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Fulvestrant

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https://www.readbyqxmd.com/read/29328488/synthesis-and-application-of-131i-fulvestrant-as-a-targeted-radiation-drug-for-endocrine-therapy-in-human-breast-cancer
#1
Guobing Yin, Bin Zeng, Zhiping Peng, Ying Liu, Lu Sun, Changan Liu
The aim of this study was to label fulvestrant (an endocrine therapy drug for breast cancer) with radioiodine and to evaluate the effect of 131I-fulvestrant on inhibiting the growth of human breast cancer and its influence on major organs in nude mice. Fulvestrant was labeled with radioiodine using a modified chloramine T method, and its chemical properties were assessed using traditional methods. The binding affinity of 131I-fulvestrant was measured by radioligand binding assays, and its antiproliferative activity was determined by MTT assays...
January 11, 2018: Oncology Reports
https://www.readbyqxmd.com/read/29328407/estrogen-receptor-%C3%AE-1-activation-accelerates-resistance-to-epidermal-growth-factor-receptor-tyrosine-kinase-inhibitors-in-non-small-cell-lung-cancer
#2
Shengling Fu, Changyu Liu, Quanfu Huang, Sheng Fan, Hexiao Tang, Xiangning Fu, Bo Ai, Yongde Liao, Qian Chu
Non-small cell lung cancer (NSCLC) is one of the leading causes of cancer-related deaths worldwide. Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR‑TKIs) have revolutionized the treatment of patients with advanced EGFR-mutant NSCLC. However, drug resistance eventually develops in the majority of patients despite an excellent initial response. The present study aimed to investigate the mechanism of acquired resistance to EGFR-TKIs and to explore strategies to overcome the resistance to EGFR-TKIs from a gender perspective...
January 4, 2018: Oncology Reports
https://www.readbyqxmd.com/read/29326029/neoadjuvant-treatment-with-trastuzumab-and-pertuzumab-plus-palbociclib-and-fulvestrant-in-her2-positive-er-positive-breast-cancer-na-pher2-an-exploratory-open-label-phase-2-study
#3
Luca Gianni, Giancarlo Bisagni, Marco Colleoni, Lucia Del Mastro, Claudio Zamagni, Mauro Mansutti, Milvia Zambetti, Antonio Frassoldati, Raffaella De Fato, Pinuccia Valagussa, Giuseppe Viale
BACKGROUND: In the neoadjuvant setting, blockade of HER2 plus use of an aromatase inhibitor in patients with HER2-positive and oestrogen receptor (ER)-positive breast cancer leads to a pathological complete response in 21% of patients. Convergence of HER2 and ER signals on RB1 suggests that a combined pharmacological intervention directed to these targets could be synergistic. To test this approach, we combined palbociclib to block RB1, fulvestrant to block ER, and trastuzumab with pertuzumab to block HER2 in patients with HER2-positive, ER-positive breast cancer...
January 8, 2018: Lancet Oncology
https://www.readbyqxmd.com/read/29324303/first-line-vs-second-line-fulvestrant-for-hormone-receptor-positive-advanced-breast-cancer-a-post-hoc-analysis-of-the-confirm-study
#4
Angelo Di Leo, Guy Jerusalem, Roberto Torres, Didier Verhoeven, Kelly Pendergrass, Luca Malorni, Jasmine Lichfield, Miguel Martin
OBJECTIVES: The double-blind, phase III CONFIRM study (NCT00099437) evaluated fulvestrant 500 mg vs fulvestrant 250 mg in postmenopausal women with hormone receptor-positive locally advanced/metastatic breast cancer (LA/MBC). This post-hoc analysis investigated the efficacy and safety of fulvestrant given either first-line or second-line for advanced disease. MATERIALS & METHODS: Progression-free survival (PFS) and overall survival (OS) with fulvestrant 500 mg vs fulvestrant 250 mg was evaluated using unadjusted log-rank tests in patients treated in the first- (progression during or within 12 months after completing adjuvant endocrine therapy; n = 387) and second-line (following endocrine therapy for LA/MBC; n = 343) settings...
January 8, 2018: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/29316692/3-3-diindolylmethane-suppressed-cyprodinil-induced-epithelial-mesenchymal-transition-and-metastatic-related-behaviors-of-human-endometrial-ishikawa-cells-via-an-estrogen-receptor-dependent-pathway
#5
Bo-Gyoung Kim, Jin-Wook Kim, Soo-Min Kim, Ryeo-Eun Go, Kyung-A Hwang, Kyung-Chul Choi
Cyprodinil (CYP) is a pyrimidine amine fungicide that has been extensively used in agricultural areas. 3,3'-Diindolylmethane (DIM) is a derivative of the dietary phytoestrogen, indole-3-carbinol (I3C), which is derived from cruciferous vegetables and considered to be a cancer-preventive phytonutrient agent. In this study, the effects of CYP and DIM were examined on the cell viability, invasion, and metastasis of human endometrial cancer cells, Ishikawa, via epithelial mesenchymal transition (EMT). CYP increased the level of cell viability of Ishikawa cells compared to DMSO as a control, as did E2...
