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Fulvestrant

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https://www.readbyqxmd.com/read/28915603/estrogen-promotes-tumor-metastasis-via-estrogen-receptor-beta-mediated-regulation-of-matrix-metalloproteinase-2-in-non-small-cell-lung-cancer
#1
Sheng Fan, Yongde Liao, Changyu Liu, Quanfu Huang, Huifang Liang, Bo Ai, Shegnling Fu, Sheng Zhou
In non-small cell lung cancer (NSCLC), estrogen significantly promotes NSCLC cell growth via estrogen receptor beta (ERβ). However, the effects by which ERβ contributes to metastasis in NSCLC have not been previously reported. This study aims at defining whether the stimulation of ERβ promotes NSCLC metastasis in vitro and in vivo. Here, Our results showed that estrogen and ERβ agonist enhanced aggressiveness of two lung cancer cell lines (A549 and H1793) and promoted murine lung metastasis formation. ER-inhibitor Fulvestrant treatment or ERβ-knockdown significantly suppressed the migration, invasion and nodule formation of NSCLC cells...
August 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28903361/fulvestrant-500-milligrams-as-endocrine-therapy-for-endocrine-sensitive-advanced-breast-cancer-patients-in-the-real-world-the-ful500-prospective-observational-trial
#2
Luca Moscetti, Maria Agnese Fabbri, Clara Natoli, Patrizia Vici, Teresa Gamucci, Isabella Sperduti, Laura Iezzi, Elena Iattoni, Laura Pizzuti, Carmine Roma, Angela Vaccaro, Giuliana D'Auria, Mariella Mauri, Lucia Mentuccia, Antonino Grassadonia, Maddalena Barba, Enzo Maria Ruggeri
The observational prospective trial herein presented aimed at evaluating the efficacy of fulvestrant 500 mg in the treatment of endocrine sensitive advanced breast cancer patients from the real world setting. The primary end point was clinical benefit rate (CBR). Secondary end points were overall survival (OS), progression free survival (PFS) and tolerability. One hundred sixty three patients were enrolled. At a median follow up of 20 months, the 61% of patients reached CBR, whose median duration was 10.8 months...
August 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28893547/17%C3%AE-estradiol-modulates-cell-proliferation-of-medullary-cords-during-ovarian-differentiation-of-the-lepidochelys-olivacea-sea-turtle
#3
Verónica Díaz-Hernández, Alma Vázquez-Gómez, Alejandro Marmolejo-Valencia, Luis Manuel Montaño, Horacio Merchant-Larios
In turtles undergoing temperature sex determination (TSD), bipotential gonads express Sox9 in medullary cords at both female- (FPT) and male-producing temperatures (MPT). Subsequently, when the sex fate of medullary cords becomes dimorphic, at FPT, Sox9 is downregulated, whereas at MPT, its expression is maintained. Medullary cords in the ovary turn into ovarian lacuna, whereas in the testis they differentiate as seminiferous cords. When embryos of Lepidochelys olivacea sea turtle are incubated at MPT and treated with estradiol, Sox9 expression persists in the medullary cords in the form of tiny ovotestis-like formations...
September 8, 2017: Developmental Biology
https://www.readbyqxmd.com/read/28885430/aggressive-angiomyxoma-of-the-vulva-and-bladder
#4
Mihae Song, Michelle Glasgow, Paari Murugan, Colleen Rivard
BACKGROUND: Aggressive angiomyxoma is a rare, locally infiltrative tumor, frequently occurring in female patients. Although wide local excision is considered standard therapy, radical surgery may be needed. CASE: A 49-year-old woman presented with an aggressive angiomyxoma involving the vulva and bladder. Given the hormone receptor status and size of the tumor, the patient was initially treated with fulvestrant and goserelin acetate in an attempt to reduce the size of the mass...
September 5, 2017: Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28882815/childhood-tolerance-of-severe-influenza-a-mortality-analysis-in-mice
#5
Freeman Suber, Lester Kobzik
During the 1918 influenza pandemic, children experienced substantially lower mortality than adults, a striking but unexplained finding. Whether this was due to enhanced resistance (reduced virus load) or better tolerance (reduced impact of infection) has not been defined. We found that prepubertal mice infected with H1N1 influenza virus also showed greater survival than infected pubertal mice, despite similar virus loads. Transcriptome profiling of infected lungs identified estrogen as a regulator of susceptibility in both sexes, and also linked better survival to late expression of IL-1beta...
