Overcoming Endocrine Resistance in Breast Cancer

Hanker, Ariella B.; Sudhan, Dhivya R.; Arteaga, Carlos L.

doi:10.1016/j.ccell.2020.03.009

Cited by 927Estrogen and related hormone effectsAdvanced Breast Cancer TherapiesBreast Cancer Treatment Studies

Overcoming Endocrine Resistance in Breast Cancer

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Hanker, Ariella B., Sudhan, Dhivya R., Arteaga, Carlos L.·2020·Cancer Cell

DOI 10.1016/j.ccell.2020.03.009PMC PMC7169993

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Abstract

Estrogen receptor-positive (ER+) breast cancer is the most common breast cancer subtype. Treatment of ER+ breast cancer comprises interventions that suppress estrogen production and/or target the ER directly (overall labeled as endocrine therapy). While endocrine therapy has considerably reduced recurrence and mortality from breast cancer, de novo and acquired resistance to this treatment remains a major challenge. An increasing number of mechanisms of endocrine resistance have been reported, including somatic alterations, epigenetic changes, and changes in the tumor microenvironment. Here, we review recent advances in delineating mechanisms of resistance to endocrine therapies and potential strategies to overcome such resistance.

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An increasing number of endocrine-resistance mechanisms have been characterized, and several small molecules have been reported to overcome Tamoxifen resistance.
“An increasing number of endocrine-resistance mechanisms have been characterized, and several small molecules have been reported to overcome Tamoxifen resistance58,59.”
From Harnessing artificial intelligence to identify Bufalin as a molecular glue degrader of estrogen receptor alpha (2025) · cites this paper as [59]
The Introduction describes recent discoveries of endocrine-resistance mechanisms. The ‘Aberrant co-factor activity’ section says tamoxifen-resistant cells may remain sensitive to selective estrogen receptor degraders, but it does not report that several small molecules have overcome tamoxifen resistance specifically. (LLM, conf=0.84)
Experimental — accuracy not yet measured
Tamoxifen resistance remains a major challenge in treating estrogen receptor-positive breast cancer.
“Tamoxifen (TAM) resistance remains a significant challenge in treating estrogen receptor (ER)-positive breast cancer.”
From Multifunctional and dual-targeting polymeric prodrug nanomicelles against tamoxifen-resistant breast cancer (2026) · cites this paper as [9]
Fulvestrant is a standard therapeutic option for endocrine-resistant or advanced metastatic ER+ breast cancer.
“Fulvestrant is a standard therapeutic option for endocrine-resistant or advanced metastatic ER+ breast cancer59,60.”
From Harnessing artificial intelligence to identify Bufalin as a molecular glue degrader of estrogen receptor alpha (2025) · cites this paper as [59]

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Key regulators of lipid metabolism drive endocrine resistance in invasive lobular breast cancer
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FGFR4 overexpression and hotspot mutations in metastatic ER+ breast cancer are enriched in the lobular subtype
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Ligand-binding Domain–activating Mutations of ESR1 Rewire Cellular Metabolism of Breast Cancer Cells
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Abstract PD5-10: A first-in-human phase I study to evaluate the oral selective estrogen receptor degrader (SERD), GDC-0927, in postmenopausal women with estrogen receptor positive (ER+) HER2-negative metastatic breast cancer (BC)
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Abstract PD7-05: A first-in-human phase I study to evaluate the oral selective estrogen receptor degrader (SERD), GDC-9545, in postmenopausal women with estrogen receptor-positive (ER+) HER2-negative (HER2-) metastatic breast cancer
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Abstract 5641: Effects of G1T48, a novel orally bioavailable selective estrogen receptor degrader (SERD), and the CDK4/6 inhibitor, G1T38, on tumor growth in animal models of endocrine resistant breast cancer
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Dose-escalation study of G1T48, an oral selective estrogen receptor degrader (SERD), in postmenopausal women with ER+/HER2- locally advanced or metastatic breast cancer (ABC)
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Abstract PD7-07: Final analysis of phase 1 study of elacestrant (RAD1901), a novel selective estrogen receptor degrader (SERD), in estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer
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Abstract GS3-06: Results from the plasmaMATCH trial: A multiple parallel cohort, multi-centre clinical trial of circulating tumour DNA testing to direct targeted therapies in patients with advanced breast cancer (CRUK/15/010)
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Abstract P3-04-05: Identification of SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that has strong antitumor activity in wild-type and mutant ER+ breast cancer models
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Abstract P5-21-04: Phase I/Ib study of the SERD LSZ102 alone or in combination with ribociclib in ER+ breast cancer
Juric, D., Curigliano, G., Cresta, S., et al. (2018) · Cancer Research · doi:10.1158/1538-7445.sabcs17-p5-21-04 · Cited by 8 · see citing works
Abstract 5776: Pharmacologic and PK/PD study of D-0502: An orally bioavailable SERD with potent antitumor activity in ER-positive breast cancer cell lines and xenograft models
Wang, Y., Shi, Z., Jiang, Y., et al. (2018) · Cancer Research · doi:10.1158/1538-7445.am2018-5776 · Cited by 8 · see citing works
Abstract PR08: Preliminary results from a phase 2 trial of tipifarnib in squamous cell carcinomas (SCCs) with HRAS mutations
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Lasofoxifene as a potential treatment for ER+ metastatic breast cancer.
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Abstract PD1-08: Phase 1/1b study of novel oral selective estrogen receptor degrader (SERD) LSZ102 for estrogen receptor-positive (ER+) advanced breast cancer (ABC) with progression on endocrine therapy (ET)
Jhaveri, K., Curigliano, G., Yap, Y.-S., et al. (2019) · Cancer Research · doi:10.1158/1538-7445.sabcs18-pd1-08 · Cited by 3 · see citing works
Abstract GS6-06: A neoadjuvant trial with letrozole identifies PRR11 in the 17q23 amplicon as a mechanism of resistance to endocrine therapy in ER-positive breast cancer
Lee, K., Zotano, Á. G., Hanker, A. B., et al. (2020) · Cancer Research · doi:10.1158/1538-7445.sabcs19-gs6-06 · Cited by 2 · see citing works
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Authors: Hanker, A. B., Sudhan, D. R., & Arteaga, C. L.
Affiliations: Harold C. Simmons Comprehensive Cancer Center (US)
Corresponding author: Hanker, Ariella B.
Arteaga, Carlos L.
ORCID: Hanker, Ariella B.
Sudhan, Dhivya R.
Arteaga, Carlos L.
Venue: Cancer Cell
Publisher: Elsevier BV
Published: 2020-04
Volume: 37
Issue: 4
Pages: 496-513
ISSN: 1535-6108 (ISSN-L)
DOI: 10.1016/j.ccell.2020.03.009
PMC: PMC7169993
OpenAlex: W3015634062
Cited by: 927
References: 200
Citations by year: 2026: 123 · 2025: 191 · 2024: 213 · 2023: 171 · 2022: 135 · 2021: 70 · 2020: 21 · 2019: 1
FWCI: 14.28
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 377 d)
Locations: Cancer Cell (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Cancer Institute
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Advanced Breast Cancer Therapies
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
Keywords: breast cancer, endocrine therapy resistance, endocrine therapy, estrogen receptor, acquired resistance, de novo resistance, epigenetic modifications, tumor microenvironment, somatic alterations, resistance mechanisms, overcoming resistance
MeSH terms: Breast Neoplasms, Female, Humans, Receptors, Estrogen, Antineoplastic Agents, Hormonal, Drug Resistance, Neoplasm, Disease Management, Tumor Microenvironment

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Overcoming Endocrine Resistance in Breast Cancer

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