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Raloxifene

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https://www.readbyqxmd.com/read/28054005/data-of-aromatase-inhibitors-alone-and-in-combination-with-raloxifene-on-microarchitecture-of-lumbar-vertebrae-and-strength-test-in-femoral-diaphysis-of-vcd-treated-ovotoxic-mice
#1
Abul Kalam, Sushama Talegaonkar, Divya Vohora
Currently, the third generation aromatase inhibitors are the drugs of choice for treatment of early and advanced breast cancer in postmenopausal women. The negative impact of these drugs on bone health is the significant limiting factor during this therapy. Here we report the effect of two aromatase inhibitors viz. letrozole and exemestane alone and in combination with raloxifene on lumbar vertebrae and femoral diaphysis after one month of treatment but no discernible effects were observed on bone when tested by micro CT and strength test except in trabecular number which was reduced in lumbar vertebrae following letrozole and exemestane...
February 2017: Data in Brief
https://www.readbyqxmd.com/read/28029084/variability-of-zaleplon-5-oxidase-activity-in-mice-and-humans-and-inhibition-by-raloxifene
#2
Chiaki Tanoue, Kazumi Sugihara, Yoshitaka Tayama, Naoto Uramaru, Yoko Watanabe, Shigeru Ohta, Shigeyuki Kitamura
Zaleplon (ZAL) is a sedative-hypnotic agent, which is mainly metabolized to inactive 5-oxidized zaleplon (5-oxo-ZAL) and N-des-ethylated ZAL (des-ethyl-ZAL) in mice and humans. The former reaction is considered to be catalyzed by aldehyde oxidase present in liver cytosol. Here, we examined sex and strain differences of ZAL metabolism to 5-oxo-ZAL among four strains of mice, as well as the inter-individual variation in humans, in order to evaluate the variability of 5-oxo-ZAL-forming activity and its relationship with aldehyde oxidase activity...
December 27, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/28028633/real-world-evidence-of-raloxifene-versus-alendronate-in-preventing-non-vertebral-fractures-in-japanese-women-with-osteoporosis-retrospective-analysis-of-a-hospital-claims-database
#3
Sakae Tanaka, Takanori Yamamoto, Eisei Oda, Masaki Nakamura, Saeko Fujiwara
We conducted a retrospective cohort study using a de-identified hospital administrative claims database to assess the risk of non-vertebral fracture in Japanese women with osteoporosis treated with raloxifene compared with alendronate. The study included Japanese women ≥50 years of age with newly initiated alendronate or raloxifene treatment between July 2008 and March 2013 (index date was defined as the day of first prescription for alendronate or raloxifene), and had any claim with an osteoporosis definition during the study period...
December 27, 2016: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/28012326/a-case-report-of-desmoid-tumour-a-forgotten-aspect-of-fap
#4
Sarah Xuereb, Rachel Xuereb, Chiara Buhagiar, Jonathan Gauci, Claude Magri
INTRODUCTION: Desmoid tumours are locally aggressive tumours which are common in Familial Adenomatous Polyposis (FAP). PRESENTATION OF CASE: A 20-year old Familial Adenomatous Polyposis (FAP) patient presented with abdominal pain and distention. Abdominal imaging showed small bowel obstruction and hydronephrosis due to a pelvic mass. This mass showed significant enlargement on repeat imaging, and a diagnostic biopsy confirmed desmoid tumour. The mass was deemed unresectable and he was initially started on sulindac and raloxifene...
December 1, 2016: International Journal of Surgery Case Reports
https://www.readbyqxmd.com/read/28003814/the-selective-estrogen-receptor-modulator-raloxifene-inhibits-neutrophil-extracellular-trap-formation
#5
Roxana Flores, Simon Döhrmann, Christina Schaal, Abdul Hakkim, Victor Nizet, Ross Corriden
Raloxifene is a selective estrogen receptor modulator typically prescribed for the prevention/treatment of osteoporosis in postmenopausal women. Although raloxifene is known to have anti-inflammatory properties, its effects on human neutrophils, the primary phagocytic leukocytes of the immune system, remain poorly understood. Here, through a screen of pharmacologically active small molecules, we find that raloxifene prevents neutrophil cell death in response to the classical activator phorbol 12-myristate 13-acetate (PMA), a compound known to induce formation of DNA-based neutrophil extracellular traps (NETs)...
