Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts

  • Andiliy Lai
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Mehmet Kahraman
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Steven Govek
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Johnny Nagasawa
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Celine Bonnefous
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Jackie Julien
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Karensa Douglas
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • John Sensintaffar
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Nhin Lu
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Kyoung-jin Lee
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Anna Aparicio
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Josh Kaufman
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Jing Qian
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Gang Shao
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Rene Prudente
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Michael J. Moon
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • James D. Joseph
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Beatrice Darimont
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Daniel Brigham
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Kate Grillot
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Richard Heyman
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Peter J. Rix
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Jeffrey H. Hager
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States
  • Nicholas D. Smith
    Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States

書誌事項

公開日
2015-05-22
DOI
  • 10.1021/acs.jmedchem.5b00054
公開者
American Chemical Society (ACS)

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