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https://www.readbyqxmd.com/read/28529550/hormonoresistance-in-advanced-breast-cancer-a-new-revolution-in-endocrine-therapy
#1
REVIEW
Paule Augereau, Anne Patsouris, Emmanuelle Bourbouloux, Carole Gourmelon, Sophie Abadie Lacourtoisie, Dominique Berton Rigaud, Patrick Soulié, Jean Sebastien Frenel, Mario Campone
Endocrine therapy is the mainstay of treatment of estrogen-receptor-positive (ER+) breast cancer with an overall survival benefit. However, some adaptive mechanisms in the tumor emerge leading to the development of a resistance to this therapy. A better characterization of this process is needed to overcome this resistance and to develop new tailored therapies. Mechanisms of resistance to hormone therapy result in activation of transduction signal pathways, including the cell cycle regulation with cyclin D/CDK4/6/Rb pathway...
May 2017: Therapeutic Advances in Medical Oncology
https://www.readbyqxmd.com/read/28529128/role-of-gper-in-the-activation-of-endothelial-nitric-oxide-synthase
#2
Natalie C Fredette, Matthias R Meyer, Eric R Prossnitz
Estrogens are potent regulators of vascular tone, yet underlying receptor- and ligand-specific signaling pathways remain poorly characterized. The primary physiological estrogen 17β-estradiol (E2), a non-selective agonist of classical nuclear estrogen receptors (ERα and ERβ) as well as the G protein-coupled estrogen receptor (GPER), stimulates formation of the vasodilator nitric oxide (NO) in endothelial cells. Here, we studied the contribution of GPER signaling in E2-dependent activation of endothelial NO formation and subsequent vasodilation...
May 18, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28503095/the-cholesterol-metabolite-27-hydroxycholesterol-stimulates-cell-proliferation-via-er%C3%AE-in-prostate-cancer-cells
#3
Shaneabbas Raza, Megan Meyer, Casey Goodyear, Kimberly D P Hammer, Bin Guo, Othman Ghribi
BACKGROUND: For every six men, one will be diagnosed with prostate cancer (PCa) in their lifetime. Estrogen receptors (ERs) are known to play a role in prostate carcinogenesis. However, it is unclear whether the estrogenic effects are mediated by estrogen receptor α (ERα) or estrogen receptor β (ERβ). Although it is speculated that ERα is associated with harmful effects on PCa, the role of ERβ in PCa is still ill-defined. The cholesterol oxidized metabolite 27-hydroxycholesterol (27-OHC) has been found to bind to ERs and act as a selective ER modulator (SERM)...
2017: Cancer Cell International
https://www.readbyqxmd.com/read/28502177/leveraging-colloidal-aggregation-for-drug-rich-nanoparticle-formulations
#4
Ahil N Ganesh, Jennifer Logie, Christopher K McLaughlin, Benjamin L Barthel, Tad H Koch, Brian K Shoichet, Molly S Shoichet
While limited drug loading continues to be problematic for chemotherapeutics formulated in nanoparticles, we found that we could take advantage of colloidal drug aggregation to achieve high loading when combined with polymeric excipients. We demonstrate this approach with two drugs, fulvestrant and pentyl-PABC doxazolidine (PPD; a prodrug of doxazolidine, which is a DNA cross-linking anthracycline), and two polymers, polysorbate 80 (UP80) and poly(d,l-lactide-co-2-methyl-2-carboxytrimethylene carbonate)-graft-poly(ethylene glycol) (PLAC-PEG; a custom-synthesized, self-assembling amphiphilic polymer)...
May 19, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28500289/stapled-big3-helical-peptide-erap-potentiates-anti-tumour-activity-for-breast-cancer-therapeutics
#5
Tetsuro Yoshimaru, Keisuke Aihara, Masato Komatsu, Yosuke Matsushita, Yasumasa Okazaki, Shinya Toyokuni, Junko Honda, Mitsunori Sasa, Yasuo Miyoshi, Akira Otaka, Toyomasa Katagiri
Estradiol (E2) and the oestrogen receptor-alpha (ERα) signalling pathway play pivotal roles in the proliferative activity of breast cancer cells. Recent findings show that the brefeldin A-inhibited guanine nucleotide-exchange protein 3-prohibitin 2 (BIG3-PHB2) complex plays a crucial role in E2/ERα signalling modulation in breast cancer cells. Moreover, specific inhibition of the BIG3-PHB2 interaction using the ERα activity-regulator synthetic peptide (ERAP: 165-177 amino acids), derived from α-helical BIG3 sequence, resulted in a significant anti-tumour effect...
