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Small Molecules in Oncology pp 91–100Cite as

Trametinib (GSK1120212)

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Part of the book series: Recent Results in Cancer Research ((RECENTCANCER,volume 211))

Abstract

The mitogen-activated protein kinase (MEK MAPK/ERK kinase) signaling pathways play a critical role in the regulation of diverse cellular activities, including survival, differentiation, proliferation, motility, and angiogenesis. Therefore, MEK inhibition was recognized as a promising target for antineoplastic therapy. Trametinib (GSK1120212), an oral MEK inhibitor which is selective for MEK1 and MEK2, has been approved by the FDA for the treatment of metastatic melanoma in a combination with a BRAF inhibitor. In this overview, preclinical and clinical data for trametinib are presented including mechanisms based on in vitro studies as well as findings from different clinical studies. The future clinical trial in different solid tumor entities will define the therapeutic role of this targeted therapy approach, possibly as a combination with other targeted therapies such as BRAF inhibitors.

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Authors and Affiliations

  1. Department of Hematology, Oncology and Stem Cell Transplantation, Medical Center - University of Freiburg, Faculty of Medicine, University of Freiburg, Hugstetterstr. 55, 79106, Freiburg, Germany

    Robert Zeiser & Hana Andrlová

  2. Department of Dermatology and Venereology, Medical Center - University of Freiburg, Faculty of Medicine, University of Freiburg, Hauptstr. 7, 79104, Freiburg, Germany

    Frank Meiss

Authors
  1. Robert Zeiser
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  2. Hana Andrlová
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  3. Frank Meiss
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Correspondence to Robert Zeiser .

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Editors and Affiliations

  1. MOLIT Institute, Cancer Center Heilbronn-Franken, SLK-Clinics, Heilbronn, Baden-Württemberg, Germany

    Uwe M. Martens

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Zeiser, R., Andrlová, H., Meiss, F. (2018). Trametinib (GSK1120212). In: Martens, U. (eds) Small Molecules in Oncology. Recent Results in Cancer Research, vol 211. Springer, Cham. https://doi.org/10.1007/978-3-319-91442-8_7

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  • DOI: https://doi.org/10.1007/978-3-319-91442-8_7

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-319-91441-1

  • Online ISBN: 978-3-319-91442-8

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