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Raloxifene

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https://www.readbyqxmd.com/read/29035723/raloxifene-reduces-the-risk-of-local-alveolar-bone-destruction-in-a-mouse-model-of-periodontitis-combined-with-systemic-postmenopausal-osteoporosis
#1
Ryota Ichimaru, Tsukasa Tominari, Shosei Yoshinouchi, Chiho Matsumoto, Kenta Watanabe, Michiko Hirata, Yukihiro Numabe, Gillian Murphy, Hideaki Nagase, Chisato Miyaura, Masaki Inada
OBJECTIVE: Periodontitis is characterized by local inflammation leading to tooth loss and severe destruction of alveolar bone. Raloxifene is a selective estrogen receptor modulator (SERM) that halts estrogen deficiency-induced systemic bone loss in postmenopausal osteoporosis without the side effects of cancer in breast and uterus. In this study, we examined the effects of raloxifene on alveolar bone mass in a mouse model with estrogen deficiency-induced periodontitis. METHODS: Periodontitis was induced by the injection of lipopolysaccharide (LPS) into the lower gingiva in ovariectomized (OVX) mice, and the alveolar bone and femur bone mineral density (BMD) were analyzed by dual-energy X-ray absorptiometry...
September 29, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/29032766/the-effects-of-drug-metabolizing-enzyme-inhibitors-on-hepatic-efflux-and-uptake-transporters
#2
Jonathan Cheong, Jason S Halladay, Jasleen K Sodhi, Emile Plise, Laurent Salphati
BACKGROUND: Non-selective chemical inhibitors of phase I and phase II enzymes are commonly used in in vitro metabolic studies to elucidate the biotransformation pathways of drugs. However, the inhibition of the inhibitors on efflux and uptake transporters is not well investigated, potentially leading to unexpected and ambiguous results in these studies. OBJECTIVE: The commonly used metabolizing enzyme inhibitors, 1-aminobenzotriazole (ABT), SKF-525A, pargyline, allopurinol, menadione, methimazole, piperine and raloxifene, were examined for their potential inhibition of the major hepatic ABC (ATP binding cassette) and SLC (solute carrier) transporters...
October 10, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29032175/the-effect-of-raloxifene-on-bone-marrow-adipose-tissue-and-bone-turnover-in-postmenopausal-women-with-osteoporosis
#3
Kerensa Beekman, Annegreet G Veldhuis-Vlug, Martin den Heijer, Mario Maas, Ania M Oleksik, Michael W Tanck, Susan M Ott, Rob J Van't Hof, Paul Lips, Peter H Bisschop, Nathalie Bravenboer
In patients with postmenopausal osteoporosis low bone volume is associated with high bone marrow adipose tissue (MAT). Moreover, high MAT is associated with increased fracture risk. This suggests an interaction between MAT and bone turnover, however literature remains equivocal. Estrogen treatment decreases MAT, but the effect of raloxifene, a selective estrogen receptor modulator (SERM) registered for treatment of postmenopausal osteoporosis, on MAT is not known. The aim of this study is 1] to determine the effect of raloxifene on MAT and 2] to determine the relationship between MAT and bone turnover in patients with osteoporosis...
October 11, 2017: Bone
https://www.readbyqxmd.com/read/29025668/sustained-raloxifene-release-from-hyaluronan-alendronate-functionalized-titanium-nanotube-arrays-capable-of-enhancing-osseointegration-in-osteoporotic-rabbits
#4
Caiyun Mu, Yan Hu, Ling Huang, Xinkun Shen, Menghuan Li, Liqi Li, Hao Gu, Yonglin Yu, Zhining Xia, Kaiyong Cai
To enhance the localized bone remodeling at titanium-based implants under osteoporotic conditions, TiO2 nanotube arrays (TNT) were used as nanoreserviors for raloxifene (Ral) and then covered with the hybrid multilayered coating of chitosan and alendronate grafted hyaluronic acid (HA-Aln) via a spin-assisted layer-by-layer technique. The fabrication of this system (TNT/Ral/LBL-Aln) was characterized by field emission scanning electron microscopy (SEM), atomic force microscope (AFM) and X-ray photoelectron spectroscopy (XPS), respectively...
January 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/29021477/management-of-osteoporosis-in-chronic-kidney-disease
#5
Kosaku Nitta, Aiji Yajima, Ken Tsuchiya
Chronic kidney disease (CKD) patients with coexisting osteoporosis are becoming common. Many of the therapeutic agents used to treat osteoporosis are known to be affected by the renal function. It is generally thought that osteoporosis in G1 to G3 CKD patients can be treated as in non-CKD patients with osteoporosis. In stage 4 or more advanced CKD patients and CKD patients on dialysis with osteoporosis, however, bisphosphonates must be used with caution, bearing in mind the potential development of such disorders as adynamic bone disease...