2016: Frontiers in Immunology
https://www.readbyqxmd.com/read/27999800/effects-of-raloxifene-on-the-proliferation-and-apoptosis-of-human-aortic-valve-interstitial-cells
#6
Zhimin Fu, Bin Luo, Mingpeng Li, Bin Peng, Zheng Wang
We aimed to explore the effects of raloxifene (RAL) on the proliferation and apoptosis of human aortic valve interstitial cells (AVICs). Different concentrations of RAL were used to act on AVICs. MTS kit is used to test the effects of different concentrations of RAL on the proliferation of AVICs. Cell cycle and apoptosis test used flow cytometry after seven-day treatment. The relative expression levels of caspase-3 and caspase-8 are tested with RT-qPCR and Western blot. The results of MTS testing revealed that the absorbance value (OD value) of the cells in the concentration groups of 10 and 100 nmol/L RAL at a wavelength of 490 nm at five, seven, and nine days significantly decreased compared with that in the control group...
2016: BioMed Research International
https://www.readbyqxmd.com/read/27988379/raloxifene-microsphere-embedded-collagen-chitosan-%C3%AE-tricalcium-phosphate-scaffold-for-effective-bone-tissue-engineering
#7
Ming-Lei Zhang, Ji Cheng, Ye-Chen Xiao, Ruo-Feng Yin, Xu Feng
Engineering novel scaffolds that can mimic the functional extracellular matrix (ECM) would be a great achievement in bone tissue engineering. This paper reports the fabrication of novel collagen/chitosan/β-tricalcium phosphate (CCTP) based tissue engineering scaffold. In order to improve the regeneration ability of scaffold, we have embedded raloxifene (RLX)-loaded PLGA microsphere in the CCTP scaffold. The average pore of scaffold was in the range of 150-200μm with ideal mechanical strength and swelling/degradation characteristics...
December 14, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27974229/selective-estrogen-receptor-modulators-and-the-vitamin-d-analogue-eldecalcitol-block-bone-loss-in-male-osteoporosis
#8
Yuiko Sato, Toshimi Tando, Mayu Morita, Kana Miyamoto, Tami Kobayashi, Ryuichi Watanabe, Takatsugu Oike, Morio Matsumoto, Masaya Nakamura, Takeshi Miyamoto
Rapid increases in the number of elderly people have dramatically increased the number of female and male osteoporosis patients. Osteoporosis often causes bone fragility fractures, and males exhibit particularly poor prognosis after these fractures, indicating that control of osteoporosis is crucial to maintain quality of men's lives. However, osteoporosis therapies available for men have lagged behind advances available for women. Here, we show that three selective estrogen receptor modulators (SERMs), namely, raloxifene, bazedoxifene, and tamoxifen, plus the vitamin D analogue ED71, also called eldecalcitol, completely block orchiectomy-induced, testosterone-depleted bone loss in male mice in vivo...
January 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27973466/treatment-of-menopausal-symptoms-new-era-with-new-options-or-new-options-for-menopausal-symptoms-after-15-years-of-whi-study
#9
Santiago Palacios, Pluvio J Coronado
Menopausal symptoms include vasomotor symptoms (VMS), vulvar-vaginal atrophy, and loss of bone mass associated with an increased risk of fracture. Treatment of VMS consists of lifestyle changes, hormone treatment (estrogens with and without progestogens, tissue selective estrogens complex or conjugated estrogens and bazedoxifene [CE/BZA], progestogens, and tibolone), and nonhormonal treatments. Genitourinary symptoms due to vulvar-vaginal atrophy are treated with systemic and local hormones, moisturizer creams and gels, CE/BZA, and a selective estrogen receptor modulator (ospemifene)...
December 14, 2016: Minerva Ginecologica
https://www.readbyqxmd.com/read/27935770/from-breast-cancer-to-antimicrobial-combating-extremely-resistant-gram-negative-superbugs-using-novel-combinations-of-polymyxin-b-with-selective-estrogen-receptor-modulators
#10
Maytham H Hussein, Elena K Schneider, Alysha G Elliott, Meiling Han, Felisa Reyes-Ortega, Faye Morris, Mark A T Blastovich, Raad Jasim, Bart Currie, Mark Mayo, Mark Baker, Matthew A Cooper, Jian Li, Tony Velkov
Novel therapeutic approaches are urgently needed to combat nosocomial infections caused by extremely drug-resistant (XDR) "superbugs." This study aimed to investigate the synergistic antibacterial activity of polymyxin B in combination with selective estrogen receptor modulators (SERMs) against problematic Gram-negative pathogens. In vitro synergistic antibacterial activity of polymyxin B and the SERMs tamoxifen, raloxifene, and toremifene was assessed using the microdilution checkerboard and static time-kill assays against a panel of Gram-negative isolates...
