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Aromatase inhibitors

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https://www.readbyqxmd.com/read/29144249/effect-of-antiandrogen-aromatase-inhibitor-and-gonadotropin-releasing-hormone-analog-on-adult-height-in-familial-male-precocious-puberty
#1
Ellen Werber Leschek, Armando C Flor, Joy C Bryant, Janet V Jones, Kevin M Barnes, Gordon B Cutler
OBJECTIVE: Antiandrogen, aromatase inhibitor, and gonadotropin-releasing hormone analog (GnRHa) treatment normalizes growth rate and bone maturation and increases predicted adult height (AH) in boys with familial male-limited precocious puberty (FMPP). To evaluate the effect of long-term antiandrogen, aromatase inhibitor, and GnRHa on AH, boys with FMPP who were treated were followed to AH. STUDY DESIGN: Twenty-eight boys with FMPP, referred to the National Institutes of Health, were started on antiandrogen and aromatase inhibitor at 4...
November 2017: Journal of Pediatrics
https://www.readbyqxmd.com/read/29141657/local-estrogen-axis-in-the-human-bone-microenvironment-regulates-estrogen%C3%A2-receptor-positive%C3%A2-breast-cancer-cells
#2
Derek F Amanatullah, John S Tamaresis, Pauline Chu, Michael H Bachmann, Nhat M Hoang, Deborah Collyar, Aaron T Mayer, Robert B West, William J Maloney, Christopher H Contag, Bonnie L King
BACKGROUND: Approximately 70% of all breast cancers express the estrogen receptor, and are regulated by estrogen. While the ovaries are the primary source of estrogen in premenopausal women, most breast cancer is diagnosed following menopause, when systemic levels of this hormone decline. Estrogen production from androgen precursors is catalyzed by the aromatase enzyme. Although aromatase expression and local estrogen production in breast adipose tissue have been implicated in the development of primary breast cancer, the source of estrogen involved in the regulation of estrogen receptor-positive (ER+) metastatic breast cancer progression is less clear...
November 15, 2017: Breast Cancer Research: BCR
https://www.readbyqxmd.com/read/29137864/synthesis-molecular-docking-and-qsar-study-of-sulfonamide-based-indoles-as-aromatase-inhibitors
#3
Ratchanok Pingaew, Prasit Mandi, Veda Prachayasittikul, Supaluk Prachayasittikul, Somsak Ruchirawat, Virapong Prachayasittikul
Thirty four of indoles bearing sulfonamides (11-44) were synthesized and evaluated for their anti-aromatase activities. Interestingly, all indole derivatives inhibited the aromatase with IC50 range of 0.7-15.3 μM. Indoles (27-36) exerted higher aromatase inhibitory activity than that of ketoconazole. The phenoxy analogs 28 and 34 with methoxy group were shown to be the most potent compounds with sub-micromolar IC50 values (i.e., 0.7 and 0.8 μM, respectively) without affecting to the normal cell line. Molecular docking demonstrated that the indoles 28, 30 and 34 could occupy the same binding site on the aromatase pocket and share several binding residues with those of the natural substrate (androstenedione), which suggested the competitive binding could be the mode of inhibition of the compounds...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29137842/comparison-of-pharmacokinetics-of-newly-discovered-aromatase-inhibitors-by-a-cassette-microdosing-approach-in-healthy-japanese-subjects
#4
Hiroyuki Kusuhara, Tadayuki Takashima, Hisako Fujii, Tsutomu Takashima, Masaaki Tanaka, Akira Ishii, Shusaku Tazawa, Kazuhiro Takahashi, Kayo Takahashi, Hidekichi Tokai, Tsuneo Yano, Makoto Kataoka, Akihiro Inano, Suguru Yoshida, Takamitsu Hosoya, Yuichi Sugiyama, Shinji Yamashita, Taisuke Hojo, Yasuyoshi Watanabe
The aim of the present study is to investigate the pharmacokinetics of our newly developed aromatase inhibitors (cetrozole and TMD-322) in healthy subjects by a cassette microdose strategy. A cocktail of cetrozole and TMD-322 was administered intravenously or orally (1.98 μg for each drug) to six healthy volunteers in a crossover fashion. Anastrozole (1.98 μg) was also included in the oral cocktail. Total body clearance and bioavailability were 12.1 ± 7.1 mL/min/kg and 34.9 ± 32.3% for cetrozole, and 16...
September 21, 2017: Drug Metabolism and Pharmacokinetics
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/29136387/randomized-multicenter-placebo-controlled-clinical-trial-of-duloxetine-versus-placebo-for-aromatase-inhibitor-associated-arthralgias-in-early-stage-breast-cancer-swog-s1202
#6
N Lynn Henry, Joseph M Unger, Anne F Schott, Louis Fehrenbacher, Patrick J Flynn, Debra M Prow, Carl W Sharer, Gary V Burton, Charles S Kuzma, Anna Moseley, Danika L Lew, Michael J Fisch, Carol M Moinpour, Dawn L Hershman, James L Wade
Purpose Adherence to aromatase inhibitor (AI) therapy for early-stage breast cancer is limited by AI-associated musculoskeletal symptoms (AIMSS). Duloxetine is US Food and Drug Administration approved for treatment of multiple chronic pain disorders. We hypothesized that treatment of AIMSS with duloxetine would improve average joint pain compared with placebo. Methods This randomized, double-blind, phase III trial included AI-treated postmenopausal women with early-stage breast cancer and who had average joint pain score of ≥ 4 out of 10 that developed or worsened since AI therapy initiation...