May 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28493933/direct-estrogen-receptor-er-her-family-crosstalk-mediating-sensitivity-to-lumretuzumab-and-pertuzumab-in-er-breast-cancer
#6
Denis Collins, Wolfgang Jacob, Juan Miguel Cejalvo, Maurizio Ceppi, Ian James, Max Hasmann, John Crown, Andrés Cervantes, Martin Weisser, Birgit Bossenmaier
Bidirectional cross talk between members of the human epidermal growth factor family of receptors (HER) and the estrogen receptor (ER) is believed to underlie resistance mechanisms that develop in response to treatment with anti-HER agents and endocrine therapy. We investigated the interaction between HER2, HER3 and the ER in vitro using human embryonic kidney cells transfected with human HER2, HER3, and ERα. We also investigated the additive efficacy of combination regimens consisting of anti-HER3 (lumretuzumab), anti-HER2 (pertuzumab), and endocrine (fulvestrant) therapy in vivo...
2017: PloS One
https://www.readbyqxmd.com/read/28488183/palbociclib-a-review-in-hr-positive-her2-negative-advanced-or-metastatic-breast-cancer
#7
REVIEW
Esther S Kim, Lesley J Scott
Oral palbociclib (Ibrance®) is a first-in-class, highly selective inhibitor of cyclin-dependent kinases 4 and 6 (i.e. a CDK4/6 inhibitor). It is indicated for the treatment of women with HR-positive, HER2-negative advanced or metastatic breast cancer, in combination with an aromatase inhibitor as initial endocrine-based therapy, and in combination with fulvestrant (with or without a luteinizing hormone-releasing hormone agonist) in those previously treated with endocrine therapy. In clinical trials, palbociclib in combination with letrozole as initial endocrine-based therapy in postmenopausal women (PALOMA-1 and PALOMA-2), or in combination with fulvestrant in pre-, peri-, or postmenopausal women with disease progression after endocrine therapy (PALOMA-3), significantly prolonged progression-free survival (PFS) and improved clinical benefit response (CBR) rates...
May 9, 2017: Targeted Oncology
https://www.readbyqxmd.com/read/28477031/fulvestrant-500-milligrams-as-endocrine-therapy-for-endocrine-sensitive-advanced-breast-cancer-patients-in-the-real-world-the-ful500-prospective-observational-trial
#8
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...
April 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/28472324/cost-effectiveness-of-palbociclib-in-hormone-receptor-positive-advanced-breast-cancer
#9
H Mamiya, R K Tahara, S M Tolaney, N Choudhry, M Najafzadeh
BACKGROUND: Palbociclib, a novel small-molecule inhibitor of cyclin-dependent kinases 4 and 6 for the treatment of advanced breast cancer, has demonstrated significant efficacy in prolonging progression-free survival when added to existing therapies. Considering the high cost of palbociclib, we assessed cost-effectiveness of adding palbociclib to usual care in treatment of advanced breast cancer. METHODS: We developed a discrete event simulation model to simulate time to cancer progression and to compare life time clinical benefit and cost of alternative treatment strategies for patients with metastatic disease from societal perspective...
May 2, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/28472036/accurate-detection-of-low-prevalence-akt1-e17k-mutation-in-tissue-or-plasma-from-advanced-cancer-patients
#10
Elza C de Bruin, Jessica L Whiteley, Claire Corcoran, Pauline M Kirk, Jayne C Fox, Javier Armisen, Justin P O Lindemann, Gaia Schiavon, Helen J Ambrose, Alexander Kohlmann
Personalized healthcare relies on accurate companion diagnostic assays that enable the most appropriate treatment decision for cancer patients. Extensive assay validation prior to use in a clinical setting is essential for providing a reliable test result. This poses a challenge for low prevalence mutations with limited availability of appropriate clinical samples harboring the mutation. To enable prospective screening for the low prevalence AKT1 E17K mutation, we have developed and validated a competitive allele-specific TaqMan® PCR (castPCR™) assay for mutation detection in formalin-fixed paraffin-embedded (FFPE) tumor tissue...
