GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer

Author:

Liang Jun1ORCID,Zbieg Jason R.1ORCID,Blake Robert A.1,Chang Jae H.1ORCID,Daly Stephen2,DiPasquale Antonio G.1,Friedman Lori S.1,Gelzleichter Thomas1,Gill Matthew2,Giltnane Jennifer M.1,Goodacre Simon2,Guan Jane1,Hartman Steven J.1,Ingalla Ellen Rei1,Kategaya Lorn1,Kiefer James R.1,Kleinheinz Tracy1,Labadie Sharada S.1,Lai Tommy3,Li Jun1,Liao Jiangpeng3,Liu Zhiguo3,Mody Vidhi1,McLean Neville2,Metcalfe Ciara1ORCID,Nannini Michelle A.1,Oeh Jason1,O’Rourke Martin G.2,Ortwine Daniel F.1,Ran Yingqing1,Ray Nicholas C.2,Roussel Fabien2,Sambrone Amy1,Sampath Deepak1,Schutt Leah K.1,Vinogradova Maia1,Wai John3,Wang Tao3,Wertz Ingrid E.1,White Jonathan R.2,Yeap Siew Kuen2,Young Amy1,Zhang Birong1,Zheng Xiaoping3,Zhou Wei1,Zhong Yu1,Wang Xiaojing1

Affiliation:

1. Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

2. Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom

3. WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, P. R. China

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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