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Exemestane

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https://www.readbyqxmd.com/read/29221608/a-case-of-eruptive-disseminated-porokeratosis-in-a-cancer-patient-after-trastuzumab-and-exemestane-treatment-cancer-related-or-drug-induced-phenomenon
#1
C Mangas, V Espeli, R Blum
No abstract text is available yet for this article.
December 5, 2017: Actas Dermo-sifiliográficas
https://www.readbyqxmd.com/read/29177605/evaluation-of-applying-ihc4-as-a-prognostic-model-in-the-translational-study-of-intergroup-exemestane-study-ies-pathies
#2
M C U Cheang, J M Bliss, G Viale, V Speirs, C Palmieri, A Shaaban, P E Lønning, J Morden, N Porta, J Jassem, C J van De Velde, B B Rasmussen, D Verhoeven, J M S Bartlett, R C Coombes
BACKGROUND: Intergroup Exemestane Study (IES) was a randomised study that showed a survival benefit of switching adjuvant endocrine therapy after 2-3 years from tamoxifen to exemestane. This PathIES aimed to assess the role of immunohistochemical (IHC)4 score in determining the relative sensitivity to either tamoxifen or sequential treatment with tamoxifen and exemestane. PATIENTS AND METHODS: Primary tumour samples were available for 1274 patients (27% of IES population)...
November 24, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/29177573/triptorelin-a-review-of-its-use-as-an-adjuvant-anticancer-therapy-in-early-breast-cancer
#3
James E Frampton
A 1-month formulation of the gonadotrophin-releasing hormone agonist (GnRHa) triptorelin (Decapeptyl®) has been approved in the EU as an adjuvant treatment in combination with tamoxifen or an aromatase inhibitor (AI), of endocrine-responsive, early-stage breast cancer in women at high risk of recurrence who are confirmed as premenopausal after completion of chemotherapy. This indication reflects the results of the 5-year SOFT and TEXT studies, especially SOFT, in which ovarian function suppression (OFS; mainly achieved with triptorelin) added to tamoxifen provided a significant benefit in the overall study population of premenopausal patients only after adjusting for prognostic factors...
November 25, 2017: Drugs
https://www.readbyqxmd.com/read/29141561/steroidal-anticancer-agents-an-overview-of-estradiol-related-compounds
#4
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/29137418/a-randomized-phase-ii-study-of-aromatase-inhibitors-plus-metformin-in-pre-treated-postmenopausal-patients-with-hormone-receptor-positive-metastatic-breast-cancer
#5
Yannan Zhao, Chengcheng Gong, Zhonghua Wang, Jian Zhang, Leiping Wang, Sheng Zhang, Jun Cao, Zhonghua Tao, Ting Li, Biyun Wang, Xichun Hu
Background: Everolimus significantly improves progression-free survival (PFS) and has been approved to use in aromatase inhibitor pretreated patients with hormone receptor positive advanced breast cancer. Metformin has been shown to inhibit mTOR pathway, with more favorable safety profile, leading to this hypothesis-generating trial to assess whether metformin enhances the efficacy of aromatase inhibitors. Methods: 60 postmenopausal women with hormone receptor positive locally advanced or metastatic breast cancer were randomly assigned 1:1 to aromatase inhibitor (exemestane 25mg/d or letrozole 2...
October 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/29128813/effect-of-aromatase-inhibitors-on-learning-and-memory-and-modulation-of-hippocampal-dickkopf-1-and-sclerostin-in-female-mice
#6
Saima Zameer, Divya Vohora
BACKGROUND: There has been conflicting reports on the effect of third generation aromatase inhibitors on cognition in estrogen-deficient states. Since aromatase inhibitors themselves cause estrogen deprivation, the present work was designed to evaluate the comparative effect of three aromatase inhibitors on behavioral measures of learning and memory in female mice. Further, in view of the reports of estrogen and Wnt signaling pathway in cognition, the role of two Wnt signaling antagonists (dickkopf-1 and sclerostin) in mediation of cognitive effects of aromatase inhibitors was evaluated...