January 8, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29311658/local-delivery-of-hormonal-therapy-with-silastic-tubing-for-prevention-and-treatment-of-breast-cancer
#6
Jeenah Park, Scott Thomas, Allison Y Zhong, Alan R Wolfe, Gregor Krings, Manuela Terranova-Barberio, Nela Pawlowska, Leslie Z Benet, Pamela N Munster
Broad use of germline testing has identified an increasing number of women at risk for breast cancer with a need for effective chemoprevention. We report a novel method to selectively deliver various anti-estrogens at high drug levels to the breast tissue by implanting a device comprised of silastic tubing. Optimized tubing properties allow elution of otherwise poorly bioavailable anti-estrogens, such as fulvestrant, into mammary tissue in vitro and in vivo with levels sufficient to inhibit estrogen receptor activation and tumor cell proliferation...
January 8, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29307843/development-of-leads-targeting-er-%C3%AE-in-breast-cancer-an-in-silico-exploration-from-natural-domain
#7
Snehal S Ashtekar, Neela M Bhatia, Manish S Bhatia
The steroid, estrogen has been recognized as being important for stimulating the growth of breast cancers primarily mediated via the steroidal estrogen receptor-α (ER-α). Inhibition of estrogen activity by small molecules with increased target specificity has proven to be an effective treatment for breast cancer. After the success stories of SERMs and fulvestrant, there is a need for the development of new small molecule modulating ER-α is due to developing resistance and side effects to current breast cancer therapy...
January 4, 2018: Steroids
https://www.readbyqxmd.com/read/29289986/phase-i-trial-to-evaluate-the-addition-of-alisertib-to-fulvestrant-in-women-with-endocrine-resistant-er-metastatic-breast-cancer
#8
Tufia C Haddad, Antonino D'Assoro, Vera Suman, Mateusz Opyrchal, Prema Peethambaram, Minetta C Liu, Matthew P Goetz, James N Ingle
PURPOSE: In estrogen receptor-positive (ER+) breast cancer models, activation of Aurora A kinase (AURKA) is associated with downregulation of ERα expression and resistance to endocrine therapy. Alisertib is an oral selective inhibitor of AURKA. The primary objectives of this phase I trial were to determine the recommended phase II dose (RP2D) and evaluate the toxicities and clinical activity of alisertib combined with fulvestrant in patients with ER+ metastatic breast cancer (MBC). METHODS: In this standard 3 + 3 dose-escalation phase I study, postmenopausal patients with endocrine-resistant, ER+ MBC previously treated with endocrine therapy were assigned to one of two dose levels of alisertib (40 or 50 mg) in combination with fixed-dose fulvestrant...
December 30, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/29247442/efficacy-of-palbociclib-plus-fulvestrant-after-everolimus-in-hormone-receptor-positive-metastatic-breast-cancer
#9
Pauline du Rusquec, Clément Palpacuer, Loic Campion, Anne Patsouris, Paule Augereau, Carole Gourmelon, Marie Robert, Laurence Dumas, Folliard Caroline, Mario Campone, Jean-Sébastien Frenel
BACKGROUND: Palbociclib, a CDK4-6 inhibitor, combined with endocrine therapy (ET) is a new standard of treatment for Hormone Receptor-positive Metastatic Breast Cancer. We present the first real-life efficacy and tolerance data of palbociclib plus fulvestrant in this population. METHODS: From November 2015 to November 2016, patients receiving in our institution palbociclib + fulvestrant according to the Temporary Authorization for Use were prospectively analyzed...
December 15, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/29234250/are-we-ready-to-use-esr1-mutations-in-clinical-practice
#10
REVIEW
Rinath Jeselsohn
The recurrent ligand-binding domain ESR1 mutations are an important mechanism of endocrine resistance in estrogen receptor-positive (ER+) metastatic breast cancer. These mutations evolve under the selective pressure of endocrine treatments and are rarely found in treatment-naïve ER+ breast cancers. Preclinical studies showed that these mutations lead to ligand-independent activity facilitating resistance to aromatase inhibitors and relative resistance to tamoxifen and fulvestrant. Retrospective analyses of ESR1 mutations in baseline plasma circulating tumor DNA from clinical trials suggest that these mutations are prognostic of poor overall survival and predictive of resistance to aromatase inhibitors in metastatic disease...
