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Exemestane

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https://www.readbyqxmd.com/read/28817387/response-of-an-ovarian-granulosa-cell-tumor-with-everolimus-and-exemestane-after-initial-response-to-letrozole
#1
Tarek Assi, Hampig R Kourie, Elie El Rassy, Tania Moussa, Joseph Kattan
Granulosa cell tumors of the ovaries (GCTO), the most common sex cord tumors of the female genitalia, are characterized by a remarkably favorable prognosis but tend to recur even after several years of follow-up. Standard approach to manage these relapsing tumors is almost inexistent and physicians' choice is most commonly based on his/her personal expertise. Recently, the use of hormone therapy in GCTO has induced prolonged response and survival. In this case report, we report the first successful use of everolimus in the combination of exemestane to reverse the resistance to hormonal therapy with letrozole in a 53-year-old woman with GCTO...
September 2017: Anti-cancer Drugs
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
#2
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/28770670/potential-repositioning-of-exemestane-as-a-neuroprotective-agent-for-parkinson-s-disease
#3
Hyo Jin Son, Se Hee Han, Ji Ae Lee, Eun Jung Shin, Onyou Hwang
Parkinson's disease (PD) is a neurodegenerative disorder characterised by selective degeneration of the nigral dopaminergic neurons, and neuroinflammation and oxidative stress are believed to be involved in its pathogenesis. In the present study, we provide data that the synthetic steroid exemestane, which is currently being used to treat breast cancer, may be useful for PD therapy. In BV-2 microglial cells, exemestane activated the transcription factor Nrf2 and induced expression of the Nrf2-dependent genes that encode the antioxidant enzymes NAD(P)H: quinone oxidoreductase 1, haem oxygenase-1, and glutamylcysteine ligase...
June 2017: Free Radical Research
https://www.readbyqxmd.com/read/28765859/clinical-consultations-and-investigations-before-and-after-discontinuation-of-endocrine-therapy-in-women-with-primary-breast-cancer
#4
Derrick Lopez, Anna Kemp-Casey, Christobel Saunders, Elizabeth Roughead, Frances Boyle, Max Bulsara, David Preen
OBJECTIVE: Although clinical trials recommend that women with hormone-dependent primary breast cancer remain on endocrine therapy for at least 5 years, up to 60% discontinue treatment early. We determined whether these women had consulted with clinicians or had investigations for cancer recurrence or metastasis around the time they discontinued endocrine therapy, and whether clinical contact continued after discontinuation. METHODS: We performed case-control and cohort studies of women from the 45 and Up Study who were diagnosed with invasive primary breast cancer between January 2003 and December 2008, and who had ≥12 months of anastrozole, exemestane, letrozole or tamoxifen subsequently dispensed...
July 26, 2017: Public Health Research & Practice
https://www.readbyqxmd.com/read/28755088/adjuvant-endocrine-monotherapy-for-postmenopausal-early-breast-cancer-patients-with-hormone-receptor-positive-a-systemic-review-and-network-meta-analysis
#5
REVIEW
Zhu Yu, Xiaojing Guo, Yicheng Jiang, Lei Teng, Jinwu Luo, Pengfei Wang, Yunsheng Liang, Haitian Zhang
BACKGROUND: In patients with hormone receptor-positive postmenopausal of early stage breast cancer, adjuvant endocrine monotherapies include letrozole, anastrozole, exemestane, toremifene and tamoxifen. But the optimum regimen remains controversial. METHODS: PubMed, Cochrane Database and ClinicalTrials.gov were systematically reviewed of abstract for randomized-controlled trials (RCTs) to assess the efficacy of tamoxifen, letrozole, exemestane, anastrozle and toremifene for postmenopausal patients with hormone-receptor positive (HR+), who have not received prior therapy for early stage breast cancer...
July 28, 2017: Breast Cancer: the Journal of the Japanese Breast Cancer Society
https://www.readbyqxmd.com/read/28732650/adjuvant-tamoxifen-and-exemestane-in-women-with-postmenopausal-early-breast-cancer-team-10-year-follow-up-of-a-multicentre-open-label-randomised-phase-3-trial
#6
Marloes G M Derks, Erik J Blok, Caroline Seynaeve, Johan W R Nortier, Elma Meershoek-Klein Kranenbarg, Gerrit-Jan Liefers, Hein Putter, Judith R Kroep, Daniel Rea, Annette Hasenburg, Christos Markopoulos, Robert Paridaens, Jan B E Smeets, Luc Y Dirix, Cornelis J H van de Velde
BACKGROUND: After 5 years of median follow-up, the Tamoxifen Exemestane Adjuvant Multinational (TEAM) trial reported no difference in disease-free survival between exemestane monotherapy and a sequential scheme of tamoxifen followed by exemestane in postmenopausal patients with early-stage, hormone receptor-positive breast cancer. As recurrence risk in hormone receptor-positive breast cancer remains linear beyond 5 years after diagnosis, we analysed long-term follow-up outcomes of this trial...
