honoraria paid to UCLA.

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Authors and Affiliations

  1. Department of Medicine, Division of Hematology/Oncology, University of California Los Angeles (UCLA), Le Conte Avenue, Los Angeles, CA, 10833, USA

    Deborah J. L. Wong & Antoni Ribas

  2. Jonsson Comprehensive Cancer Center, UCLA, Los Angeles, CA, USA

    Antoni Ribas

Authors
  1. Deborah J. L. Wong
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  2. Antoni Ribas
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Correspondence to Antoni Ribas .

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Editors and Affiliations

  1. Rutgers Cancer Institute of New Jersey, New Brunswick, New York, USA

    Howard L. Kaufman

  2. Robert Wood Johnson Medical School, Rutgers Cancer Institute of New Jersey, New Brunswick, New Jersey, USA

    Janice M. Mehnert

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© 2016 Springer International Publishing Switzerland

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Wong, D.J.L., Ribas, A. (2016). Targeted Therapy for Melanoma. In: Kaufman, H., Mehnert, J. (eds) Melanoma. Cancer Treatment and Research, vol 167. Springer, Cham. https://doi.org/10.1007/978-3-319-22539-5_10

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  • DOI: https://doi.org/10.1007/978-3-319-22539-5_10

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-319-22538-8

  • Online ISBN: 978-3-319-22539-5

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