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https://www.readbyqxmd.com/read/28439061/-calcium-and-bone-metabolism-across-women-s-life-stages-bone-quality-and-treatment-of-osteoporosis-by-serm
#1
Mitsuru Saito, Keishi Marumo
Estrogen deficiency induces bone resorption and bone collagen crosslink abnormalities such as reductions in enzymatic cross-links and accumulation of Advanced glycation end products(AGEs). In this review, we described that the mechanism of poor bone quality in estrogen deficiency and how selective estrogen receptor modulators such as raloxifene and bazedoxifene improve bone structural and material properties.
2017: Clinical Calcium
https://www.readbyqxmd.com/read/28430601/growth-suppressive-activity-of-raloxifene-on-liver-cancer-cells-by-targeting-il-6-gp130-signaling
#2
Yina Wang, Haiyan Ma, Chongqiang Zhao, Tianshu Liu, Dan Yan, David Jou, Huameng Li, Cuntai Zhang, Jiagao Lü, Chenglong Li, Jiayuh Lin, Sheng Li, Li Lin
BACKGROUND: Interleukin-6 (IL-6) is a multifunctional cytokine, which is involved in the regulation of differentiation and growth of certain types of tumor cells. Constitutive activation of Signal Transducer and Activator of Transcription 3 (STAT3) induced by IL-6 is frequently detected in liver cancer and has emerged as a viable molecular target for liver cancer treatment. However, few inhibitors targeting up-streams of STAT3 are available for the therapy of liver cancer. We reported the discovery of EVISTA (Raloxifene HCl) as novel inhibitor of IL-6/GP130 protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning...
April 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28407578/a-peek-into-the-drug-development-scenario-of-endometriosis-a-systematic-review
#3
REVIEW
Luxitaa Goenka, Melvin George, Maitrayee Sen
PURPOSE AND OBJECTIVE: Endometriosis is a gynaecological disease that is characterised by the presence of endometrium like tissue-epithelium and stroma that develops outside the uterine cavity, which is responsible for pelvic pain and infertility. Even though several medical therapies exist for the treatment of endometriosis, each of the drug class has its own limitations such as cost of treatment, side-effects and its short-term effect on the symptoms of endometriosis. In this review, we have attempted to summarize the current status and challenges of drug development for endometriosis...
April 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28396978/a-novel-strategy-to-co-target-estrogen-receptor-and-nuclear-factor-%C3%AE%C2%BAb-pathways-with-hybrid-drugs-for-breast-cancer-therapy
#4
Irida Kastrati, Marton I Siklos, Svitlana D Brovkovych, Gregory R J Thatcher, Jonna Frasor
Nearly 75% of breast tumors express estrogen receptor (ER), and will be treated with endocrine therapy, such as selective estrogen receptor modulator (SERM), tamoxifen, or aromatase inhibitors. Despite their proven success, as many as 40-50% of ER+ tumors fail to respond to endocrine therapy and eventually recur as aggressive, metastatic cancers. Therefore, preventing and/or overcoming endocrine resistance in ER+ tumors remains a major clinical challenge. Deregulation or activation of the nuclear factor κB (NFκB) pathway has been implicated in endocrine resistance and poor patient outcome in ER+ tumors...
April 10, 2017: Hormones & Cancer
https://www.readbyqxmd.com/read/28395318/benefits-and-harms-of-osteoporosis-medications-in-patients-with-chronic-kidney-disease-a-systematic-review-and-meta-analysis
#5
Lisa M Wilson, Casey M Rebholz, Ermias Jirru, Marisa Chi Liu, Allen Zhang, Jessica Gayleard, Yue Chu, Karen A Robinson
Background: Complications of chronic kidney disease (CKD) include weak bones and increased fracture risk. Purpose: To review the benefits and harms of osteoporosis medications (bisphosphonates, teriparatide, raloxifene, and denosumab) compared with placebo, usual care, or active control in terms of bone mineral density (BMD), fractures, and safety in patients with CKD. Data Sources: PubMed and the Cochrane Central Register of Controlled Trials from December 2006 through December 2016...
