The therapeutic role of fulvestrant in the management of patients with hormone receptor-positive breast cancer

Ciruelos, Eva; Pascual, Tomás; Vozmediano, M.L. Arroyo; Blanco, Marta; Manso, Luís; Parrilla, Lucía; Muñoz, Carmen García; Vega, Estela; Calderón, Mónica; Sancho, B.; Cortés, Javier

doi:10.1016/j.breast.2014.01.016

Cited by 63 publications

(80 citation statements)

References 40 publications

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“…Estrogen dependent breast cancers express functional ERs and respond clinically to selective estrogen receptor modulators (SERMs) that act by inhibiting ER transactivational activity (28,30). Tumors from the prostate, colon, lung, and CNS, while not estrogen dependent, are also estrogen responsive; however, the role of ER␤ in tumor progression is not clear (29).…”

Section: Discussionmentioning

confidence: 98%

“…For ER-positive breast cancer, the selective estrogen receptor modulator (SERM) tamoxifen is used clinically as the first-line treatment to block ER activity and inhibit breast tumor growth. The ER antagonist fulvestrant (Faslodex) is also used as an adjuvant therapy for treating advanced or metastatic breast cancer (30). While it is known that ER␣ promotes growth of estrogen dependent cancers, results from studies investigating the role of ER␤ in estrogen responsive tumors from other tissues are less clear-cut, and the mechanisms underlying the reported differential effects of ER␤ remain unclear.…”

mentioning

confidence: 98%

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Estrogen Receptor-β Up-Regulates IGF1R Expression and Activity to Inhibit Apoptosis and Increase Growth of Medulloblastoma

Cookman

Belcher

2015

Endocrinology

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Medulloblastoma (Med) is the most common malignant brain tumor in children. The role of ESR2 [estrogen receptor (ER)-β] in promoting Med growth was comprehensively examined in three in vivo models and human cell lines. In a novel Med ERβ-null knockout model developed by crossing Esr2(-/-) mice with cerebellar granule cell precursor specific Ptch1 conditional knockout mice, the tumor growth rate was significantly decreased in males and females. The absence of Esr2 resulted in increased apoptosis, decreased B-cell lymphoma 2 (BCL2), and IGF-1 receptor (IGF1R) expression, and decreased levels of active MAPKs (ERK1/2) and protein kinase B (AKT). Treatment of Med in Ptch1(+/-) Trp53(-/-) mice with the antiestrogen chemotherapeutic drug Faslodex significantly increased symptom-free survival, which was associated with increased apoptosis and decreased BCL2 and IGF1R expression and signaling. Similar effects were also observed in nude mice bearing D283Med xenografts. In vitro studies in human D283Med cells metabolically stressed by glutamine withdrawal found that 17β-estradiol and the ERβ selective agonist 2,3-bis(4-hydroxyphenyl)-propionitrile dose dependently protected Med cells from caspase-3-dependent cell death. Those effects were associated with increased phosphorylation of IGF1R, long-term increases in ERK1/2 and AKT signaling, and increased expression of IGF-1, IGF1R, and BCL2. Results of pharmacological experiments revealed that the cytoprotective actions of estradiol were dependent on ERβ and IGF1R receptor tyrosine kinase activity and independent of ERα and G protein-coupled estrogen receptor 1 (G protein coupled receptor 30). The presented results demonstrate that estrogen promotes Med growth through ERβ-mediated increases in IGF1R expression and activity, which induce cytoprotective mechanisms that decrease apoptosis.

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Section: Discussionmentioning

confidence: 98%

mentioning

confidence: 98%

Estrogen Receptor-β Up-Regulates IGF1R Expression and Activity to Inhibit Apoptosis and Increase Growth of Medulloblastoma

Cookman

Belcher

2015

Endocrinology

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“…In the current study, fulvestrant and micronized progesterone antagonized all these pathways and contributed to the prevention of adhesion formation by creating a hypoestrogenic milieu. In addition, fulvestrant which is the first in a new class of anti-estrogens and SERDs, without any agonist activity exerts anti-proliferative activity and induction of apoptosis [39]. Micronized progesterone has also anti-proliferative and anti-inflammatory effects [40].…”

Section: Discussionmentioning

confidence: 99%

Evaluation of the effects of fulvestrant and micronized progesterone on the post-operative adhesion formation and ovarian reserve in rat model with immunohistochemical and biochemical analysis

Öner

Ulug

Demirci³

et al. 2015

Gynecological Endocrinology

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“…As previously described, Fulvestrant (Faslodex; ICI 182780) is an FDA approved drug for use in postmenopausal patients following failure of first-line endocrine therapies (such as tamoxifen or aromatase inhibitors) [91]. Despite the potent antiestrogen effects of this drug, most breast cancer cases eventually develop resistance to fulvestrant through poorly understood mechanisms [92,93].…”

Section: Micrornas In Endocrine Therapymentioning

confidence: 99%

miRNA clusters as therapeutic targets for hormone-resistant breast cancer

Leva

Cheung

Croce

2015

Expert Review of Endocrinology & Metabolism

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MicroRNAs are small non coding RNAs that typically inhibit the translation and stability of messenger RNAs, controlling genes involved in cellular processes such as inflammation, cell cycle regulation, stress response, differentiation, apoptosis, and migration. Not surprisingly, microRNAs are also aberrantly expressed in cancer and promote tumorigenesis by disrupting these vital cellular functions. In this review, we first broadly summarize the role of microRNAs in breast cancer and Estrogen Receptor alpha signaling. Then we focus on what is currently known about the role of microRNAs in anti-hormonal therapy or resistance to endocrine agents. Specifically, we will discuss key miRNAs involved in tamoxifen (miR-221/222, 181, 101, 519a, 301, 375, 342, 451, and the let-7 family), fulvestrant (miR-221/222, miR-200 family), and aromatase inhibitor (miR-128 and the let-7 family) resistance.

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The therapeutic role of fulvestrant in the management of patients with hormone receptor-positive breast cancer

Cited by 63 publications

References 40 publications

Estrogen Receptor-β Up-Regulates IGF1R Expression and Activity to Inhibit Apoptosis and Increase Growth of Medulloblastoma

Estrogen Receptor-β Up-Regulates IGF1R Expression and Activity to Inhibit Apoptosis and Increase Growth of Medulloblastoma

Evaluation of the effects of fulvestrant and micronized progesterone on the post-operative adhesion formation and ovarian reserve in rat model with immunohistochemical and biochemical analysis

miRNA clusters as therapeutic targets for hormone-resistant breast cancer

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