November 14, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/29135127/is-switching-to-tamoxifen-the-only-choice-of-treatment-for-improving-aromatase-inhibitor-toxicity
#7
Kadri Altundag
No abstract text is available yet for this article.
September 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/29134635/ribociclib-bioavailability-is-not-affected-by-gastric-ph-changes-or-food-intake-in-silico-and-clinical-evaluations
#8
Tanay S Samant, Shyeilla Dhuria, Yasong Lu, Marc Laisney, Shu Yang, Arnaud Grandeury, Martin Mueller-Zsigmondy, Kenichi Umehara, Felix Huth, Michelle Miller, Caroline Germa, Mohamed Elmeliegy
Ribociclib (KISQALI®), a cyclin-dependent kinase 4/6 inhibitor approved for the first-line treatment of HR+/HER2- advanced breast cancer with an aromatase inhibitor, is administered with no restrictions on concomitant gastric pH-elevating agents or food intake. The influence of proton pump inhibitors (PPIs) on ribociclib bioavailability was assessed using (1) biorelevant media solubility, (2) physiologically based pharmacokinetic (PBPK) modeling, (3) non-compartmental analysis (NCA) of clinical trial data, and (4) population PK (PopPK) analysis...
November 14, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29132462/-familial-male-limited-precocious-puberty-due-to-asp578his-mutations-in-the-lhcgr-gene-clinical-characteristics-and-gene-analysis-in-an-infant
#9
Min Wang, Min Li, Yue-Sheng Liu, Si-Min Lei, Yan-Feng Xiao
The aim of the study was to provide a descriptive analysis of familial male-limited precocious puberty (FMPP), which is a rare inherited disease caused by heterozygous constitutively activating mutations of the luteinizing hormone/choriogonadotropin receptor gene (LHCGR). The patient was a ten-month-old boy, presenting with penile enlargement, pubic hair formation, and spontaneous erections. Based on the clinical manifestations and laboratory data, including sexual characteristics, serum testosterone levels, GnRH stimulation test, and bone age, this boy was diagnosed with peripheral precocious puberty...
November 2017: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/29131988/treatment-adoption-and-relative-effectiveness-of-aromatase-inhibitors-compared-to-tamoxifen-in-early-breast-cancer-a-multi-institutional-observational-study
#10
Arlindo R Ferreira, Ana Palha, Lurdes Correia, Pedro Filipe, Vasco Rodrigues, Ana Miranda, Rosário André, João Fernandes, Joaquim Gouveia, José L Passos-Coelho, António Moreira, Margarida Brito, Joana Ribeiro, Otto Metzger-Filho, Nancy U Lin, Luís Costa, Inês Vaz-Luis
BACKGROUND: Since 2005, aromatase inhibitors (AIs) have been the adjuvant treatment of choice for postmenopausal women with early breast cancer (BC). In this study we characterize the adoption of AIs in Portugal, variables associated with treatment administration, and compare its effectiveness (either in monotherapy or sequential therapy) to tamoxifen monotherapy (TAM). PATIENTS AND METHODS: This was a retrospective cohort study that included postmenopausal women with stage I-III hormone receptor (HR) positive BC diagnosed from 2006 to 2008 and treated with adjuvant endocrine therapy in four participating institutions...
November 10, 2017: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/29131020/androgen-triggers-the-pro-migratory-cxcl12-cxcr4-axis-in-ar-positive-breast-cancer-cell-lines-underlying-mechanism-and-possible-implications-for-the-use-of-aromatase-inhibitors-in-breast-cancer
#11
Kalliopi Azariadis, Fotini Kiagiadaki, Vasiliki Pelekanou, Vasiliki Bempi, Kostas Alexakis, Marilena Kampa, Andreas Tsapis, Elias Castanas, George Notas
BACKGROUND/AIMS: Reports regarding the role of androgen in breast cancer (BC) are conflicting. Some studies suggest that androgen could lead to undesirable responses in the presence of certain BC tumor characteristics. We have shown that androgen induces C-X-C motif chemokine 12 (CXCL12) in BC cell lines. Our aim was to identify the mechanisms regulating the phenotypic effects of androgen-induced CXCL12 on Androgen Receptor (AR) positive BC cell lines. METHODS: We analyzed the expression of CXCL12 and its receptors with qPCR and ELISA and the role of Nuclear Receptor Coactivator 1 (NCOA1) in this effect...