September 7, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28877783/g-protein-coupled-estrogen-receptor-antagonist-g15-decreases-estrogen-induced-development-of-non-small-cell-lung-cancer
#6
Changyu Liu, Yongde Liao, Sheng Fan, Xiangning Fu, Jing Xiong, Sheng Zhou, Man Zou, Jianmiao Wang
G-protein-coupled estrogen receptor (GPER) was found to promote Non-small cell lung cancer (NSCLC) by estrogen, indicating the potential necessity of inhibiting GPER by selective antagonist. This study was performed to elucidate the function of GPER selective inhibitor G15 in NSCLC development. Cytoplasmic GPER (cGPER) and nuclear GPER (nGPER) were detected by immunohistochemical analysis in NSCLC samples. The relation of GPER and estrogen receptor β (ERβ) expression and correlation between GPER, ERβ and clinical factors were analyzed...
September 25, 2017: Oncology Research
https://www.readbyqxmd.com/read/28877739/estrogen-and-soy-isoflavonoids-decrease-sensitivity-of-medulloblastoma-and-central-nervous-system-primitive-neuroectodermal-tumor-cells-to-chemotherapeutic-cytotoxicity
#7
Scott M Belcher, Caleb C Burton, Clifford J Cookman, Michelle Kirby, Gabriel L Miranda, Fatima O Saeed, Kathleen E Wray
BACKGROUND: Our previous studies demonstrated that growth and migration of medulloblastoma (MB), the most common malignant brain tumor in children, are stimulated by 17β-estradiol. The growth stimulating effects of estrogens are mediated through ERβ and insulin-like growth factor 1 signaling to inhibit caspase 3 activity and reduce tumor cell apoptosis. The objective of this study was to determine whether estrogens decreased sensitivity of MB cells to cytotoxic actions of chemotherapeutic drugs...
September 6, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28862117/hormone-therapy-in-breast-cancer
#8
Mădălina Drăgănescu, Codruţa Carmocan
Hormonal therapy is mandatory for all patients with hormonereceptor- positive breast neoplasms. It is active both in adjuvant and metastatic disease. The only active adjuvant hormonal therapy in pre- and postmenopause is Tamoxifen. The adjuvant treatment duration influences disease-free survival, the risk of a contralateral breast cancer apparition and overall survival. The aromatase inhibitors: Anastrozol, Letrozol, Exemestan are only used in postmenopause. Fulvestrant is used in recurrent disease after or during treatment with Tamoxifen...
July 2017: Chirurgia
https://www.readbyqxmd.com/read/28860130/how-does-oestradiol-influence-the-avt-it-system-in-female-round-gobies-during-different-reproductive-phases
#9
Hanna Kalamarz-Kubiak, Magdalena Gozdowska, Tatiana Guellard, Ewa Kulczykowska
In this in vitro gradient perfusion study, we determined whether there is a functional relationship between oestradiol and the arginine vasotocin/isotocin (AVT/IT) system in the female round goby (Neogobius melanostomus). Brain explants were perfused in medium supplemented with 17β-oestradiol (E2) at doses mimicking the plasma levels of this hormone in nature during the spawning-capable phase and regressing phase. We aimed to establish which pathway, genomic or non-genomic, is involved in this mechanism in different reproductive phases...
August 31, 2017: Biology Open
https://www.readbyqxmd.com/read/28854070/first-in-human-phase-i-study-of-the-tamoxifen-metabolite-z-endoxifen-in-women-with-endocrine-refractory-metastatic-breast-cancer
#10
Matthew P Goetz, Vera J Suman, Joel M Reid, Don W Northfelt, Michael A Mahr, Andrew T Ralya, Mary Kuffel, Sarah A Buhrow, Stephanie L Safgren, Renee M McGovern, John Black, Travis Dockter, Tufia Haddad, Charles Erlichman, Alex A Adjei, Dan Visscher, Zachary R Chalmers, Garrett Frampton, Benjamin R Kipp, Minetta C Liu, John R Hawse, James H Doroshow, Jerry M Collins, Howard Streicher, Matthew M Ames, James N Ingle
Purpose Endoxifen is a tamoxifen metabolite with potent antiestrogenic activity. Patients and Methods We performed a phase I study of oral Z-endoxifen to determine its toxicities, maximum tolerated dose (MTD), pharmacokinetics, and clinical activity. Eligibility included endocrine-refractory, estrogen receptor-positive metastatic breast cancer. An accelerated titration schedule was applied until moderate or dose-limiting toxicity occurred, followed by a 3+3 design and expansion at 40, 80, and 100 mg per day...
