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Dabrafenib

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Small Molecules in Oncology

Part of the book series: Recent Results in Cancer Research ((RECENTCANCER,volume 201))

Abstract

Dabrafenib was developed as a highly specific reversible inhibitor of V600-mutant BRAF kinase, an oncogenic mutation driving proliferation in many different types of aggressive tumors. Metastatic melanoma has a high prevalence of V600-mutant BRAF, and clinical trials showed that dabrafenib improved response rates and median progression-free survival in patients with V600E BRAF mutations, including those with brain metastasis. Preliminary results suggest that dabrafenib may also have some role in non-melanoma V600-mutant solid tumors; however, more studies are needed. With a well-tolerated toxicity profile and few drug interactions, dabrafenib is effective as a monotherapy; however, resistance eventually develops in most patients after persistent exposure to the drug. Current research focuses on combination strategies with dabrafenib to not only improve response rates but also overcome resistance.

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Authors and Affiliations

  1. Department of Internal Medicine, Baylor College of Medicine, Houston, TX, USA

    Radhika Kainthla

  2. Department of Melanoma Medical Oncology, The University of Texas MD Anderson Cancer Center, Houston, TX, USA

    Kevin B. Kim

  3. Department of Investigational Cancer Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX, USA

    Gerald S. Falchook

Authors
  1. Radhika Kainthla
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  2. Kevin B. Kim
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  3. Gerald S. Falchook
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Corresponding author

Correspondence to Radhika Kainthla .

Editor information

Editors and Affiliations

  1. Cancer Center Heilbronn-Franken, SLK-Kliniken Heilbronn GmbH Medizinische Klinik III, Heilbronn, Germany

    Uwe M. Martens

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© 2014 Springer-Verlag Berlin Heidelberg

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Kainthla, R., Kim, K.B., Falchook, G.S. (2014). Dabrafenib. In: Martens, U. (eds) Small Molecules in Oncology. Recent Results in Cancer Research, vol 201. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-54490-3_14

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  • DOI: https://doi.org/10.1007/978-3-642-54490-3_14

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  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-54489-7

  • Online ISBN: 978-3-642-54490-3

  • eBook Packages: MedicineMedicine (R0)

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