October 11, 2017: Internal Medicine
https://www.readbyqxmd.com/read/28978567/what-factors-influence-decision-making-about-breast-cancer-chemoprevention-among-high-risk-women
#6
EDITORIAL
Katherine D Crew
Estrogen exposure is one of the strongest risk factors for breast cancer development. Chemoprevention with selective estrogen receptor modulators (SERM), such as tamoxifen and raloxifene, has been shown in randomized controlled trials to reduce breast cancer incidence by up to 50% among high-risk women. Despite the strength of this evidence, there is significant underutilization of chemoprevention. Given the relatively few modifiable breast cancer risk factors, SERM use provides an important strategy for the primary prevention of this disease...
October 4, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28966632/effects-of-estrogen-receptor-modulators-on-cytoskeletal-proteins-in-the-central-nervous-system
#7
REVIEW
Julia J Segura-Uribe, Rodolfo Pinto-Almazán, Angélica Coyoy-Salgado, Claudia E Fuentes-Venado, Christian Guerra-Araiza
Estrogen receptor modulators are compounds of interest because of their estrogenic agonistic/antagonistic effects and tissue specificity. These compounds have many clinical applications, particularly for breast cancer treatment and osteoporosis in postmenopausal women, as well as for the treatment of climacteric symptoms. Similar to estrogens, neuroprotective effects of estrogen receptor modulators have been described in different models. However, the mechanisms of action of these compounds in the central nervous system have not been fully described...
August 2017: Neural Regeneration Research
https://www.readbyqxmd.com/read/28926415/semantic-memory-in-the-clinical-progression-of-alzheimer-disease
#8
Christophe T Tchakoute, Kristin L Sainani, Victor W Henderson
BACKGROUND AND OBJECTIVE: Semantic memory measures may be useful in tracking and predicting progression of Alzheimer disease. We investigated relationships among semantic memory tasks and their 1-year predictive value in women with Alzheimer disease. METHODS: We conducted secondary analyses of a randomized clinical trial of raloxifene in 42 women with late-onset mild-to-moderate Alzheimer disease. We assessed semantic memory with tests of oral confrontation naming, category fluency, semantic recognition and semantic naming, and semantic density in written narrative discourse...
September 2017: Cognitive and Behavioral Neurology: Official Journal of the Society for Behavioral and Cognitive Neurology
https://www.readbyqxmd.com/read/28924735/the-g-protein-coupled-estrogen-receptor-gper-gpr30-may-serve-as-a-prognostic-marker-in-early-stage-cervical-cancer
#9
Klaus Friese, Bernd Kost, Aurelia Vattai, Frederik Marmé, Christina Kuhn, Sven Mahner, Christian Dannecker, Udo Jeschke, Sabine Heublein
BACKGROUND: Estrogen signalling is transmitted via various receptors and multiple intracellular signalling pathways. Estrogen receptor alpha (ERα)-mediated transcription of target genes has been demonstrated to be closely linked to human papilloma virus (HPV)-induced carcinogenesis in case of cervical cancer. So far, the role of non-genomic estrogen signals in cervical cancer, e.g. transmitted by the G protein-coupled estrogen receptor (GPER) remains to be rather elusive. Today's knowledge on the role of GPER in cervical cancer is sparse and-to the best of our knowledge-GPER has not been investigated in context with clinicopathological parameters or prognosis of cervical cancer...
September 18, 2017: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/28921820/systematic-review-and-network-meta-analysis-on-the-relative-efficacy-of-osteoporotic-medications-men-with-prostate-cancer-on-continuous-androgen-deprivation-therapy%C3%A2-to-reduce-risk-of-fragility-fractures
#10
REVIEW
Yeesha Poon, Petros Pechlivanoglou, Shabbir M H Alibhai, David Naimark, Jeffrey S Hoch, Emmanuel Papadimitropoulos, Mary-Ellen Hogan, Murray Krahn
BACKGROUND: Androgen deprivation therapy (ADT) is an effective treatment for men with advanced prostate cancer, but loss of bone mineral density (BMD) is a major risk factor for fractures. This analysis evaluated the relative effectiveness of osteoporosis treatments using BMD as a surrogate endpoint for fragility fractures in men on continuous ADT. METHOD: We included randomized controlled trials studying bisphosphonates, denosumab, toremifene, and raloxifene in patients with non-metastatic prostate cancer on ADT for review...
