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Molecular Cancer Therapeutics
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Small Molecule Therapeutics

FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer

Andreas Weiss, Flavia Adler, Alexandra Buhles, Christelle Stamm, Robin A. Fairhurst, Michael Kiffe, Dario Sterker, Mario Centeleghe, Markus Wartmann, Jacqueline Kinyamu-Akunda, Heiko S. Schadt, Philippe Couttet, Armin Wolf, Youzhen Wang, Patrizia Barzaghi-Rinaudo, Masato Murakami, Audrey Kauffmann, Thomas Knoepfel, Nicole Buschmann, Catherine Leblanc, Robert Mah, Pascal Furet, Jutta Blank, Francesco Hofmann, William R. Sellers and Diana Graus Porta
Andreas Weiss
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Flavia Adler
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Alexandra Buhles
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Christelle Stamm
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Robin A. Fairhurst
2Novartis Institutes for Biomedical Research, Global Discovery Chemistry, Basel, Switzerland.
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  • ORCID record for Robin A. Fairhurst
Michael Kiffe
3Novartis Institutes for Biomedical Research, PK Sciences, Basel, Switzerland.
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Dario Sterker
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Mario Centeleghe
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Markus Wartmann
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Jacqueline Kinyamu-Akunda
4Novartis Institutes for Biomedical Research, Preclinical Safety, East Hanover New Jersey.
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Heiko S. Schadt
5Novartis Institutes for Biomedical Research, Preclinical Safety, Basel, Switzerland.
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Philippe Couttet
5Novartis Institutes for Biomedical Research, Preclinical Safety, Basel, Switzerland.
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Armin Wolf
5Novartis Institutes for Biomedical Research, Preclinical Safety, Basel, Switzerland.
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Youzhen Wang
6Novartis Institutes for Biomedical Research, Oncology Disease Area, Cambridge, Massachusetts.
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Patrizia Barzaghi-Rinaudo
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Masato Murakami
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Audrey Kauffmann
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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Thomas Knoepfel
2Novartis Institutes for Biomedical Research, Global Discovery Chemistry, Basel, Switzerland.
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Nicole Buschmann
2Novartis Institutes for Biomedical Research, Global Discovery Chemistry, Basel, Switzerland.
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Catherine Leblanc
2Novartis Institutes for Biomedical Research, Global Discovery Chemistry, Basel, Switzerland.
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Robert Mah
2Novartis Institutes for Biomedical Research, Global Discovery Chemistry, Basel, Switzerland.
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Pascal Furet
2Novartis Institutes for Biomedical Research, Global Discovery Chemistry, Basel, Switzerland.
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Jutta Blank
7Novartis Institutes for Biomedical Research, Chemical Biology and Therapeutics, Basel, Switzerland.
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Francesco Hofmann
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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William R. Sellers
6Novartis Institutes for Biomedical Research, Oncology Disease Area, Cambridge, Massachusetts.
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Diana Graus Porta
1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
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  • For correspondence: diana.graus_porta@novartis.com
DOI: 10.1158/1535-7163.MCT-18-1291 Published December 2019
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ARTICLE USAGE: August 2019 to January 2021

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Total60868971806

Cited By

Article Information

Volume 18, Issue 12, pp. 2194-2206

DOI 
https://doi.org/10.1158/1535-7163.MCT-18-1291
PubMed 
31409633

Published By 
American Association for Cancer Research
Print ISSN 
1535-7163
Online ISSN 
1538-8514
History 
  • Received December 16, 2018
  • Revision received June 12, 2019
  • Accepted August 6, 2019
  • Published first August 13, 2019.

Article Versions

  • Previous version (August 13, 2019 - 07:19).
  • You are viewing the most recent version of this article.
Copyright & Usage 
©2019 American Association for Cancer Research.

Author Information

  1. Andreas Weiss1,
  2. Flavia Adler1,
  3. Alexandra Buhles1,
  4. Christelle Stamm1,
  5. Robin A. Fairhurst2,
  6. Michael Kiffe3,
  7. Dario Sterker1,
  8. Mario Centeleghe1,
  9. Markus Wartmann1,
  10. Jacqueline Kinyamu-Akunda4,
  11. Heiko S. Schadt5,
  12. Philippe Couttet5,
  13. Armin Wolf5,
  14. Youzhen Wang6,
  15. Patrizia Barzaghi-Rinaudo1,
  16. Masato Murakami1,
  17. Audrey Kauffmann1,
  18. Thomas Knoepfel2,
  19. Nicole Buschmann2,
  20. Catherine Leblanc2,
  21. Robert Mah2,
  22. Pascal Furet2,
  23. Jutta Blank7,
  24. Francesco Hofmann1,
  25. William R. Sellers6, and
  26. Diana Graus Porta1,*
  1. 1Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.
  2. 2Novartis Institutes for Biomedical Research, Global Discovery Chemistry, Basel, Switzerland.
  3. 3Novartis Institutes for Biomedical Research, PK Sciences, Basel, Switzerland.
  4. 4Novartis Institutes for Biomedical Research, Preclinical Safety, East Hanover New Jersey.
  5. 5Novartis Institutes for Biomedical Research, Preclinical Safety, Basel, Switzerland.
  6. 6Novartis Institutes for Biomedical Research, Oncology Disease Area, Cambridge, Massachusetts.
  7. 7Novartis Institutes for Biomedical Research, Chemical Biology and Therapeutics, Basel, Switzerland.
  1. ↵*Corresponding Author:
    Diana Graus Porta, Novartis Institutes for BioMedical Research, Klybeckstrasse 141, Basel 4002, Switzerland. Phone: +41-61-6965093; Fax: +41-61-6966242; E-mail: diana.graus_porta{at}novartis.com
  • Current address for A. Wolf: InSphero, CSO, Schlieren, Switzerland; current address for M. Murakami, Daiichi Sankyo Co., Ltd, Tokyo, Japan; and current address for W.R. Sellers, Broad Institute, Cambridge, Massachusetts.

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Molecular Cancer Therapeutics: 18 (12)
December 2019
Volume 18, Issue 12
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FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer
Andreas Weiss, Flavia Adler, Alexandra Buhles, Christelle Stamm, Robin A. Fairhurst, Michael Kiffe, Dario Sterker, Mario Centeleghe, Markus Wartmann, Jacqueline Kinyamu-Akunda, Heiko S. Schadt, Philippe Couttet, Armin Wolf, Youzhen Wang, Patrizia Barzaghi-Rinaudo, Masato Murakami, Audrey Kauffmann, Thomas Knoepfel, Nicole Buschmann, Catherine Leblanc, Robert Mah, Pascal Furet, Jutta Blank, Francesco Hofmann, William R. Sellers and Diana Graus Porta
Mol Cancer Ther December 1 2019 (18) (12) 2194-2206; DOI: 10.1158/1535-7163.MCT-18-1291

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FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer
Andreas Weiss, Flavia Adler, Alexandra Buhles, Christelle Stamm, Robin A. Fairhurst, Michael Kiffe, Dario Sterker, Mario Centeleghe, Markus Wartmann, Jacqueline Kinyamu-Akunda, Heiko S. Schadt, Philippe Couttet, Armin Wolf, Youzhen Wang, Patrizia Barzaghi-Rinaudo, Masato Murakami, Audrey Kauffmann, Thomas Knoepfel, Nicole Buschmann, Catherine Leblanc, Robert Mah, Pascal Furet, Jutta Blank, Francesco Hofmann, William R. Sellers and Diana Graus Porta
Mol Cancer Ther December 1 2019 (18) (12) 2194-2206; DOI: 10.1158/1535-7163.MCT-18-1291
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