Author Manuscript Published OnlineFirst on May 4, 2017; DOI: 10.1158/1078-0432.CCR-16-2561 Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. ORIGINAL RESEARCH Elacestrant (RAD1901), a selective estrogen receptor degrader (SERD), has anti- tumor activity in multiple ER+ breast cancer patient-derived xenograft models Teeru Bihani1, Hitisha K. Patel1, Heike Arlt1, Nianjun Tao1, Hai Jiang1, Jeffrey L. Brown1, Dinesh M. Purandare1, Gary Hattersley1, and Fiona Garner1* 1Radius Health, Inc, Waltham, MA, USA Running Title: Elacestrant inhibits growth of ER+ breast cancer PDX models Key words: elacestrant, SERD, ESR1 mutations, CDK4/6, breast cancer, hormone signaling and inhibitors, preclinical studies of endocrine-related cancers, steroid hormones and receptors, xenograft models, novel antitumor agents. ABBREVIATIONS 17β-estradiol – E2 aromatase inhibitor – AI AUC – area under the curve estrogen receptor-alpha gene – ESR1 estrogen receptor – ER gene regulated by estrogen in breast cancer 1 – GREB1 human epidermal growth factor 2 - Her2 immunohistochemical, immunohistochemistry - IHC patient-derived xenograft – PDX progesterone receptor – PGR, PR 1 Downloaded from clincancerres.aacrjournals.org on September 27, 2021. © 2017 American Association for Cancer Research. Author Manuscript Published OnlineFirst on May 4, 2017; DOI: 10.1158/1078-0432.CCR-16-2561 Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. quantitative reverse transcriptase polymerase chain reaction – RT-qPCR selective estrogen receptor degrader – SERD selective estrogen receptor modulator – SERM trefoil factor 1 – TFF1 percent tumor growth inhibition - %TGI Competing Interest and Financial Disclosures: All authors are employees of Radius Health, Inc. *Corresponding Author: Fiona Garner; Radius Health, 950 Winter Street, Waltham, MA, Phone: 617-551-4000, Fax: 617-551-4701,
[email protected] 2 Downloaded from clincancerres.aacrjournals.org on September 27, 2021.