December 9, 2016: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
https://www.readbyqxmd.com/read/27915335/network-meta-analysis-of-pharmacological-agents-for-osteoporosis-treatment-and-fracture-prevention
#11
Xu-Cheng Yang, Zhen-Han Deng, Ting Wen, Wei Luo, Wen-Feng Xiao, Rui-Bo Zhao, Yu-Sheng Li
BACKGROUND AND OBJECTIVE: Osteoporosis afflicts a large number of populations in the world and is featured by systemic impairment of bone mass and strength which may further trigger an increase in the risk of fragile fractures. This network meta-analysis (NMA) is designed to distinguish therapies more preferable than others with respect to efficacy and safety. METHODS: We searched the medical literature for relevant studies systematically. Both direct and indirect evidence were synthesized to compare the efficacy, described by odds ratios (OR) and 95% credible intervals (CrI)...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27900864/-raloxifene-an-unexploited-possibility-of-prevention-and-treatment-of-postmenopausal-osteoporosis
#12
Jan Štěpán, Jan Rosa, Karel Pavelka
Long-term estrogen deficiency after menopause is responsible for different disorders, which not only make the quality of life in the older age worse but also are the major causes of womens mortality. It is especially the case for cardiovascular disease and osteoporosis. Aim of this review is to point at efficacy of raloxifene (a selective estrogen receptor modulator) in the long-term care of the women in their non-reproductive period of life, and namely in prevention and treatment of postmenopausal osteoporosis...
2016: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/27887655/fracture-risk-and-healthcare-resource-utilization-and-costs-among-osteoporosis-patients-with-type-2-diabetes-mellitus-and-without-diabetes-mellitus-in-japan-retrospective-analysis-of-a-hospital-claims-database
#13
Masayo Sato, Wenyu Ye, Tomoko Sugihara, Yoshitaka Isaka
BACKGROUND: Osteoporosis, osteoporosis-related fractures, and diabetes are considerable health burdens in Japan. Diabetes in patients with osteoporosis has been reported to be associated with increased fracture risk. This retrospective analysis of a Japanese hospital claims database investigated the real-world effect of type 2 diabetes mellitus (T2DM) on the incidence of clinical fractures, costs, and healthcare resource utilization in patients with osteoporosis and a subgroup of patients prescribed raloxifene...
November 25, 2016: BMC Musculoskeletal Disorders
https://www.readbyqxmd.com/read/27879272/quantification-of-pathway-cross-talk-reveals-novel-synergistic-drug-combinations-for-breast-cancer
#14
Samira Jaeger, Ana Igea, Rodrigo Arroyo, Victor Alcalde, Begoña Canovas, Modesto Orozco, Angel R Nebreda, Patrick Aloy
Combinatorial therapeutic approaches are an imperative to improve cancer treatment, because it is critical to impede compensatory signaling mechanisms that can engender drug resistance to individual targeted drugs. Currently approved drug combinations result largely from empirical clinical experience and cover only a small fraction of a vast therapeutic space. Here we present a computational network biology approach, based on pathway cross-talk inhibition, to discover new synergistic drug combinations for breast cancer treatment...
November 22, 2016: Cancer Research
https://www.readbyqxmd.com/read/27857920/effectiveness-of-osteoporosis-drug-in-postmenopausal-women-with-spinal-compression-fracture-combined-consecutive-therapy-of-teriparatide-and-raloxifene-versus-bisphosphonate-single
#15
Chang Jin Shin, Sion Kim, Chun Sik Choi, Hyun Chul Shin, Young Joon Kwon
OBJECTIVE: Bisphosphonate, a typical bone resorption inhibitor, is an important first-line drug for treating osteoporosis. Recent studies show a novel paradigm in stimulating bone formation. Teriparatide, which is composed of recombinant human parathyroid hormone, stimulates osteoblasts and induces bone regeneration. Bone mineral density (BMD) that was used before and after the treatment with anti-osteoporosis drug was compared for the effectiveness in therapy between a combination of teriparatide and selective estrogen receptor modulator (SERM), and bisphosphonate...
