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https://www.readbyqxmd.com/read/27900864/-raloxifene-an-unexploited-possibility-of-prevention-and-treatment-of-postmenopausal-osteoporosis
#1
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
#2
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-crosstalk-reveals-novel-synergistic-drug-combinations-for-breast-cancer
#3
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, since 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 crosstalk 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
#4
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
#5
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
#6
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
#7
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...
November 11, 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
#8
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
#9
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...
November 8, 2016: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/27832523/ovariectomy-induced-mitochondrial-oxidative-stress-apoptosis-and-calcium-ion-influx-through-trpa1-trpm2-and-trpv1-are-prevented-by-17%C3%AE-estradiol-tamoxifen-and-raloxifene-in-the-hippocampus-and-dorsal-root-ganglion-of-rats
#10
Yener Yazğan, Mustafa Nazıroğlu
Relative 17β-estradiol (E2) deprivation and excessive production of mitochondrial oxygen free radicals (OFRs) with a high amount of Ca(2+) influx TRPA1, TRPM2, and TRPV1 activity is one of the main causes of neurodegenerative disease in postmenopausal women. In addition to the roles of tamoxifen (TMX) and raloxifene (RLX) in cancer and bone loss treatments, regulator roles in Ca(2+) influx and mitochondrial oxidative stress in neurons have not been reported. The aim of this study was to evaluate whether TMX and RLX interactions with TRPA1, TRPM2, and TRPV1 in primary hippocampal (HPC) and dorsal root ganglion (DRG) neuron cultures of ovariectomized (OVX) rats...
November 10, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27802325/selective-estrogen-receptor-modulators-suppress-hif1%C3%AE-protein-accumulation-in-mouse-osteoclasts
#11
Mayu Morita, Yuiko Sato, Ryotaro Iwasaki, Tami Kobayashi, Ryuichi Watanabe, Takatsugu Oike, Kana Miyamoto, Yoshiaki Toyama, Morio Matsumoto, Masaya Nakamura, Hiromasa Kawana, Taneaki Nakagawa, Takeshi Miyamoto
Anti-bone resorptive drugs such as bisphosphonates, the anti-RANKL antibody (denosumab), or selective estrogen receptor modulators (SERMs) have been developed to treat osteoporosis. Mechanisms underlying activity of bisphosphonates or denosumab in this context are understood, while it is less clear how SERMs like tamoxifen, raloxifene, or bazedoxifene inhibit bone resorption. Recently, accumulation of hypoxia inducible factor 1 alpha (Hif1α) in osteoclasts was shown to be suppressed by estrogen in normal cells...
2016: PloS One
https://www.readbyqxmd.com/read/27798863/substituted-tetrahydroisoquinolines-as-microtubule-destabilizing-agents-in-triple-negative-human-breast-cancer-cells
#12
Madhavi Gangapuram, Riccardo Jean, Elizabeth Mazzio, Ramesh Badisa, Suresh Eyunni, Carl B Goodman, Kinfe K Redda, Karam F Soliman
Triple-negative breast cancer (TNBC) occurs at greater frequency amongst African-Americans, being characterized by the absence of estrogen receptor (ER), progesterone receptor (PR) and human epidermal receptor 2 (HER2). TNBC is often invasive and typically treated with cytostatic agents such as taxanes in combination with anthracyclines or platinum-based drugs. In this study, we synthesized a number of tetrahydroisoquinoline moieties by N-amination of substituted isoquinolines by O-mesytelene sulfonylhydroxylamine followed by ylide formation and reduction, which yielded the desired, substituted tetrahydroisoquinolines (THIQs) in moderate to good yield...
October 2016: Anticancer Research
https://www.readbyqxmd.com/read/27796444/effects-of-raloxifene-and-alendronate-on-non-enzymatic-collagen-cross-links-and-bone-strength-in-ovariectomized-rabbits-in-sequential-treatments-after-daily-human-parathyroid-hormone-1-34-administration
#13
S Kimura, M Saito, Y Kida, A Seki, Y Isaka, K Marumo
: This study investigated the effects of raloxifene and alendronate to follow parathyroid hormone (PTH) on bone collagen and biomechanical properties in ovariectomized rabbits. Sequential treatments of raloxifene and alendronate after hPTH(1-34) treatment improved biomechanical properties with and without bone collagen improvement, respectively. INTRODUCTION: The standard sequential treatment to follow human parathyroid hormone (hPTH) (1-34) therapy for osteoporosis has yet to be determined...
October 29, 2016: Osteoporosis International
https://www.readbyqxmd.com/read/27777390/-pharmacokinetics-of-selective-estrogen-receptor-modulators-serms
#14
Masakazu Terauchi
Selective estrogen receptor modulators(SERMs), or estrogen receptor agonists/antagonists(ERAAs), are a class of compounds that function as estrogen receptor(ER)agonists or antagonists tissue-dependently. Two types of SERMs are currently used in Japan to treat osteoporosis, raloxifene(RLX:Evista)and bazedoxifene(BZA:Viviant). This article describes the pharmacokinetics of these two drugs.
