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Larotrectinib (LOXO-101)

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Book cover Small Molecules in Oncology

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

Abstract

One of the most challenging issues in oncology research and treatment is identifying oncogenic drivers within an individual patient’s tumor which can be directly targeted by a clinically available therapeutic drug. In this context, gene fusions as one important example of genetic aberrations leading to carcinogenesis follow the widely accepted concept that cell growth and proliferation are driven by the accomplished fusion (usually involving former proto-oncogenes) and may therefore be successfully inhibited by substances directed against the fusion. This concept has already been established with oncogenic gene fusions like BCR-ABL in chronic myelogenous leukemia (CML) or anaplastic lymphoma kinase (ALK) in lung cancer, including special tyrosine kinase inhibitors (TKIs) which are able to block the activation of the depending downstream proliferation pathways and, consequently, tumor growth. During the last decade, the NTRK1, 2, and 3 genes, encoding the TRKA, B, and C proteins, have attracted increasing attention as another significant and targetable gene fusion in a variety of cancers. Several TRK inhibitors have been developed, and one of them, Larotrectinib (formerly known as LOXO-101), represents an orally available, selective inhibitor of the TRK receptor family that has already shown substantial clinical benefit in both pediatric and adult patients harboring an NTRK gene fusion over the last few years.

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Authors and Affiliations

  1. Cancer Center Heilbronn-Franken, MOLIT Institute, SLK-Kliniken Heilbronn GmbH, Am Gesundbrunnen 20-26, 74078, Heilbronn, Germany

    Stephanie Berger, Uwe M. Martens & Sylvia Bochum

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  1. Stephanie Berger
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  2. Uwe M. Martens
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  3. Sylvia Bochum
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Correspondence to Stephanie Berger .

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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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Berger, S., Martens, U.M., Bochum, S. (2018). Larotrectinib (LOXO-101). 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_10

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  • DOI: https://doi.org/10.1007/978-3-319-91442-8_10

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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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