October 2016: Korean Journal of Neurotrauma
https://www.readbyqxmd.com/read/27852187/prevention-of-breast-cancer
#16
Ian N Olver
Modifiable lifestyle factors may reduce the risk of developing breast cancer. Obesity is associated particularly with post-menopausal breast cancer. Diet is important, and exercise equivalent to running for up to 8 hours each week reduces the risk of breast cancer, both in its own right and through reducing obesity. Alcohol consumption may be responsible for 5.8% of breast cancers in Australia and it is recommended to reduce this to two standard drinks per day. Drinking alcohol and smoking increases the risk for breast cancer and, therefore, it is important to quit tobacco smoking...
November 21, 2016: Medical Journal of Australia
https://www.readbyqxmd.com/read/27848887/metabolism-and-toxicological-implications-of-commonly-used-chemopreventive-drugs-against-breast-cancer-carcinogenesis
#17
Aliyu Muhammad, Mohammed Auwal Ibrahim, Ochuko Lucky Erukainure, Ibrahim Malami, Hadiza Sani, Hafsat Abdullahi Mohammed
BACKGROUND: Breast cancer has been reported to be among the frequently diagnosed cancer in women worldwide despite advances in early detection and treatment. Several drugs are currently used for chemoprevention as a result of a number of drawbacks associated with breast cancer therapy. AIM: This review focuses on the metabolism and toxicological implications of these drugs against breast cancer/carcinogenesis. METHODOLOGY: Relevant articles on the commonly used anti-breast cancer drugs (raloxifene, tamoxifen, anastrozole, letrozole and exemestane) used in chemoprevention were searched using the major scientific databases including Scopus, Embase, PubMed/ Medline, Sciencedirect and Google Scholar...
November 16, 2016: Current Drug Metabolism
https://www.readbyqxmd.com/read/27842943/raloxifene-increases-prefrontal-activity-during-emotional-inhibition-in-schizophrenia-based-on-estrogen-receptor-genotype
#18
Jochen Kindler, Cynthia Shannon Weickert, Peter R Schofield, Rhoshel Lenroot, Thomas W Weickert
People with schizophrenia show decreased prefrontal cortex (PFC) activity during emotional response inhibition, a cognitive process sensitive to hormonal influences. Raloxifene, a selective estrogen receptor modulator, binds estrogen receptor alpha (ESR-α), improves memory, attention and normalizes cortical and hippocampal activity during learning and emotional face recognition in schizophrenia. Here, we tested the extent to which raloxifene restores neuronal activity during emotional response inhibition in schizophrenia...
December 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27833522/histamine-h3-receptors-and-its-antagonism-as-a-novel-mechanism-for-antipsychotic-effect-a-current-preclinical-clinical-perspective
#19
REVIEW
Danish Mahmood
Histamine H3 receptors are present as autoreceptors on histaminergic neurons and as heteroreceptors on nonhistaminergic neurones. They control the release and synthesis of histamine and several other key neurotransmitters in the brain. H3 antagonism may be a novel approach to develop a new class of antipsychotic medications given the gathering evidence reporting therapeutic efficacy in several central nervous system disorders. Several medications such as cariprazine, lurasidone, LY214002, bexarotene, rasagiline, raloxifene, BL-1020 and ITI-070 are being developed to treat the negative symptoms and cognitive impairments of schizophrenia...
October 2016: International Journal of Health Sciences
https://www.readbyqxmd.com/read/27832985/effects-of-raloxifene-against-letrozole-induced-bone-loss-in-chemically-induced-model-of-menopause-in-mice
#20
Abul Kalam, Sushama Talegaonkar, Divya Vohora
INTRODUCTION: The deleterious effects of letrozole, an aromatase inhibitor, used in the adjuvant treatment of breast cancer in postmenopausal women, on bone are well-documented and represent a major drawback to its clinical use. Raloxifene, a selective estrogen receptor modulator and a clinically approved anti-osteoporotic drug, has been recently demonstrated to be efficacious in women with breast cancer. The present study evaluated the effects of preventive and curative treatment with raloxifene on letrozole-induced alterations of bone microarchitecture and turnover markers in a chemically-induced menopause model in mice...
January 15, 2017: Molecular and Cellular Endocrinology
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