October 2017: Breast Care
https://www.readbyqxmd.com/read/29223745/buparlisib-plus-fulvestrant-in-postmenopausal-women-with-hormone-receptor-positive-her2-negative-advanced-breast-cancer-progressing-on-or-after-mtor-inhibition-belle-3-a-randomised-double-blind-placebo-controlled-phase-3-trial
#11
Angelo Di Leo, Stephen Johnston, Keun Seok Lee, Eva Ciruelos, Per E Lønning, Wolfgang Janni, Ruth O'Regan, Marie-Ange Mouret-Reynier, Dimitar Kalev, Daniel Egle, Tibor Csőszi, Roberto Bordonaro, Thomas Decker, Vivianne C G Tjan-Heijnen, Sibel Blau, Alessio Schirone, Denis Weber, Mona El-Hashimy, Bharani Dharan, Dalila Sellami, Thomas Bachelot
BACKGROUND: Activation of the PI3K/AKT/mTOR pathway occurs frequently in breast cancer that is resistant to endocrine therapy. Approved mTOR inhibitors effectively inhibit cell growth and proliferation but elicit AKT phosphorylation via a feedback activation pathway, potentially leading to resistance to mTOR inhibitors. We evaluated the efficacy and safety of buparlisib plus fulvestrant in patients with advanced breast cancer who were pretreated with endocrine therapy and mTOR inhibitors...
December 6, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/29192207/discovery-of-naturally-occurring-esr1-mutations-in-breast-cancer-cell-lines-modelling-endocrine-resistance
#12
Lesley-Ann Martin, Ricardo Ribas, Nikiana Simigdala, Eugene Schuster, Sunil Pancholi, Tencho Tenev, Pascal Gellert, Laki Buluwela, Alison Harrod, Allan Thornhill, Joanna Nikitorowicz-Buniak, Amandeep Bhamra, Marc-Olivier Turgeon, George Poulogiannis, Qiong Gao, Vera Martins, Margaret Hills, Isaac Garcia-Murillas, Charlotte Fribbens, Neill Patani, Zheqi Li, Matthew J Sikora, Nicholas Turner, Wilbert Zwart, Steffi Oesterreich, Jason Carroll, Simak Ali, Mitch Dowsett
Resistance to endocrine therapy remains a major clinical problem in breast cancer. Genetic studies highlight the potential role of estrogen receptor-α (ESR1) mutations, which show increased prevalence in the metastatic, endocrine-resistant setting. No naturally occurring ESR1 mutations have been reported in in vitro models of BC either before or after the acquisition of endocrine resistance making functional consequences difficult to study. We report the first discovery of naturally occurring ESR1 Y537C and ESR1 Y537S mutations in MCF7 and SUM44 ESR1-positive cell lines after acquisition of resistance to long-term-estrogen-deprivation (LTED) and subsequent resistance to fulvestrant (ICIR)...
November 30, 2017: Nature Communications
https://www.readbyqxmd.com/read/29180066/inhibition-of-estrogen-receptor-reduces-connexin-43-expression-in-breast-cancers
#13
Cheng-Fang Tsai, Yu-Kai Cheng, Dah-Yuu Lu, Shu-Lin Wang, Chen-Ni Chang, Pei-Chun Chang, Wei-Lan Yeh
Connexins are widely supported as tumor suppressors due to their downregulation in cancers, nevertheless, more recent evidence suggests roles for connexins in facilitating tumor progression in later stages, including metastasis. One of the key factors regulating the expression, modification, stability, and localization of connexins is hormone receptors in hormone-dependent cancers. It is reasonable to consider that hormones/hormone receptors may modulate connexins expression and play critical roles in the cellular control of connexins during breast cancer progression...
November 24, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29178019/efficacy-of-fulvestrant-in-the-treatment-of-postmenopausal-women-with-endocrine-resistant-advanced-breast-cancer-in-routine-clinical-practice
#14
I Blancas, M Fontanillas, V Conde, J Lao, E Martínez, M J Sotelo, A Jaen, J L Bayo, F Carabantes, J J Illarramendi, M M Gordon, J Cruz, A García-Palomo, C Mendiola, E Pérez-Ruiz, J S Bofill, J M Baena-Cañada, N M Jáñez, G Esquerdo, M Ruiz-Borrego
INTRODUCTION: This study aimed to describe the efficacy of fulvestrant 500 mg in postmenopausal women with estrogen receptor (ER)-positive advanced/metastatic breast cancer who had disease progression after receiving anti-estrogen therapy in clinical practice, getting real-world data. MATERIALS AND METHODS: Multicenter, retrospective, observational study conducted in Spain. Postmenopausal women with locally advanced/metastatic ER-positive breast cancer who received treatment with fulvestrant 500 mg after progression with a previous anti-estrogen therapy were eligible...