2017: PloS One
https://www.readbyqxmd.com/read/28468943/estradiol-activates-chloride-channels-via-the-estrogen-receptor-alpha-in-the-cell-membrane-in-osteoblasts
#11
Zhiqin Deng, Shuang Peng, Yanfang Zheng, Xiaoya Yang, Haifeng Zhang, Qiuchan Tan, Xiechou Liang, Hong Gao, Yuan Li, Yanqing Huang, Linyan Zhu, Tim Jc Jacob, Lixin Chen, Liwei Wang
Estrogen plays important roles in regulation of bone formation. Chloride channels in the ClC family are expressed in osteoblasts and are associated with bone physiology and pathology, but the relationship between chloride channels and estrogen is not clear. In this study, the action of estrogen on chloride channels was investigated in osteoblastic MC3T3-E1 cells. Results showed that 17β-estradiol could activate a current which reversed at a potential close to Cl(-) equilibrium potential with the anion selectivity I- >Br->Cl->gluconate and was inhibited by the chloride channel blockers 5-nitro-2-(3-phenylpropylamino)-benzoate (NPPB) and 4,4'-Diisothiocyano-2,2'-stilbenedisulfonic acid (DIDS) and knockdown of ClC-3 chloride channel expression...
May 3, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28463012/comparison-of-palbociclib-in-combination-with-letrozole-or-fulvestrant-with-endocrine-therapies-for-advanced-metastatic-breast-cancer-network-meta-analysis
#12
Costel Chirila, Debanjali Mitra, Ann Colosia, Caroline Ling, Dawn Odom, Shrividya Iyer, James A Kaye
BACKGROUND: Palbociclib is the first cyclin-dependent kinase 4/6 inhibitor approved in the United States for HR+/HER2- advanced/metastatic breast cancer, in combination with letrozole as initial endocrine-based therapy in postmenopausal women or with fulvestrant in women with disease progression following endocrine therapy. We compared progression-free survival (PFS) and discontinuations due to adverse events for palbociclib combinations against other endocrine therapies using a mixed-treatment comparison meta-analysis of randomized, controlled trials...
May 16, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28454109/anthropometric-clinical-and-molecular-determinants-of-treatment-outcomes-in-postmenopausal-hormone-receptor-positive-metastatic-breast-cancer-patients-treated-with-fulvestrant-results-from-a-real-word-setting
#13
Laura Pizzuti, Clara Natoli, Teresa Gamucci, Mariella Mauri, Domenico Sergi, Luigi Di Lauro, Giancarlo Paoletti, Enzo Ruggeri, Laura Iezzi, Isabella Sperduti, Lucia Mentuccia, Agnese Fabbri, Marcello Maugeri-Saccà, Luca Moscetti, Maddalena Barba, Patrizia Vici
To characterize determinants of treatment outcome in a real world population of 161 post-menopausal hormone receptor-positive metastatic breast cancer patients treated with fulvestrant. Descriptive statistics for demographics, anthropometrics, clinical and molecular characteristic were compared across subgroups of sensitivity/resistance to prior endocrine therapy and tested in uni/multivariate models. Clinical benefit was more common in sensitive patients with higher estrogen receptor expression and when fulvestrant was given in first line (p=0...
April 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28454082/estrogen-promotes-tumor-metastasis-via-estrogen-receptor-beta-mediated-regulation-of-matrix-metalloproteinase-2-in-non-small-cell-lung-cancer
#14
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...