September 18, 2017: BJU International
https://www.readbyqxmd.com/read/28919384/the-combination-of-gis-and-biphasic-to-better-predict-in-vivo-dissolution-of-bcs-class-iib-drugs-ketoconazole-and-raloxifene
#11
Yasuhiro Tsume, Naoto Igawa, Adam J Drelich, Gregory E Amidon, Gordon L Amidon
The formulation developments and the in vivo assessment of Biopharmaceutical Classification System (BCS) class II drugs are challenging due to their low solubility and high permeability in the human gastrointestinal (GI) tract. Since the GI environment influences the drug dissolution of BCS class II drugs, the human GI characteristics should be incorporated into the in vitro dissolution system to predict bioperformance of BCS class II drugs. An absorptive compartment may be important in dissolution apparatus for BCS class II drugs, especially for bases (BCS IIb) because of high permeability, precipitation and supersaturation...
September 14, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28894848/risk-reduction-strategies-in-breast-cancer-prevention
#12
REVIEW
Mauricio Costa, Paula Saldanha
Evaluating the risk of breast cancer makes it possible to identify women with a high risk of developing breast cancer in the future. Adopting a healthier lifestyle, involving diet and exercise, is one way of reducing this risk-but there are other, non-modifiable risk factors, such as family history, genetics and diagnosis of premalignant lesions. In this high-risk population, the tracking must be rigorous and involve the participation of the patient herself, earlier and more frequent clinical assessment, and the use of imaging screening...
July 2017: Eur J Breast Health
https://www.readbyqxmd.com/read/28859903/bazedoxifene-and-raloxifene-protect-neocortical-neurons-undergoing-hypoxia-via-targeting-er%C3%AE-and-ppar-%C3%AE
#13
J Rzemieniec, E Litwa, A Wnuk, W Lason, M Kajta
Selective estrogen receptor modulators (SERMs) such as bazedoxifene and raloxifene are recognized to mainly act via estrogen receptors (ERs), but there is no study examining the involvement of PPAR-γ in their actions, especially in neurons undergoing hypoxia. Little is also known about age-dependent actions of the SERMs on neuronal tissue challenged with hypoxia. In this study, bazedoxifene and raloxifene protected neocortical cells against hypoxia at early and later developmental stages. Both SERMs evoked caspase-3-independent neuroprotection and increased protein levels of ERα (66 and 46 kDa isoforms) and PPAR-γ...
August 28, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28837504/efficacy-and-safety-of-bazedoxifene-in-postmenopausal-latino-women-with-osteoporosis
#14
Jose A Hernández Bueno, Lizbeth Arias, Ching-Ray Yu, Robert Williams, Barry S Komm
OBJECTIVE: Bazedoxifene (BZA) reduces fractures and bone turnover in postmenopausal women with osteoporosis. This report evaluates safety and efficacy of BZA in Latin American women in the global trial. METHODS: In the 3-year, phase 3, randomized, double-blind trial, postmenopausal women with osteoporosis (N = 7,492) received BZA 20 or 40 mg/d, raloxifene 60 mg/d, or placebo. Outcomes included vertebral fractures, bone mineral density, bone turnover markers, and safety...
September 2017: Menopause: the Journal of the North American Menopause Society
https://www.readbyqxmd.com/read/28793321/effects-of-combination-treatment-with-alendronate-and-raloxifene-on-skeletal-properties-in-a-beagle-dog-model
#15
Matthew R Allen, Erin McNerny, Mohammad Aref, Jason M Organ, Christopher L Newman, Brian McGowan, Tim Jang, David B Burr, Drew M Brown, Max Hammond, Paul R Territo, Chen Lin, Scott Persohn, Lei Jiang, Amanda A Riley, Brian P McCarthy, Gary D Hutchins, Joseph M Wallace
A growing number of studies have investigated combination treatment as an approach to treat bone disease. The goal of this study was to investigate the combination of alendronate and raloxifene with a particular focus on mechanical properties. To achieve this goal we utilized a large animal model, the beagle dog, used previously by our laboratory to study both alendronate and raloxifene monotherapies. Forty-eight skeletally mature female beagles (1-2 years old) received daily oral treatment: saline vehicle (VEH), alendronate (ALN), raloxifene (RAL) or both ALN and RAL...