November 3, 2017: Cellular Physiology and Biochemistry
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
#12
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
#13
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/29121290/pain-in-cancer-survivors-filling-in-the-gaps
#14
M Brown, P Farquhar-Smith
Cancer survivorship represents a growing clinical challenge for pain clinicians. The population of cancer survivors is rapidly expanding and many of these patients experience pain as a sequelae of their disease and its treatment. The features, pathophysiology and natural history of some painful conditions observed in cancer survivors, such as direct tumour effects, cancer induced bone pain (CIBP) or chronic post-surgical pain have received extensive exposure elsewhere in the literature. In this narrative review, we attempt to 'fill in the gaps' in the knowledge, by providing a succinct outline of a range of less well known pain states encountered in the cancer survivor population...
October 1, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29120657/-anabolic-steroid-induced-hypogonadism-in-men-overview-and-case-report
#15
Luboslav Stárka, Michaela Dušková, Lucie Kolátorová, Oldřich Lapčík
An important potential consequence of the anabolic steroid misuse is hypogonadotropic hypogonadism due to the inhibition of pituitary secretion of gonadotropins. By the symptoms as testicular atrophy, spermatogenic and fertility disturbances or dysfunction in sexual life, the anabolic steroids induced hypogonadism (ASIH) could be differentiated from organic hypogonadotropic hypogonadism only with difficulty unless the misuse is reported by the user. When diagnosed, the crucial step in the therapy is the stop of anabolic use...
2017: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29117210/quality-of-life-and-impact-of-pain-in-women-treated-with-aromatase-inhibitors-for-breast-cancer-a-multicenter-cohort-study
#16
Françoise Laroche, Serge Perrot, Terkia Medkour, Paul-Henri Cottu, Jean-Yves Pierga, Jean-Pierre Lotz, Karine Beerblock, Christophe Tournigand, Laure Chauvenet, Didier Bouhassira, Joël Coste
Women with hormone-dependent breast cancer are treated with aromatase inhibitors (AI) to slow disease progression by decreasing estrogen levels. However, AI have adverse effects, including pain, with potentially serious impact on quality of life (QOL) and treatment compliance. We evaluated quality of life during the first year of AI treatment, focusing particularly on the impact of pain. In a multicenter cohort study of 135 women with early-stage breast cancer, free of pain at the initiation of AI treatment, quality of life (by the EORTC QLQ-BR23), somatic and psychic symptoms, psychological characters, temperament and coping strategies were assessed at baseline and at each follow-up visit (1, 3, 6 and 12 months)...
2017: PloS One
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
#17
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/29116414/effect-of-denosumab-administration-on-low-bone-mineral-density-t-score-1-0-to-2-5-in-postmenopausal-japanese-women-receiving-adjuvant-aromatase-inhibitors-for-non-metastatic-breast-cancer
#18
Katsuhiko Nakatsukasa, Hiroshi Koyama, Yoshimi Ouchi, Kouichi Sakaguchi, Yoshifumi Fujita, Takayuki Matsuda, Makoto Kato, Eiichi Konishi, Tetsuya Taguchi
Although adjuvant aromatase inhibitor (AI) therapy is widely used in postmenopausal women with hormone receptor-positive breast cancer, it is known to be associated with bone loss and increased fracture risk. Denosumab, a fully human monoclonal antibody against the receptor activator of nuclear factor-κB ligand, has been shown to protect against AI-induced bone loss. However, the efficacy of denosumab in the treatment of AI-associated bone loss has not been prospectively evaluated in Japan. We prospectively monitored bone mineral density (BMD) of the lumbar spine and bilateral femoral necks in 100 postmenopausal women with hormone receptor-positive postoperative breast cancer of clinical stage I-IIIA in whom treatment with AI as adjuvant endocrine therapy was planned or had been ongoing...
November 7, 2017: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/29115707/in-vitro-screening-and-isolation-of-human-aromatase-inhibitors-from-cicer-arietinum-by-a-novel-continuous-online-method-combining-chromatographic-techniques
#19
Yuchi Zhang, Yan He, Chengyu Liu, Chunming Liu, Sainan Li
Ultrafiltration liquid chromatography with mass spectrometry can efficiently and rapidly screen and identify ligands from the seeds of Cicer arietinum for human aromatase. Using this method, we identified 11 major compounds, including organic acids, organic acid glycosides, flavone glycosides, isoflavones, and isoflavone glycosides, as potent human aromatase inhibitors. A continuous online method, including pressurized liquid extraction, countercurrent chromatography, and preparative liquid chromatography, was developed for scaling up the production of these compounds with high purity and efficiency...
November 8, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/29103853/adherence-to-adjuvant-endocrine-therapy-in-christchurch-women-with-early-breast-cancer
#20
B Robinson, B Dijkstra, V Davey, S Tomlinson, C Frampton
AIMS: To assess adherence to adjuvant endocrine therapy by a real-world cohort of women in Christchurch and to determine any associated factors. MATERIALS AND METHODS: Records were retrieved of all women newly diagnosed with early breast cancer and registered on the Christchurch Breast Cancer Patient Register over 4 years from June 2009. Demographic and pathological factors, dates of starting and stopping endocrine therapies and reported side-effects were collected...
November 2, 2017: Clinical Oncology: a Journal of the Royal College of Radiologists
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