April 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445992/interaction-between-the-estrogen-receptor-and-fibroblast-growth-factor-receptor-pathways-in-non-small-cell-lung-cancer
#15
Jill M Siegfried, Mariya Farooqui, Natalie J Rothenberger, Sanja Dacic, Laura P Stabile
The estrogen receptor (ER) promotes non-small cell lung cancer (NSCLC) proliferation. Since fibroblast growth factors (FGFs) are known regulators of stem cell markers in ER positive breast cancer, we investigated whether a link between the ER, FGFs, and stem cell markers exists in NSCLC. In lung preneoplasias and adenomas of tobacco carcinogen exposed mice, the anti-estrogen fulvestrant and/or the aromatase inhibitor anastrozole blocked FGF2 and FGF9 secretion, and reduced expression of the stem cell markers SOX2 and nanog...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28444131/fulvestrant-plus-lhrh-analogs-in-male-with-synchronous-breast-and-prostate-cancer
#16
C Martinez, L A Fernández-Morales, H Oliveres, M Marín, P Ribera, J C Pardo, E Dalmau, M A Segui
No abstract text is available yet for this article.
April 24, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/28441073/orbital-and-conjunctival-metastasis-from-lobular-breast-carcinoma
#17
Margarita Sánchez Orgaz, Tais Gonzalez Pessolani, José J Pozo Kreilinger, Pilar Zamora, Covadonga Martí Álvarez, Ana Boto-de-Los-Bueis
This article examines the clinical presentation of ocular metastasis from an infiltrating lobular breast carcinoma. We examined a conjunctival biopsy from a 69-year-old woman who developed unilateral conjunctival inflammation together with a neurotrophic corneal ulcer and proptosis. Infiltrating lobular breast carcinoma (ILBC) was diagnosed using routine histology and immunohistochemistry. She had a past history of a hormone receptor-positive infiltrating ILBC 11 years ago with cutaneous and diffuse osteoblastic metastases, and she was kept under treatment with lezotrol...
April 25, 2017: Orbit
https://www.readbyqxmd.com/read/28439683/genistein-modulation-of-seizure-involvement-of-estrogen-and-serotonin-receptors
#18
Saeed Amiri Gheshlaghi, Razieh Mohammad Jafari, Mohammad Algazo, Nastaran Rahimi, Hussein Alshaib, Ahmad Reza Dehpour
Genistein, a major source of phytoestrogen exposure for humans and animals, has been shown to mediate neuroprotection in Alzheimer's disease and status epilepticus. In the present study, we investigated the effect of genistein on pentylenetetrazole-induced seizures in ovariectomized mice and the possible involvement of estrogenic and serotonergic pathways in the probable effects of genistein. Intraperitoneal (i.p.) administration of genistein (10 mg/kg) significantly increased the seizure threshold 30 min prior to induction of seizures 14 days after ovariectomy surgery...
April 24, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28438180/recent-advances-of-highly-selective-cdk4-6-inhibitors-in-breast-cancer
#19
REVIEW
Hanxiao Xu, Shengnan Yu, Qian Liu, Xun Yuan, Sridhar Mani, Richard G Pestell, Kongming Wu
Uncontrolled cell division is the hallmark of cancers. Full understanding of cell cycle regulation would contribute to promising cancer therapies. In particular, cyclin-dependent kinases 4/6 (CDK4/6), which are pivotal drivers of cell proliferation by combination with cyclin D, draw more and more attention. Subsequently, extensive studies were carried out to explore drugs inhibiting CDK4/6 and assess the efficacy and safety of these drugs in cancer, especially breast cancer. Due to the insuperable adverse events and the less activity observed in vivo, the drug development of the initial pan-CDK inhibitor flavopiridol was consequently discontinued, and then highly specific inhibitors were extensively researched and developed, including palbociclib (PD0332991), ribociclib (LEE011), and abemaciclib (LY2835219)...
April 24, 2017: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/28430646/immunotherapeutic-target-expression-on-breast-tumors-can-be-amplified-by-hormone-receptor-antagonism-a-novel-strategy-for-enhancing-efficacy-of-targeted-immunotherapy
#20
Ritika Jaini, Matthew G Loya, Charis Eng
Immunotherapy has historically been successful in highly antigenic tumors but has shown limited therapeutic efficacy in non-antigenic tumors such as breast cancers. Our previous studies in autoimmunity have demonstrated that increased antigen load within a tissue enhances immune reactivity against it. We therefore hypothesized that enhancing expression of target proteins on breast tumors can increase efficacy of targeted immunotherapy. We hypothesized that antagonism of the estrogen receptor (ER) can increase expression of targets that are hormonally regulated and facilitate enhanced tumor recognition by targeted immunotherapy...
May 16, 2017: Oncotarget
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