November 24, 2017: Clinical & Translational Oncology
https://www.readbyqxmd.com/read/29176653/estrogen-induces-c-kit-and-an-aggressive-phenotype-in-a-model-of-invasive-lobular-breast-cancer
#15
J Chuck Harrell, Thomas M Shroka, Britta M Jacobsen
Among the molecular subtypes of breast cancer are luminal (A or B) estrogen receptor positive (ER+), HER2+, and triple negative (basal-like). In addition to the molecular subtypes, there are 18 histologic breast cancer subtypes classified on appearance, including invasive lobular breast carcinoma (ILC), which are 8-15% of all breast cancers and are largely ER+ tumors. We used a new model of ER+ ILC, called BCK4. To determine the estrogen regulated genes in our ILC model, we examined BCK4 xenograft tumors from mice supplemented with or without estrogen using gene expression arrays...
November 27, 2017: Oncogenesis
https://www.readbyqxmd.com/read/29167821/ptk6-regulates-growth-and-survival-of-endocrine-therapy-resistant-er-breast-cancer-cells
#16
Koichi Ito, Sun Hee Park, Igor Katsyv, Weijia Zhang, Carmine De Angelis, Rachel Schiff, Hanna Y Irie
The non-receptor tyrosine kinase, PTK6/BRK, is highly expressed in multiple tumor types, including prostate, ovarian, and breast cancers, and regulates oncogenic phenotypes such as proliferation, migration, and survival. PTK6 inhibition also overcomes targeted therapy resistance of HER2+ breast cancer. Although PTK6 is highly expressed in ER+ Luminal breast cancers, the role of PTK6 in this subtype has not been elucidated. In this study, we investigated the functions of PTK6 in ER+ Luminal breast cancer cells, including those that are relatively resistant to estrogen deprivation or targeted endocrine therapies used in the treatment of ER+ cancers...
2017: NPJ Breast Cancer
https://www.readbyqxmd.com/read/29141561/steroidal-anticancer-agents-an-overview-of-estradiol-related-compounds
#17
Renata Minorics, Istvan Zupko
Research of steroidal compounds as anticancer agents started almost 50 years ago. During the past decades several innovative new steroids, like cyproterone, finasteride, estramustin, exemestane and fulvestrant have successfully become part of routine clinical practice. Meanwhile, a vast amount of new information have accumulated about the functions of the endogenous steroid system (including the characterization of enzymes, receptors, transcription pathways, etc.) and about the role of steroids in carcinogenesis...
November 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29128965/abemaciclib-first-global-approval
#18
Esther S Kim
Abemaciclib (Verzenio™) is an orally administered inhibitor of cyclin-dependent kinases 4 and 6 that is being developed by Eli Lilly and Company. Abemaciclib has been approved in the USA for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer, in combination with fulvestrant in women with disease progression following endocrine therapy, and as monotherapy in adult patients with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting...
December 2017: Drugs
https://www.readbyqxmd.com/read/29122702/estrogenic-effects-following-larval-exposure-to-the-putative-anti-estrogen-fulvestrant-in-the-fathead-minnow-pimephales-promelas
#19
Jonathan M Ali, Michael T Palandri, Alex T Kallenbach, Edwin Chavez, Jonathan Ramirez, Sathaporn Onanong, Daniel D Snow, Alan S Kolok
The objective of the present study was to investigate the consequences of early-life exposure to fulvestrant on estrogenic gene expression in fathead minnow larvae. To address this objective, fathead minnow larvae were exposed to fulvestrant (ICI 182,780) during the window of sexual differentiation between 0 to 30 days post-hatch (dph). The four treatment groups in this study included: filtered water controls (never exposed), solvent controls (ethanol 0.01%), and nominally low (0.10μg/L) and high (10.0μg/L) doses of fulvestrant...
November 6, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/29106989/gonadal-hormones-affect-alcohol-drinking-but-not-cue-yohimbine-induced-alcohol-seeking-in-male-and-female-rats
#20
Megan L Bertholomey, Mary M Torregrossa
Alcohol use disorder (AUD) is a chronic, relapsing disease characterized by maladaptive patterns of alcohol drinking and seeking. Though sex differences exist in the etiology of AUD, much remains to be elucidated concerning the mechanisms underlying sex-related vulnerability to developing excessive alcohol-motivated behavior. While a large body of evidence points to an important role of circulating gonadal hormones in mediating cocaine reinforcement, findings are less consistent with respect to ethanol. Critically, the effects of gonadal hormones on the reinstatement of ethanol seeking, a model of "craving"-like behavior that reveals pronounced sex differences, has not yet been examined...
October 26, 2017: Physiology & Behavior
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