July 18, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/28727815/polymorphisms-associated-with-everolimus-pharmacokinetics-toxicity-and-survival-in-metastatic-breast-cancer
#7
Tomas Pascual, María Apellániz-Ruiz, Cristina Pernaut, Cecilia Cueto-Felgueroso, Pablo Villalba, Carlos Álvarez, Luis Manso, Lucia Inglada-Pérez, Mercedes Robledo, Cristina Rodríguez-Antona, Eva Ciruelos
PURPOSE: Metastatic breast cancer (MBC) progressing after endocrine therapy frequently activates PI3K/AKT/mTOR pathway. The BOLERO-2 trial showed that everolimus-exemestane achieves increased progression free survival (PFS) compared with exemestane. However, there is great inter-patient variability in toxicity and response to exemestane-everolimus treatment. The objective of this study was to perform an exploratory study analyzing the implication of single nucleotide polymorphisms (SNPs) on outcomes from this treatment through a pharmacogenetic analysis...
2017: PloS One
https://www.readbyqxmd.com/read/28725277/sabcs-2016-systemic-therapy-for-metastatic-breast-cancer
#8
REVIEW
Simon Peter Gampenrieder, Gabriel Rinnerthaler, Richard Greil
At the 2016 San Antonio Breast Cancer Symposium, several interesting phase II and phase III studies investigating systemic therapies for metastatic breast cancer were presented. The PrEGOC 0102 trial demonstrated that the combination of fulvestrant plus everolimus is safe and effective and could be an alternative to exemestane plus everolimus for selected patients with hormone-receptor positive, HER2-negative disease. The pan-PI3K inhibitor buparlisib showed some activity in combination with fulvestrant after failure of everolimus in the BELLE-3 trial...
2017: Memo
https://www.readbyqxmd.com/read/28715929/molecular-interactions-of-bisphenols-and-analogs-with-glucocorticoid-biosynthetic-pathway-enzymes-an-in-silico-approach
#9
Garima Verma, Mohemmed Faraz Khan, Wasim Akhtar, Mohammad Mumtaz Alam, Mymoona Akhter, Mohammad Shaquiquzzaman
Glucocorticoids are known to have vital effects on metabolism, behavior and immunity. Any sort of impairment in their synthesis may lead to the generation of numerous ill health effects. Different environmental toxicants, including bisphenols and their analogs pose deleterious effect on the biosynthesis of glucocorticoids, thereby leading to endocrine disruption. In order to assess the effect of these environmental toxicants on gluocorticoid biosynthetic pathway, an in silico study was performed. This involved molecular docking studies of 18 ligands with the selected participating enzymes of the pathway...
July 17, 2017: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/28711793/efficacy-and-safety-of-everolimus-and-exemestane-in-hormone-receptor-positive-hr-human-epidermal-growth-factor-negative-her2-advanced-breast-cancer-patients-new-insights-beyond-clinical-trials-the-eva-study
#10
M E Cazzaniga, M Airoldi, V Arcangeli, S Artale, F Atzori, A Ballerio, G V Bianchi, L Blasi, S Campidoglio, M Ciccarese, M C Cursano, M Piezzo, A Fabi, L Ferrari, A Ferzi, C Ficorella, A Frassoldati, A Fumagalli, O Garrone, V Gebbia, D Generali, N La Verde, M Maur, A Michelotti, G Moretti, A Musolino, R Palumbo, M Pistelli, M Porpiglia, D Sartori, C Scavelli, A Schirone, A Turletti, M R Valerio, P Vici, A Zambelli, L Clivio, V Torri
BACKGROUND: The BOLERO-2 trial reported efficacy and safety of Everolimus (EVE) and Exemestane (EXE) combination in HR+ advanced breast cancer (ABC) patients. The BALLET trial further evaluated the safety of EVE-EXE in HR+ ABC patients, without reporting efficacy data. Aim of the EVA real-life study was to collect data of efficacy and safety of EVE-EXE combination in the clinical setting, as well as exploring efficacy according to EVE Dose-Intensity (DI) and to previous treatment with Fulvestrant...