April 11, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28357643/raloxifene-but-not-alendronate-can-compensate-the-impaired-osseointegration-in-osteoporotic-rats
#6
Leonardo Perez Faverani, Tárik Ocon Braga Polo, Gabriel Ramalho-Ferreira, Gustavo Antonio Correa Momesso, Jaqueline Suemi Hassumi, Ana Cláudia Rossi, Alexandre Rodrigues Freire, Felippe Bevilacqua Prado, Eloá Rodrigues Luvizuto, Reinhard Gruber, Roberta Okamoto
OBJECTIVES: Alendronate and raloxifene, a bisphosphonate and a selective estrogen modulator, respectively, are established osteoporosis therapies. Current evidence suggests that simultaneous application of osteoporosis therapies modulates osseointegration. However, alendronate shows inconsistent findings and raloxifene has not been studied comprehensively. This study aimed to evaluate the bone dynamics and molecular and microstructural features at the peri-implant bone interface in osteoporotic rats...
March 29, 2017: Clinical Oral Investigations
https://www.readbyqxmd.com/read/28351480/melasma-treatment-a-novel-approach-using-a-topical-agent-that-contains-an-anti-estrogen-and-a-vascular-endothelial-growth-factor-inhibitor
#7
Philip R Cohen
Melasma is an acquired disorder of pigmentation that presents with asymptomatic symmetric darkening of the face. The pathogenesis of this condition is multifactorial and influenced by several factors including female sex hormones, genetic predisposition and ultraviolet light exposure. The management of melasma is usually directed at more than one of the causative etiologic factors and often incorporates a combination of topical agents, with or without the addition of physical modalities. Estrogen and angiogenesis are significant factors in the etiology of melasma...
April 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/28350760/involvement-of-hsp70-and-ho-1-in-the-protective-effects-of-raloxifene-on-multiple-organ-dysfunction-syndrome-by-endotoxemia-in-ovariectomized-rats
#8
Hsin-Hsueh Shen, Shieh-Yang Huang, Pao-Yun Cheng, Yen-Ju Chu, Shu-Ying Chen, Kwok-Keung Lam, Yen-Mei Lee
OBJECTIVE: Accumulating evidence demonstrates that raloxifene, a selective estrogen receptor modulator, possesses anti-inflammatory action. This study evaluates the preventive effects of long-term treatment of raloxifene on acute inflammation and multiple organ dysfunction syndrome (MODS) in ovariectomized (OVX) rats with endotoxemia and its underlying mechanism of action. METHODS: Adult female rats were OVX bilaterally to induce estrogen insufficiency. OVX rats were administered with raloxifene (1 mg/kg, gavage, once daily) for 8 weeks, beginning 1 week after surgery, followed by induction of sepsis via intravenous infusion of lipopolysaccharides (LPS; 30 mg/kg) for 4 hours...
March 27, 2017: Menopause: the Journal of the North American Menopause Society
https://www.readbyqxmd.com/read/28334925/simultaneous-lc-ms-ms-determination-of-lopinavir-and-rifabutin-in-human-plasma
#9
Swati Jaiswal, Abhisheak Sharma, Mahendra Shukla, Jawahar Lal
Tuberculosis (TB) with human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome represents the most common infectious diseases worldwide. Anti-TB drugs are used concurrently with antiretroviral drug for treatment of TB-HIV co-morbidities. Due to lower risk of interaction with protease inhibitors, rifabutin is preferred over rifampicin in treatment of HIV and TB co-morbidity. A simple and specific liquid chromatography tandem mass spectrometry method was developed for quantification of rifabutin (RBT) and lopinavir (LPV) simultaneously in human plasma...
March 3, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28293779/effect-of-osteoporosis-medication-on-changes-in-bone-mineral-density-and-bone-turnover-markers-after-24-month-administration-of-daily-teriparatide-comparison-among-minodronate-raloxifene-and-eldecalcitol
#10
Shinichi Nakatoh
This study reveals the changes in bone mineral density (BMD), the turnover rate, and the balance [multiple of median formation/multiple of median resorption (MoMf/MoMr)] affected by the selection of different bone resorption inhibitors after 24-month daily teriparatide (20 µg/day) administration. The turnover rate was calculated as √(MoMf(2) + MoMr(2)), where MoMf = bone-specific alkaline phosphatase (BAP) value/18.6 and MoMr = tartrate-resistant acid phosphatase 5b (TRACP-5b) value/463. One hundred and twenty-one osteoporotic women (mean age 82...
