Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer

Author:

Tria George S.1ORCID,Abrams Tinya1,Baird Jason1,Burks Heather E.1ORCID,Firestone Brant1,Gaither L. Alex1,Hamann Lawrence G.1,He Guo1,Kirby Christina A.1,Kim Sunkyu1,Lombardo Franco1,Macchi Kaitlin J.1,McDonnell Donald P.2,Mishina Yuji1,Norris John D.2,Nunez Jill1,Springer Clayton1,Sun Yingchuan1,Thomsen Noel M.1,Wang Chunrong1,Wang Jianling1,Yu Bing1,Tiong-Yip Choi-Lai1,Peukert Stefan1

Affiliation:

1. Novartis Institutes for BioMedical Research, Inc., 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States

2. Department of Pharmacology and Cancer Biology, Duke University School of Medicine, Durham, North Carolina 27710, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference35 articles.

1. Breast Cancer Facts & Figures 2015–2016; American Cancer Society, Inc: Atlanta, 2015.

2. Prognostic effect of estrogen receptor status across age in primary breast cancer

3. Oestrogen-related receptors in breast cancer: control of cellular metabolism and beyond

4. Contrasting Endocrine Activities of cis and trans Isomers in a Series of Substituted Triphenylethylenes

5. Edwards, P. N.; Large, M. S. Preparation and Formulation of (Substituted Aralkyl) Heterocyclic Compounds as Aromatase Inhibitors. Eur. Pat. Appl. EP 0296749 B1, 1988.

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