July 13, 2017: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/28711612/exemestane-loaded-alginate-nanoparticles-for-cancer-treatment-formulation-and-in-vitro-evaluation
#11
Jayapal John Joseph, Dhanaraj Sangeetha
Alginate, a biopolymer is most useful for anticancer drug delivery, because of it is biocompatible, nontoxic, biodegradable and exploiting ligand-receptor interaction. Breast cancer is spreading very fast due to the changing food habits and environmental causes. Exemestane (EXE) an oral chemotherapeutic drug was used to treat breast cancer, while loading EXE in alginate nanoparticles, the side effects which was faced during administration are expected to be reduced and control the release of exemestane. Thus, in the present study, an anticancer drug EXE was loaded into the Alginate nanoparticles (ALG-NPs) through simple controlled gelation method and evaluated in vitro to study the performance of ALG-NPs in delivering the anticancer drug EXE...
July 12, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28681171/a-randomized-phase-ii-trial-of-ridaforolimus-dalotuzumab-and-exemestane-compared-with-ridaforolimus-and-exemestane-in-patients-with-advanced-breast-cancer
#12
Hope S Rugo, Olivier Trédan, Jungsil Ro, Serafin M Morales, Mario Campone, Antonino Musolino, Noémia Afonso, Marta Ferreira, Kyong Hwa Park, Javier Cortes, Antoinette R Tan, Joanne L Blum, Lamar Eaton, Christine K Gause, Zhen Wang, Ellie Im, David J Mauro, Mary Beth Jones, Andrew Denker, José Baselga
PURPOSE: To evaluate whether adding humanized monoclonal insulin growth factor-1 receptor (IGF-1R) antibody (dalotuzumab) to mammalian target of rapamycin (mTOR) inhibitor (ridaforolimus) plus aromatase inhibitor (exemestane) improves outcomes in patients with estrogen receptor (ER)-positive advanced/metastatic breast cancer. METHODS: This randomized, open-label, phase II trial enrolled 80 postmenopausal women with high-proliferation (Ki67 index staining ≥15%), ER-positive breast cancer that progressed after a non-steroidal aromatase inhibitor (NCT01605396)...
July 5, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28680952/a-review-of-fulvestrant-in-breast-cancer
#13
REVIEW
Mark R Nathan, Peter Schmid
Fulvestrant is a selective estrogen receptor degrader that binds, blocks and degrades the estrogen receptor (ER), leading to complete inhibition of estrogen signaling through the ER. This review article further explains the mechanism of action of the drug and goes on to review the trials carried out to optimize its dosing. Multiple trials have been undertaken to compare fulvestrant with other endocrine treatments, and results have shown it to have similar efficacy to anastrozole, tamoxifen and exemestane at 250 mg every 28 days...
2017: Oncology and Therapy
https://www.readbyqxmd.com/read/28669713/adjuvant-endocrine-therapy-for-premenopausal-women-type-and-duration
#14
Prudence A Francis
The Early Breast Cancer Trialists' Collaborative Group (EBCTCG) meta-analysis of randomized tamoxifen trials, found that women age <45 years with estrogen receptor-positive (ER+ve) breast cancer, allocated 5 years of adjuvant tamoxifen, have substantial long-term reduction of breast cancer recurrence. Breast cancer mortality was reduced by about one-third through the first 15 years. Increasing the duration of tamoxifen to 10 years can further reduce the risk of recurrence. For women age <45 years allocated 5 years of tamoxifen, the risk of contralateral breast cancer is halved over 15 years...
June 29, 2017: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/28663037/freeze-dried-solid-dispersion-of-exemestane-a-way-to-negate-an-aqueous-solubility-and-oral-bioavailability-problems
#15
Shamandeep Kaur, Sunil K Jena, Sanjaya K Samal, Vaishali Saini, Abhay T Sangamwar
This study was envisaged to demonstrate the potential of exemestane loaded phospholipid/sodium deoxycholate solid dispersions (EXE-PL/SDC-SDs) on the solubility and oral bioavailability of EXE. Initial studies were performed to screen the best suitable phospholipid among lysophosphatidylcholine, Phospholipon® P80H and Lipoid® E80S for solid dispersion preparation. Further studies were carried out to optimize the molar concentration of phospholipid and sodium deoxycholate (SDC) for EXE-PL/SDC-SDs preparation...