March 14, 2017: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/28283467/responsiveness-of-brca1-and-trp53-deficiency-induced-mammary-preneoplasia-to-selective-estrogen-modulators-versus-an-aromatase-inhibitor-in-mus-musculus
#11
Sahar J Alothman, Weisheng Wang, David S Goerlitz, Md Islam, Xiaogang Zhong, Archana Kishore, Redha I Azhar, Bhaskar V Kallakury, Priscilla A Furth
An intervention study initiated at age 4 months compared the impact of tamoxifen (25 mg), raloxifene (22.5 mg), and letrozole (2.5 mg) administered by 60-day release subcutaneous pellet on mammary preneoplasia prevalence at age 6 months in conditional genetically engineered mouse models with different Breast cancer 1 (Brca1) gene dosages targeted to mammary epithelial cells and germline Tumor protein P53 (Trp53) haploinsufficiency (10-16/cohort). The proportion of unexposed control mice demonstrating mammary preneoplasia at age 6 months was highest in Brca1(fl11/fl11/Cre/p53-/+) (54%) mice followed by Brca1(WT/fl11/Cre/p53-/+) mice (30%)...
April 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28265881/raloxifene-lowers-plasma-lipoprotein-a-concentrations-a-systematic-review-and-meta-analysis-of-randomized-placebo-controlled-trials
#12
Gianna Ferretti, Tiziana Bacchetti, Luis E Simental-Mendía, Željko Reiner, Maciej Banach, Amirhossein Sahebkar
BACKGROUND AND AIMS: Lipoprotein(a) (Lp(a)) is a proatherogenic plasma lipoprotein and an independent risk factor for atherosclerotic cardiovascular disease. We investigated the effects of raloxifene, selective estrogen receptor modulator, on circulating Lp(a) levels in postmenopausal women using a systematic review and meta-analysis of randomized controlled trials (RCTs). METHODS: To identify relevant studies, electronic databases (PUBMED, Scopus, Web of Science, and Google Scholar) were searched by up to May 2015 to find controlled trials exploring the effects of oral raloxifene treatment on plasma Lp(a) levels in postmenopausal women...
March 7, 2017: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/28261281/induction-of-mitochondrial-apoptotic-pathway-by-raloxifene-and-estrogen-in-human-endometrial-stromal-thesc-cell-line
#13
Ivana Nikolic, Marija Andjelkovic, Milan Zaric, Ivanka Zelen, Petar Canovic, Zoran Milosavljevic, Marina Mitrovic
INTRODUCTION: Endometrial hyperplasia is a condition that occurs as a result of hormonal imbalance between estrogen and progesterone. Morphological disturbance of endometrial cells occurs consequently leading towards endometrial cancer. In therapy of endometrial hyperplasia SERMs are used to supress effects of locally high estrogen level in uterus. There is strong evidence suggesting that estrogen could be involved in cell death - apoptosis. There are no experimental data demstrating the direct apoptotic effect of both raloxifene and estrogen on the ThESC cell line...
March 1, 2017: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/28246928/raloxifene-improves-bone-mechanical-properties-in-mice-previously-treated-with-zoledronate
#14
Cory N Meixner, Mohammad W Aref, Aryaman Gupta, Erin M B McNerny, Drew Brown, Joseph M Wallace, Matthew R Allen
Bisphosphonates represent the gold-standard pharmaceutical agent for reducing fracture risk. Long-term treatment with bisphosphonates can result in tissue brittleness which in rare clinical cases manifests as atypical femoral fracture. Although this has led to an increasing call for bisphosphonate cessation, few studies have investigated therapeutic options for follow-up treatment. The goal of this study was to test the hypothesis that treatment with raloxifene, a drug that has cell-independent effects on bone mechanical material properties, could reverse the compromised mechanical properties that occur following zoledronate treatment...
February 28, 2017: Calcified Tissue International
https://www.readbyqxmd.com/read/28246081/the-4ps-of-breast-cancer-chemoprevention-putting-proven-principles-into-practice
#15
EDITORIAL
V Craig Jordan
The pioneering Royal Marsden Tamoxifen Prevention Trial recruited 2,471 eligible high-risk women to be randomized to either placebo or tamoxifen (20 mg daily) for 8 years. Breast cancer incidence was evaluated at a median of 18.4 years from the start of the study. There was a 32% reduction in estrogen/progesterone receptor (ER/PR)-positive breast cancers after tamoxifen treatment finished. Translational research, to study "the good, the bad, and the ugly of tamoxifen" in the 1980s, subsequently ensured women's safety from possible increases in osteoperosis, coronary heart disease, and endometrial cancer...