June 13, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29128193/vitamin-d-levels-vitamin-d-receptor-polymorphisms-and-inflammatory-cytokines-in-aromatase-inhibitor-induced-arthralgias-an-analysis-of-cctg-ma-27
#7
Polly Niravath, Bingshu Chen, Judy-Anne W Chapman, Sandeep K Agarwal, Robert L Welschhans, Tim Bongartz, Krishna R Kalari, Lois E Shepherd, John Bartlett, Kathleen Pritchard, Karen Gelmon, Susan G Hilsenbeck, Mothaffar F Rimawi, C Kent Osborne, Paul E Goss, James N Ingle
BACKGROUND: Approximately half of women taking aromatase inhibitor (AI) therapy develop AI-induced arthralgia (AIA), and many might discontinue AI therapy because of the pain. Using plasma samples from the MA.27 study, we assessed several factors potentially associated with AIA. PATIENTS AND METHODS: MA.27 is a phase III adjuvant trial comparing 2 AIs, exemestane versus anastrozole. Within an 893-participant nested case-control AIA genome-wide association study, we nested a 72 AIA case-144 control assessment of vitamin D plasma concentrations, corrected for seasonal and geographic variation...
October 16, 2017: Clinical Breast Cancer
https://www.readbyqxmd.com/read/29124456/serial-immunological-parameters-in-a-phase-ii-trial-of-exemestane-and-low-dose-oral-cyclophosphamide-in-advanced-hormone-receptor-positive-breast-cancer
#8
Maryann Kwa, Xiaochun Li, Yelena Novik, Ruth Oratz, Komal Jhaveri, Jennifer Wu, Ping Gu, Marleen Meyers, Franco Muggia, James Speyer, Alyssa Iwano, Maryam Bonakdar, Lina Kozhaya, Ece Tavukcuoglu, Bahar Budan, Roy Raad, Judith D Goldberg, Derya Unutmaz, Sylvia Adams
BACKGROUND AND PURPOSE: Resistance to endocrine therapies in hormone receptor (HR)-positive breast cancer is a significant challenge. Prior studies have shown that low-dose oral cyclophosphamide can transiently deplete regulatory T cells (Tregs) and improve anti-tumor immunity. We investigated the combination of exemestane with cyclophosphamide in patients with advanced HR-positive breast cancer and assessed changes in circulating immune cell subsets. METHODS: This was a single-arm phase II trial of exemestane with cyclophosphamide in patients with metastatic HR-positive/HER2-negative breast cancer who had progressed on prior endocrine therapy (ClinicalTrials...
November 9, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/29116433/safety-of-everolimus-plus-exemestane-in-patients-with-hormone-receptor-positive-her2-negative-locally-advanced-or-metastatic-breast-cancer-results-of-phase-iiib-ballet-trial-in-spain
#9
E Ciruelos, M Vidal, E Martínez de Dueñas, N Martínez-Jáñez, Y Fernández, J A García-Sáenz, L Murillo, F Carabantes, A Beliera, R Fonseca, J Gavilá
BACKGROUND: Everolimus with exemestane has shown promising activity in patients with hormone-receptor (HR)-positive HER2-negative endocrine-resistant advanced breast cancer. It is necessary, therefore, to characterize the safety profile of this new combination in the real-world clinical setting and in the broadest possible population. PATIENTS AND METHODS: Post-menopausal women with HR-positive HER2-negative advanced breast cancer progressing after prior non-steroidal aromatase inhibitors (NSAIs) were included...
November 7, 2017: Clinical & Translational Oncology
https://www.readbyqxmd.com/read/29103175/efficacy-and-safety-in-older-patient-subsets-in-studies-of-endocrine-monotherapy-versus-combination-therapy-in-patients-with-hr-her2-%C3%A2-advanced-breast-cancer-a-review
#10
REVIEW
Rachel A Freedman, Sara M Tolaney
PURPOSE: Prospective information regarding the tolerability and efficacy of endocrine therapy (ET) alone and in combination with targeted agents in older patients in the metastatic setting is limited. This review summarizes available trial data in this population. METHODS: We searched PubMed for Phase 2 or 3 trials with age-stratified patient cohorts (≥ 65 vs. < 65 years in most studies) with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer treated with ET ± targeted agents...