August 30, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28841614/autologous-fat-grafting-as-a-novel-antiestrogen-vehicle-for-the-treatment-of-breast-cancer
#11
Scott Thomas, Stephanie Chen, Hani Sbitany, Edwin Kwon, Merisa Piper, Jeenah Park, Manuela Terranova Barberio, Nela Pawlowska, Pamela N Munster
BACKGROUND: Adipose fat transfer is increasingly used for contour corrections of the tumor bed after lumpectomy and breast reconstructions after mastectomy. The lipophilic nature of the fat tissue may render adipocytes an ideal vehicle with which to deliver a high boost of an antiestrogen to the tumor bed to serve as an adjunct systemic hormonal therapy. The authors therefore tested whether adipocytes could safely be loaded with an antiestrogen and allow for release at therapeutic concentrations to treat breast cancer...
September 2017: Plastic and Reconstructive Surgery
https://www.readbyqxmd.com/read/28839227/estrogen-receptor-%C3%AE-hdac-nfat-axis-for-delphinidin-effects-on-proliferation-and-differentiation-of-t-lymphocytes-from-patients-with-cardiovascular-risks
#12
Ousama Dayoub, Soazig Le Lay, Raffaella Soleti, Nicolas Clere, Gregory Hilairet, Séverine Dubois, Frédéric Gagnadoux, Jérôme Boursier, Maria Carmen Martínez, Ramaroson Andriantsitohaina
Delphinidin, an anthocyanin present in red wine, has been reported to preserve the integrity of endothelium via an estrogen receptor alpha (ERα)-dependent mechanism. However, the effect of delphinidin on the immune response in obesity-related inflammation remains unknown. Given the important role of T lymphocytes in obesity-related inflammation, we investigated the effect of delphinidin on proliferation and differentiation of T lymphocytes from healthy subjects and metabolic syndrome patients. Delphinidin decreased the proliferation stimulated by different agents acting through different mechanisms...
August 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28831437/paloma-3-phase-iii-trial-of-fulvestrant-with-or-without-palbociclib-in-premenopausal-and-postmenopausal-women-with-hormone-receptor-positive-human-epidermal-growth-factor-receptor-2-negative-metastatic-breast-cancer-that-progressed-on-prior-endocrine-therapy
#13
Hiroji Iwata, Seock-Ah Im, Norikazu Masuda, Young-Hyuck Im, Kenichi Inoue, Yoshiaki Rai, Rikiya Nakamura, Jee Hyun Kim, Justin T Hoffman, Ke Zhang, Carla Giorgetti, Shrividya Iyer, Patrick T Schnell, Cynthia Huang Bartlett, Jungsil Ro
PURPOSE: To assess efficacy and safety of palbociclib plus fulvestrant in Asians with endocrine therapy-resistant metastatic breast cancer. PATIENTS AND METHODS: The Palbociclib Ongoing Trials in the Management of Breast Cancer 3 (PALOMA-3) trial, a double-blind phase III study, included 521 patients with hormone receptor-positive/human epidermal growth factor receptor 2-negative metastatic breast cancer with disease progression on endocrine therapy. Patient-reported outcomes (PROs) were assessed on study treatment and at the end of treatment...
August 2017: Journal of Global Oncology
https://www.readbyqxmd.com/read/28816986/efficacy-and-safety-of-endocrine-monotherapy-as-first-line-treatment-for-hormone-sensitive-advanced-breast-cancer-a-network-meta-analysis
#14
Jingwen Zhang, Yanhong Huang, Changyi Wang, Yuanfang He, Shukai Zheng, Kusheng Wu
BACKGROUND: Endocrine therapy was recommended as the preferred first-line treatment for hormone receptor-positive (HR+, i.e., ER+ and/or PgR+), human epidermal growth factor receptor-2-negative (HER2-) postmenopausal advanced breast cancer (ABC), but which endocrine monotherapy is optimal lacks consensus. We aimed to identify the optimal endocrine monotherapy with a network meta-analysis. METHODS: We performed a network meta-analysis for a comprehensive analysis of 6 first-line endocrine monotherapies (letrozole, anastrozole, exemestane, tamoxifen, fulvestrant 250 mg and 500 mg) for HR+ HER2- metastatic or locally advanced breast cancer in postmenopausal patients...