June 27, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28654365/treatment-efficacy-adherence-and-quality-of-life-among-women-younger-than-35-years-in-the-international-breast-cancer-study-group-text-and-soft-adjuvant-endocrine-therapy-trials
#16
Poornima Saha, Meredith M Regan, Olivia Pagani, Prudence A Francis, Barbara A Walley, Karin Ribi, Jürg Bernhard, Weixiu Luo, Henry L Gómez, Harold J Burstein, Vani Parmar, Roberto Torres, Josephine Stewart, Meritxell Bellet, Antonia Perelló, Faysal Dane, Antonio Moreira, Daniel Vorobiof, Michelle Nottage, Karen N Price, Alan S Coates, Aron Goldhirsch, Richard D Gelber, Marco Colleoni, Gini F Fleming
Purpose To describe benefits and toxicities of adjuvant endocrine therapies in women younger than 35 years with breast cancer (n = 582) enrolled in the Suppression of Ovarian Function Trial (SOFT) and Tamoxifen and Exemestane Trial (TEXT). Methods In SOFT, women still premenopausal after surgery with or without chemotherapy were randomly assigned to tamoxifen alone, tamoxifen plus ovarian function suppression (OFS), or exemestane plus OFS. In TEXT, all received OFS with or without concomitant chemotherapy and were randomly assigned to exemestane plus OFS or tamoxifen plus OFS...
June 27, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28649643/molecular-stratification-of-early-breast-cancer-identifies-drug-targets-to-drive-stratified-medicine
#17
Jane Bayani, Cindy Q Yao, Mary Anne Quintayo, Fu Yan, Syed Haider, Alister D'Costa, Cassandra L Brookes, Cornelis J H van de Velde, Annette Hasenburg, Dirk G Kieback, Christos Markopoulos, Luc Dirix, Caroline Seynaeve, Daniel Rea, Paul C Boutros, John M S Bartlett
Many women with hormone receptor-positive early breast cancer can be managed effectively with endocrine therapies alone. However, additional systemic chemotherapy treatment is necessary for others. The clinical challenges in managing high-risk women are to identify existing and novel druggable targets, and to identify those who would benefit from these therapies. Therefore, we performed mRNA abundance analysis using the Tamoxifen and Exemestane Adjuvant Multinational (TEAM) trial pathology cohort to identify a signature of residual risk following endocrine therapy and pathways that are potentially druggable...
2017: NPJ Breast Cancer
https://www.readbyqxmd.com/read/28643023/variable-aromatase-inhibitor-plasma-concentrations-do-not-correlate-with-circulating-estrogen-concentrations-in-post-menopausal-breast-cancer-patients
#18
Daniel L Hertz, Kelly A Speth, Kelley M Kidwell, Christina L Gersch, Zeruesenay Desta, Anna Maria Storniolo, Vered Stearns, Todd C Skaar, Daniel F Hayes, N Lynn Henry, James M Rae
PURPOSE: The aromatase inhibitors (AI) exemestane (EXE), letrozole (LET), and anastrozole suppress estrogen biosynthesis, and are effective treatments for estrogen receptor (ER)-positive breast cancer. Prior work suggests that anastrozole blood concentrations are associated with the magnitude of estrogen suppression. The objective of this study was to determine whether the magnitude of estrogen suppression, as determined by plasma estradiol (E2) concentrations, in EXE or LET treated patients is associated with plasma AI concentrations...
June 22, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28639029/cox2-induction-a-mechanism-of-endocrine-breast-cancer-resistance
#19
Brandi L Clark, Michael A Murphy, Landry K Kamdem
PURPOSE: Urine prostaglandin E2 (PGE2) levels have shown to be a risk factor of breast cancer, and the use of nonsteroidal anti-inflammatory drugs (NSAIDs) is known to be beneficial in preventing breast cancer risk and/or recurrence with or without aromatase inhibitors. We hypothesized that the use of an aromatase inhibitor triggers the activation of the inflammatory pathway via release of PGE2. METHODS: A single oral 25 mg dose of an aromatase inhibitor (exemestane) was given to 14 healthy postmenopausal female volunteers...
June 21, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28614542/use-of-anastrozole-in-the-chemoprevention-and-treatment-of-breast-cancer-a-literature-review
#20
Maria da Conceição Barros-Oliveira, Danylo Rafhael Costa-Silva, Danielle Benigno de Andrade, Umbelina Soares Borges, Cléciton Braga Tavares, Rafael Soares Borges, Janaína de Moraes Silva, Benedito Borges da Silva
Aromatase inhibitors have emerged as an alternative endocrine therapy for the treatment of hormone sensitive breast cancer in postmenopausal women. The use of third-generation inhibitors represented by exemestane, letrozol and anastrozole is currently indicated. Anastrozole is a nonsteroidal compound and a potent selective inhibitor of the aromatase enzyme. Although a few studies have shown that its pharmacodynamic and pharmacokinetic properties may be affected by interindividual variability, this drug has been recently used in all configurations of breast cancer treatment...
April 2017: Revista da Associação Médica Brasileira
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