April 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28243883/two-year-persistence-and-compliance-with-osteoporosis-therapies-among-postmenopausal-women-in-a-commercially-insured-population-in-the-united-states
#16
Emily Durden, Lionel Pinto, Lorena Lopez-Gonzalez, Paul Juneau, Richard Barron
This retrospective, observational study assessed 2-year persistence and compliance by treatment, route of administration, and dosing frequency in postmenopausal women initiating a new osteoporosis therapy. Two-year persistence and compliance rates were higher in women receiving injectables compared with oral agents. PURPOSE: This study extends previous studies limited to 1-year follow-up by examining persistence with osteoporosis therapies over a 2-year period and compares short- and long-term trends in persistence and compliance among postmenopausal women with commercial or Medicare supplemental insurance in the USA...
December 2017: Archives of Osteoporosis
https://www.readbyqxmd.com/read/28239652/estrogens-regulate-glycosylation-of-igg-in-women-and-men
#17
Altan Ercan, Wendy M Kohrt, Jing Cui, Kevin D Deane, Marija Pezer, Elaine W Yu, Jonathan S Hausmann, Harry Campbell, Ursula B Kaiser, Pauline M Rudd, Gordan Lauc, James F Wilson, Joel S Finkelstein, Peter A Nigrovic
The immunologic potency of IgG is modulated by glycosylation, but mechanisms regulating this process are undefined. A role for sex hormones is suggested by differences in IgG glycans between women and men, most prominently with respect to galactose. We therefore assessed IgG galactosylation in 713 healthy adults from 2 cohorts as well as in 159 subjects from 4 randomized controlled studies of endocrine manipulation: postmenopausal women receiving conjugated estrogens, raloxifene, or placebo; premenopausal women deprived of gonadal hormones with leuprolide and treated with estradiol or placebo; men deprived of gonadal hormones with goserelin and given testosterone or placebo; and men deprived of gonadal hormones with goserelin and given testosterone or placebo together with anastrozole to block conversion of testosterone to estradiol...
February 23, 2017: JCI Insight
https://www.readbyqxmd.com/read/28238769/effects-of-raloxifene-on-portal-hypertension-and-hepatic-encephalopathy-in-cirrhotic-rats
#18
Ching-Chih Chang, Wen-Shin Lee, Chiao-Lin Chuang, I-Fang Hsin, Shao-Jung Hsu, Ting Chang, Hui-Chun Huang, Fa-Yauh Lee, Shou-Dong Lee
Raloxifene, a selective estrogen receptor modulator, has been used extensively for osteoporosis. In addition to the effect of osteoporosis treatment, emerging evidences show that raloxifene affects the vascular function in different tissues. Cirrhosis is characterized with portal hypertension and complicated with hepatic encephalopathy. Portal hypertension affects portal-systemic shunt which leads to hepatic encephalopathy that the vascular modulation might influence severity of hepatic encephalopathy. Herein, we evaluated the impact of raloxifene on bile duct ligation (BDL)-induced cirrhotic rats...
February 24, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28224392/investigation-of-need-of-natural-bioenhancer-for-a-metabolism-susceptible-drug-raloxifene-in-a-designed-self-emulsifying-drug-delivery-system
#19
Poonam Singh Thakur, Narinder Singh, Abhay T Sangamwar, Arvind Kumar Bansal
Bioenhancers can increase the bioavailability of metabolism susceptible drugs. The present study was designed to understand the impact of bioenhancer on permeability and bioavailability of a biopharmaceutical drug disposition classification system (BDDCS) class II drug raloxifene (RLX). RLX undergoes extensive first pass metabolism by UGT enzymes in gastrointestinal tract (GIT) and has an oral bioavailability of about 2%. Self-emulsifying drug delivery system (SEDDS) of RLX was developed using a designed approach and this formulation was loaded with reported bioenhancers: quercetin and piperine...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28185712/the-effect-of-selective-estrogen-receptor-modulators-on-type-2-diabetes-onset-in-women-basic-and-clinical-insights
#20
REVIEW
Beibei Xu, Dragana Lovre, Franck Mauvais-Jarvis
Selective estrogen receptor modulators (SERMs) are a class of compounds that interact with estrogen receptors (ERs) and exert agonist or antagonist effects on ERs in a tissue-specific manner. Tamoxifen, a first generation SERM, is used for treatment of ER positive breast cancer. Raloxifene, a second generation SERM, was used to prevent postmenopausal osteoporosis. The third-generation SERM bazedoxifene (BZA) effectively prevents osteoporosis while preventing estrogenic stimulation of breast and uterus. Notably, BZA combined with conjugated estrogens (CE) is a new menopausal treatment...
April 2017: Journal of Diabetes and its Complications
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