August 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28811679/bisphenol-a-does-not-mimic-estrogen-in-the-promotion-of-the-in-vitro-response-of-murine-dendritic-cells-to-toll-like-receptor-ligands
#15
Marita Chakhtoura, Uma Sriram, Michelle Heayn, Joshua Wonsidler, Christopher Doyle, Joudy-Ann Dinnall, Stefania Gallucci, Rebecca A Roberts
Sex hormones affect immune responses and might promote autoimmunity. Endocrine disrupting chemicals such as bisphenol A (BPA) may mimic their immune effects. Conventional dendritic cells (cDCs) are pivotal initiators of immune responses upon activation by danger signals coming from pathogens or distressed tissues through triggering of the Toll-like receptors (TLRs). We generated in vitro murine cDCs in the absence of estrogens and measured the effects of exogenously added estrogen or BPA on their differentiation and activation by the TLR ligands LPS and CpG...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28775043/oestrogen-inhibition-reverses-pulmonary-arterial-hypertension-and-associated-metabolic-defects
#16
Xinping Chen, Eric D Austin, Megha Talati, Joshua P Fessel, Eric H Farber-Eger, Evan L Brittain, Anna R Hemnes, James E Loyd, James West
Increased oestrogen is a strong epidemiological risk factor for development of pulmonary arterial hypertension (PAH) in patients, associated with metabolic defects. In addition, oestrogens drive penetrance in mice carrying mutations in bone morphogenetic protein receptor type II (BMPR2), the cause of most heritable PAH. The goal of the present study was to determine whether inhibition of oestrogens was effective in the treatment of PAH in these mice.The oestrogen inhibitors fulvestrant and anastrozole were used in a prevention and treatment paradigm in BMPR2 mutant mice, and tamoxifen was used for treatment...
August 2017: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
https://www.readbyqxmd.com/read/28770167/fatal-statin-induced-rhabdomyolysis-by-possible-interaction-with-palbociclib
#17
Kellie Lynn Nelson, David Stenehjem, Meghan Driscoll, Glynn Weldon Gilcrease
A 60- to 65-year-old female on prior statin therapy was initiated on palbociclib and fulvestrant for the treatment of metastatic, hormone-receptor positive breast cancer. She subsequently developed sudden progressive muscle weakness that progressed to death within weeks. The patient noticed progressive proximal muscle weakness after two cycles of palbociclib, with no other medication changes in the interim. This rapidly progressed and resulted in death within 7 days of presentation to hospital. There has been one previous report of rhabdmyolysis with palbociclib, occurring in a patient on concomitant statin...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28763032/a-chip-for-estrogen-receptor-action-detection-of-biomarkers-released-by-mcf-7-cells-through-estrogenic-and-anti-estrogenic-effects
#18
Konstanze Gier, Claudia Preininger, Ursula Sauer
The fluorescence-based multi-analyte chip platform for the analysis of estrogenic and anti-estrogenic substances is a new in vitro tool for the high throughput screening of environmental samples. In contrast to existing tools, the chip investigates the complex action of xenoestrogens in a human cell model by characterizing protein expression. It allows for the quantification of 10 proteins secreted by MCF-7 cells, representing various biological and pathological endpoints of endocrine action and distinguishing between estrogen- and anti-estrogen-dependent secretion of proteins...
August 1, 2017: Sensors
https://www.readbyqxmd.com/read/28760601/a-functional-drug-re-purposing-screening-identifies-carfilzomib-as-a-drug-preventing-17%C3%AE-estradiol-er%C3%AE-signaling-and-cell-proliferation-in-breast-cancer-cells
#19
Claudia Busonero, Stefano Leone, Cinzia Klemm, Filippo Acconcia
Most cases of breast cancer (BC) are estrogen receptor α-positive (ERα+) at diagnosis. The presence of ERα drives the therapeutic approach for this disease, which often consists of endocrine therapy (ET). 4OH-Tamoxifen and faslodex (i.e., fulvestrant - ICI182,780) are two ETs that render tumor cells insensitive to 17β-estradiol (E2)-dependent proliferative stimuli and prevent BC progression. However, ET has limitations and serious failures in different tissues and organs. Thus, there is an urgent need to identify novel drugs to fight BC in the clinic...
July 29, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28752187/systematic-review-and-network-meta-analysis-comparing-palbociclib-with-chemotherapy-agents-for-the-treatment-of-postmenopausal-women-with-hr-positive-and-her2-negative-advanced-metastatic-breast-cancer
#20
Florence R Wilson, Abhishek Varu, Debanjali Mitra, Chris Cameron, Shrividya Iyer
PURPOSE: To compare palbociclib + letrozole and palbociclib + fulvestrant with chemotherapy agents in postmenopausal women with hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) advanced/metastatic breast cancer (ABC/MBC) who had no prior systemic treatment for advanced disease (first line) or whose disease progressed after prior endocrine therapy or chemotherapy (second line). METHODS: A systematic search identified randomized controlled trials (RCTs) published from January 2000 to January 2016 that compared endocrine-based therapies, chemotherapy agents, and/or chemotherapy agents + biological therapies in the first- and second-line treatment of postmenopausal women with HR+/HER2- ABC/MBC...
July 27, 2017: Breast Cancer Research and Treatment
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