2016: Clinical Calcium
https://www.readbyqxmd.com/read/27771244/a-study-of-combination-bicalutamide-and-raloxifene-for-patients-with-castration-resistant-prostate-cancer
#15
Thai H Ho, Rafael Nunez-Nateras, Yue-Xian Hou, Alan H Bryce, Donald W Northfelt, Amylou C Dueck, Bryan Wong, Melissa L Stanton, Richard W Joseph, Erik P Castle
BACKGROUND: Prostate tissue expresses 2 estrogen receptor (ER) isoforms, ER-α and ER-β, and estrogen-based therapies have shown activity in preclinical studies. Raloxifene, a selective ER modulator, has inhibited the growth of prostate cancer xenograft models and was tested in a phase II trial of castration-resistant prostate cancer (CRPC), with some patients achieving stable disease. However, no studies have examined the safety of the combination of bicalutamide plus raloxifene for CRPC...
September 8, 2016: Clinical Genitourinary Cancer
https://www.readbyqxmd.com/read/27766368/anti-osteoporotic-treatments-in-france-initiation-persistence-and-switches-over-6%C3%A2-years-of-follow-up
#16
M Belhassen, C B Confavreux, B Cortet, L Lamezec, M Ginoux, E Van Ganse
: Limited information is available on anti-osteoporotic treatment initiation patterns in France. In 2006-2013, the most frequently prescribed first-line treatment class for osteoporosis was represented by bisphosphonates (alendronic acid and risedronic acid), followed by strontium ranelate. Persistence with anti-osteoporotic treatment was low, with high proportions of treatment discontinuations and switches. INTRODUCTION: This epidemiological, longitudinal study described first-line treatment initiation, persistence, switches to second-line treatment, and medical care consumption in osteoporotic patients in France during the 2007-2013 period...
October 20, 2016: Osteoporosis International
https://www.readbyqxmd.com/read/27729460/antiestrogens-structure-activity-relationships-and-use-in-breast-cancer-treatment
#17
Tatiana Traboulsi, Mohamed El Ezzy, James Gleason, Sylvie Mader
About 70% of breast tumors express estrogen receptor alpha (ERα), which mediates the proliferative effects of estrogens on breast epithelial cells, and are candidates for treatment with antiestrogens, steroidal or non-steroidal molecules designed to compete with estrogens and antagonize ERs. The variable patterns of activity of antiestrogens (AEs) in estrogen target tissues and the lack of systematic cross-resistance between different types of molecules have provided evidence for different mechanisms of action...
October 11, 2016: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/27721470/a-transgenic-mouse-model-expressing-an-er%C3%AE-folding-biosensor-reveals-the-effects-of-bisphenol-a-on-estrogen-receptor-signaling
#18
Thillai V Sekar, Kira Foygel, Tarik F Massoud, Sanjiv S Gambhir, Ramasamy Paulmurugan
Estrogen receptor-α (ERα) plays an important role in normal and abnormal physiology of the human reproductive system by interacting with the endogenous ligand estradiol (E2). However, other ligands, either analogous or dissimilar to E2, also bind to ERα. This may create unintentional activation of ER signaling in reproductive tissues that can lead to cancer development. We developed a transgenic mouse model that constitutively expresses a firefly luciferase (FLuc) split reporter complementation biosensor (NFLuc-ER-LBDG521T-CFLuc) to simultaneously evaluate the dynamics and potency of ligands that bind to ERα...
October 10, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27663804/the-role-of-selective-estrogen-receptor-modulators-in-the-treatment-of-schizophrenia
#19
Agnieszka Bratek, Krzysztof Krysta, Karolina Drzyzga, Justyna Barańska, Krzysztof Kucia
BACKGROUND: Gender differences in schizophrenia have been recognized for a long time and it has been widely accepted that sex steroid hormones, especially estradiol, are strongly attributed to this fact. Two hypotheses regarding estradiol action in psychoses gained special research attention - the estrogen protection hypothesis and hypoestrogenism hypothesis. A growing number of studies have shown benefits in augmenting antipsychotic treatment with estrogens or selective estrogen receptor modulators (SERM)...
September 2016: Psychiatria Danubina
https://www.readbyqxmd.com/read/27644075/neuroprotective-and-immunomodulatory-effects-of-raloxifene-in-the-myenteric-plexus-of-a-mouse-model-of-parkinson-s-disease
#20
Andrée-Anne Poirier, Mélissa Côté, Mélanie Bourque, Marc Morissette, Thérèse Di Paolo, Denis Soulet
Motor symptoms in Parkinson's disease (PD) are often preceded by nonmotor symptoms related to dysfunctions of the autonomic nervous system such as constipation, defecatory problems, and delayed gastric emptying. These gastrointestinal impairments are associated with the alteration of dopaminergic (DAergic) neurons in the myenteric plexus of the gut. Recently, we demonstrated the anti-inflammatory properties of estrogens to treat intestinal neurodegeneration in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of PD...
August 16, 2016: Neurobiology of Aging
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