The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models

(2016) H. M. Weir et al.   CANCER RESEARCH

PlasmaESR1Mutations and the Treatment of Estrogen Receptor–Positive Advanced Breast Cancer

(2016) Charlotte Fribbens et al.   JOURNAL OF CLINICAL ONCOLOGY

18F-Fluoroestradiol PET: Current Status and Potential Future Clinical Applications

(2016) G. J. Liao et al.   JOURNAL OF NUCLEAR MEDICINE

Heterogeneity and clinical significance of ESR1 mutations in ER-positive metastatic breast cancer patients receiving fulvestrant

(2016) Jill M. Spoerke et al.   Nature Communications

Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation

(2016) Sean W Fanning et al.   eLife

Efficacy of SERD/SERM Hybrid-CDK4/6 Inhibitor Combinations in Models of Endocrine Therapy-Resistant Breast Cancer

(2015) S. E. Wardell et al.   CLINICAL CANCER RESEARCH

Fulvestrant 500 mg Versus Anastrozole 1 mg for the First-Line Treatment of Advanced Breast Cancer: Overall Survival Analysis From the Phase II FIRST Study

(2015) Matthew J. Ellis et al.   JOURNAL OF CLINICAL ONCOLOGY

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

(2015) Andiliy Lai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Analysis of ESR1 mutation in circulating tumor DNA demonstrates evolution during therapy for metastatic breast cancer

(2015) Gaia Schiavon et al.   Science Translational Medicine

Emergence of Constitutively Active Estrogen Receptor-  Mutations in Pretreated Advanced Estrogen Receptor-Positive Breast Cancer

(2014) R. Jeselsohn et al.   CLINICAL CANCER RESEARCH

Measuring Residual Estrogen Receptor Availability during Fulvestrant Therapy in Patients with Metastatic Breast Cancer

(2014) Michel van Kruchten et al.   Cancer Discovery

Annual Report to the Nation on the status of cancer, 1975-2010, featuring prevalence of comorbidity and impact on survival among persons with lung, colorectal, breast, or prostate cancer

(2013) Brenda K. Edwards et al.   CANCER

D538G Mutation in Estrogen Receptor- : A Novel Mechanism for Acquired Endocrine Resistance in Breast Cancer

(2013) K. Merenbakh-Lamin et al.   CANCER RESEARCH

Bazedoxifene Exhibits Antiestrogenic Activity in Animal Models of Tamoxifen-Resistant Breast Cancer: Implications for Treatment of Advanced Disease

(2013) S. E. Wardell et al.   CLINICAL CANCER RESEARCH

Relevance of breast cancer hormone receptors and other factors to the efficacy of adjuvant tamoxifen: patient-level meta-analysis of randomised trials

(2013)   LANCET

ESR1 ligand-binding domain mutations in hormone-resistant breast cancer

(2013) Weiyi Toy et al.   NATURE GENETICS

Activating ESR1 mutations in hormone-resistant metastatic breast cancer

(2013) Dan R Robinson et al.   NATURE GENETICS

Endocrine-Therapy-Resistant ESR1 Variants Revealed by Genomic Characterization of Breast-Cancer-Derived Xenografts

(2013) Shunqiang Li et al.   Cell Reports

Dose-dependent change in biomarkers during neoadjuvant endocrine therapy with fulvestrant: results from NEWEST, a randomized Phase II study

(2012) Irene Kuter et al.   BREAST CANCER RESEARCH AND TREATMENT

Hormonal therapy in breast cancer: A model disease for the personalization of cancer care

(2012) Shannon Puhalla et al.   Molecular Oncology

The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy

(2011) Suzanne E. Wardell et al.   BIOCHEMICAL PHARMACOLOGY

Fluoroestradiol Positron Emission Tomography Reveals Differences in Pharmacodynamics of Aromatase Inhibitors, Tamoxifen, and Fulvestrant in Patients with Metastatic Breast Cancer

(2011) H. M. Linden et al.   CLINICAL CANCER RESEARCH

Tumor grafts derived from women with breast cancer authentically reflect tumor pathology, growth, metastasis and disease outcomes

(2011) Yoko S DeRose et al.   NATURE MEDICINE

Three dose regimens of fulvestrant in postmenopausal Japanese women with advanced breast cancer: results from a double-blind, phase II comparative study (FINDER1)

(2010) S. Ohno et al.   ANNALS OF ONCOLOGY

Results of a phase II study comparing three dosing regimens of fulvestrant in postmenopausal women with advanced breast cancer (FINDER2)

(2010) Kathleen I. Pritchard et al.   BREAST CANCER RESEARCH AND TREATMENT

The molecular mechanisms underlying the pharmacological actions of ER modulators: implications for new drug discovery in breast cancer

(2010) Donald P McDonnell et al.   CURRENT OPINION IN PHARMACOLOGY

Results of the CONFIRM Phase III Trial Comparing Fulvestrant 250 mg With Fulvestrant 500 mg in Postmenopausal Women With Estrogen Receptor–Positive Advanced Breast Cancer

(2010) Angelo Di Leo et al.   JOURNAL OF CLINICAL ONCOLOGY

Meta-Analysis of Breast Cancer Outcomes in Adjuvant Trials of Aromatase Inhibitors Versus Tamoxifen

(2009) Mitch Dowsett et al.   JOURNAL OF CLINICAL ONCOLOGY

Letrozole Therapy Alone or in Sequence with Tamoxifen in Women with Breast Cancer

(2009)   NEW ENGLAND JOURNAL OF MEDICINE

Double-Blind, Randomized Placebo Controlled Trial of Fulvestrant Compared With Exemestane After Prior Nonsteroidal Aromatase Inhibitor Therapy in Postmenopausal Women With Hormone Receptor–Positive, Advanced Breast Cancer: Results From EFECT

(2008) Stephen Chia et al.   JOURNAL OF CLINICAL ONCOLOGY

Estrogen Receptor-α Hinge-Region Lysines 302 and 303 Regulate Receptor Degradation by the Proteasome

(2008) Nicholas B. Berry et al.   MOLECULAR ENDOCRINOLOGY

NFκB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses

(2008) Kendall W Nettles et al.   Nature Chemical Biology