2017: PloS One
https://www.readbyqxmd.com/read/28770521/styrene-maleic-acid-encapsulated-raloxifene-micelles-for-management-of-inflammatory-bowel-disease
#16
Khaled Greish, Safa Taha, Anfal Jasim, Sara Abd Elghany, Ameera Sultan, Ali AlKhateeb, Manal Othman, Fang Jun, Sebastien Taurin, Moiz Bakhiet
BACKGROUND: Inflammatory bowel disease (IBD) comprises a group of disorders that manifest through chronic inflammation of the colon and small intestine. Although the exact cause of IBD is still unclear, dysfunctional immunoregulation involving overproduction of inflammatory cytokines such as TNF-α, and IL-6 have been implicated in pathogenesis. Current therapy relies on immunosuppression, cytotoxic drugs, and monoclonal antibodies against TNF-α. These classes of drugs have severe side-effects, especially when used for long duration...
December 2017: Clinical and Translational Medicine
https://www.readbyqxmd.com/read/28770019/cardioprotective-effect-of-selective-estrogen-receptor-modulator-raloxifene-are-mediated-by-heme-oxygenase-in-estrogen-deficient-rat
#17
Anikó Posa, Renáta Szabó, Krisztina Kupai, Anikó Magyariné Berkó, Médea Veszelka, Gergő Szűcs, Denise Börzsei, Mariann Gyöngyösi, Imre Pávó, Zoltán Deim, Zoltán Szilvássy, Béla Juhász, Csaba Varga
Estrogens and raloxifene (RAL) have beneficial effects on certain cardiovascular indices in postmenopausal women characterized by estrogen deficiency. Heme oxygenase (HO) activity is increased by 17β-estradiol (E2) and RAL in estrogen-deficient rat resulting in vasorelaxation mediated by carbon monoxide. We determined the expressions of HO in cardiac and aortic tissues after ovariectomy (OVX) and subsequent RAL or E2 treatment. We investigated the effects of pharmacological inhibition of HO enzyme on the arginine vasopressin- (AVP-) induced blood pressure in vivo, the epinephrine- and phentolamine-induced electrocardiogram ST segment changes in vivo, and the myeloperoxidase (MPO) enzyme activity...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28765269/the-efficacy-and-safety-of-vertebral-fracture-prevention-therapies-in-post-menopausal-osteoporosis-treatment-which-therapies-work-best-a-network-meta-analysis
#18
G Wang, L Sui, P Gai, G Li, X Qi, X Jiang
OBJECTIVES: Osteoporosis has become an increasing concern for older people as it may potentially lead to osteoporotic fractures. This study is designed to assess the efficacy and safety of ten therapies for post-menopausal women using network meta-analysis. METHODS: We conducted a systematic search in several databases, including PubMed and Embase. A random-effects model was employed and results were assessed by the odds ratio (OR) and corresponding 95% confidence intervals (CI)...
July 2017: Bone & Joint Research
https://www.readbyqxmd.com/read/28711499/inhibition-of-il-6-stat3-signaling-in-human-cancer-cells-using-evista
#19
Wei Shi, Dan Yan, Chongqiang Zhao, Miaomiao Xiao, Yina Wang, Haiyan Ma, Tianshu Liu, Hua Qin, Cuntai Zhang, Chenglong Li, Jiayuh Lin, Sheng Li, Jiagao Lv, Li Lin
Persistent activation of IL-6/STAT3 signaling pathway has been frequently detected in human cancer including breast cancer, colon cancer and multiple myeloma. IL-6/STAT3 can be a promising target for cancer prevent and treatment. However, few STAT3 inhibitors with high efficiency, specificity and safety is available for present clinical cancer therapy. Evista (Raloxifene·HCl) is known as selective estrogen receptor modulator which has been used for the prevention and treatment of osteoporosis and was approved for reducing the risk of invasive breast cancer...
September 9, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28645573/evidence-that-fetal-death-is-associated-with-placental-aging
#20
Kaushik Maiti, Zakia Sultana, Robert J Aitken, Jonathan Morris, Felicity Park, Bronwyn Andrew, Simon C Riley, Roger Smith
BACKGROUND: The risk of unexplained fetal death or stillbirth increases late in pregnancy, suggesting that placental aging is an etiological factor. Aging is associated with oxidative damage to DNA, RNA, and lipids. We hypothesized that placentas at >41 completed weeks of gestation (late-term) would show changes consistent with aging that would also be present in placentas associated with stillbirths. OBJECTIVE: We sought to determine whether placentas from late-term pregnancies and unexplained stillbirth show oxidative damage and other biochemical signs of aging...
October 2017: American Journal of Obstetrics and Gynecology
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