November 4, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/29097108/everolimus-plus-letrozole-for-treatment-of-patients-with-hr-her2-advanced-breast-cancer-progressing-on-endocrine-therapy-an-open-label-phase-ii-trial
#11
Tamar Safra, Bella Kaufman, Luna Kadouri, Noa Efrat Ben-Baruch, Larisa Ryvo, Bella Nisenbaum, Ella Evron, Rinat Yerushalmi
PURPOSE: In the Breast cancer trials of OraL EveROlimus-2 (BOLERO-2) trial, everolimus plus exemestane improved progression-free survival (PFS) in patients with hormone receptor-positive (HR(+)), human epidermal growth factor receptor 2-negative (HER2(-)) advanced breast cancer (ABC) recurring or progressing on/after prior endocrine therapy (ET), suggesting that dual blockade using targeted therapy and ET was an effective treatment option. Here, we investigated the clinical benefit of combining everolimus with different endocrine partner, letrozole, in a similar patient population...
September 19, 2017: Clinical Breast Cancer
https://www.readbyqxmd.com/read/29094642/shell-crosslinked-zein-nanocapsules-for-oral-codelivery-of-exemestane-and-resveratrol-in-breast-cancer-therapy
#12
Ahmed O Elzoghby, Sarah A El-Lakany, Maged W Helmy, Marwa M Abu-Serie, Nazik A Elgindy
AIM: Oral administration of exemestane (EXM) and resveratrol (RES) for breast cancer therapy has been limited by their poor solubility and low permeability. METHODS: In this study, these issues were tackled using zein nanocapsules (ZNCs) for oral EXM/RES codelivery combining drug solubilization within oily core and resistance to digestion via hydrophobic protein shell. Furthermore, higher oral stability and sustained release could be enabled by glutaraldehyde crosslinking of zein shell...
December 2017: Nanomedicine
https://www.readbyqxmd.com/read/29071118/influence-of-aromatase-inhibitors-therapy-on-the-occurrence-of-rheumatoid-arthritis-in-women-with-breast-cancer-results-from-a-large-population-based-study-of-the-italian-society-for-rheumatology
#13
Marta Caprioli, Greta Carrara, Garifallia Sakellariou, Ettore Silvagni, Carlo Alberto Scirè
OBJECTIVES: The purpose of this study was to evaluate the risk of developing rheumatoid arthritis (RA) in a population of patients with breast cancer treated with aromatase inhibitors (AIs) compared with tamoxifen. METHODS: Data were collected from the administrative healthcare database of Lombardy Region, Italy, from 2004 to 2013. This study follows a nested cohort design, including women with a diagnosis of breast cancer starting treatment with tamoxifen, anastrozole, exemestane or letrozole...
2017: RMD Open
https://www.readbyqxmd.com/read/28982841/adjuvant-endocrine-therapy-for-hormone-positive-breast-cancer-focusing-on-ovarian-suppression-and-extended-treatment-an-update
#14
REVIEW
Daniel Glassman, Sue Hignett, Shazza Rehman, Richard Linforth, Mohamed Salhab
The benefits of five years of adjuvant endocrine therapy for oestrogen receptor (ER)-positive early breast cancer are well established. However, recent evidence suggests that extended endocrine treatment and ovarian suppression in selected groups of patients have significant advantages. In this article, we review the current evidence for adjuvant endocrine therapy in breast cancer with focus on extended adjuvant endocrine therapy and ovarian suppression, and also highlight the advantages and disadvantages of these therapeutic strategies...
October 2017: Anticancer Research
https://www.readbyqxmd.com/read/28959637/depsidones-inhibit-aromatase-activity-and-tumor-cell-proliferation-in-a-co-culture-of-human-primary-breast-adipose-fibroblasts-and-t47d-breast-tumor-cells
#15
Suthat Chottanapund, M B M Van Duursen, Anne Zwartsen, Supatchaya Timtavorn, Panida Navasumrit, Prasat Kittakoop, Sanya Sureram, Mathuros Ruchirawat, Martin Van den Berg
Naturally occurring depsidones from the marine fungus Aspergillus unguis are known to have substantial anti-cancer activity, but their mechanism of action remains elusive. The purpose of this study was to examine the anti-aromatase activity of two common depsidones, unguinol and aspergillusidone A, in a co-culture system of human primary breast adipose fibroblasts and hormonal responsive T47D breast tumor cells. Using this in vitro model it was shown that these depsidones inhibit the growth of T47D tumor cells most likely via inhibition of aromatase (CYP19) activity...
2017: Toxicology Reports
https://www.readbyqxmd.com/read/28927154/resistance-to-the-mtor-inhibitor-everolimus-is-reversed-by-the-downregulation-of-survivin-in-breast-cancer-cells
#16
Ludovica Taglieri, Francesca De Iuliis, Anna Giuffrida, Sabrina Giantulli, Ida Silvestri, Susanna Scarpa
Everolimus (RAD001) is an inhibitor of mammalian target of rapamycin used in combination with exemestane to treat hormone receptor-positive advanced breast cancer. However, not all patients are equally sensitive to RAD001 and certain patients develop resistance. Therefore, the present study analyzed the mechanisms involved in the resistance of breast cancer cells to RAD001 in order to identify a potential tool to overcome it. The effects of RAD001 on the inhibition of cell viability, on the induction of apoptosis and autophagy and on the regulation of survivin, an anti-apoptotic protein, were evaluated in two breast cancer cell lines: BT474 (luminal B) and MCF7 (luminal A)...
September 2017: Oncology Letters
https://www.readbyqxmd.com/read/28878375/fasting-glucose-and-body-mass-index-as-predictors-of-activity-in-breast-cancer-patients-treated-with-everolimus-exemestane-the-everext-study
#17
Laura Pizzuti, Paolo Marchetti, Clara Natoli, Teresa Gamucci, Daniele Santini, Angelo Fedele Scinto, Laura Iezzi, Lucia Mentuccia, Loretta D'Onofrio, Andrea Botticelli, Luca Moscetti, Francesca Sperati, Claudio Botti, Francesca Ferranti, Simonetta Buglioni, Giuseppe Sanguineti, Simona Di Filippo, Luigi di Lauro, Domenico Sergi, Teresa Catenaro, Silverio Tomao, Antonio Giordano, Marcello Maugeri-Saccà, Maddalena Barba, Patrizia Vici
Evidence on everolimus in breast cancer has placed hyperglycemia among the most common high grade adverse events. Anthropometrics and biomarkers of glucose metabolism were investigated in a observational study of 102 postmenopausal, HR + HER2- metastatic breast cancer patients treated with everolimus-exemestane in first and subsequent lines. Best overall response (BR) and clinical benefit rate (CBR) were assessed across subgroups defined upon fasting glucose (FG) and body mass index (BMI). Survival was estimated by Kaplan-Meier method and log-rank test...
September 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28868654/impact-of-the-oatp1b1-c-521t-c-single-nucleotide-polymorphism-on-the-pharmacokinetics-of-exemestane-in-healthy-post-menopausal-female-volunteers
#18
B J Gregory, S M Chen, M A Murphy, D H Atchley, L K Kamdem
WHAT IS KNOWN AND OBJECTIVE: OATP1B1 mediates the transport of a diverse range of amphiphilic organic compounds that include bile acids, steroid conjugates and hormones. This retrospective pharmacogenetic study was conducted to assess the impact of the OATP1B1 c.521T>C single nucleotide polymorphism (SNP) on the pharmacokinetics of the steroidal aromatase inhibitor drug exemestane in healthy volunteers. METHODS: Exemestane (25 mg) was administered orally to 14 healthy post-menopausal women...
October 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28865686/use-of-the-hyphenated-lc-ms-ms-technique-and-nmr-ir-spectroscopy-for-the-identification-of-exemestane-stress-degradation-products-during-the-drug-development
#19
Elżbieta U Stolarczyk, Anna Rosa, Marek Kubiszewski, Joanna Zagrodzka, Marcin Cybulski, Łukasz Kaczmarek
Exemestane (6-Methyleneandrosta-1,4-diene-3,17-dione) active pharmaceutical ingredient (EE-3) was subjected to thermal, photolytic, oxidative, acidic and base stress conditions prescribed by the ICH (International Conference on Harmonization) guideline Q1A(R2). EE-3 was found to degrade in base, acidic and oxidative conditions. Eleven new degradation products of EE-3 were characterized by the LC-MS/MS technique. One of these impurities was isolated and identified by the LC-MS/MS, NMR and IR techniques. The LC-MS/MS studies were carried out to establish fragmentation pathways of EE-3 and its new impurity...
September 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28862117/hormone-therapy-in-breast-cancer
#20
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
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