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Raloxifene

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https://www.readbyqxmd.com/read/28523264/erratum-to-raloxifene-administration-in-women-treated-with-long-term-gonadotropin-releasing-hormone-agonist-for-severe-endometriosis-effects-on-bone-mineral-density
#1
Young Hwa Cho, Mi Jung Um, Suk Jin Kim, Soo Ah Kim, Hyuk Jung
[This corrects the article on p. 174 in vol. 22, PMID: 28119898.].
April 2017: Journal of Menopausal Medicine
https://www.readbyqxmd.com/read/28523260/combination-therapy-of-raloxifene-and-alendronate-for-treatment-of-osteoporosis-in-elderly-women
#2
Mi Jung Um, Eun A Cho, Hyuk Jung
OBJECTIVES: To evaluate and compare the efficacy and safety of the combination of raloxifene and alendronate with those of monotherapies in elderly women with osteoporosis. METHODS: Sixty-two postmenopausal women (mean age 63.5 ± 0.5 years) attending gynecologic osteoporosis clinics with established osteoporosis were randomly allocated to one of four treatment groups and monitored for 3 years. All patients enrolled in this study, including those in the control group (n = 14), received 1...
April 2017: Journal of Menopausal Medicine
https://www.readbyqxmd.com/read/28509316/effects-of-17%C3%AE-estradioland-raloxifene-on-endothelial-opg-and-rankl-secretion
#3
Wojciech Karwowski, Katarzyna Lekesiz, Ewa Koc-Żórawska, Krzysztof Wnuczko, Hanna Borysewicz-Sanczyk, Beata Naumnik
OBJECTIVES: This study aims to asses the effects of estradiol vs. raloxifene on the levels of osteoprotegerin and soluble Receptor Activator of Nuclear Factor kB Ligand (sRANKL) in Human Umbilical Vein Endothelial Cells (HUVEC) culture in standard and calcifying medium. MATERIAL AND METHODS: Human Umbilical Vein Endothelial Cells were isolated from human umbilical vein by standard method. The supernatant concentrations of osteoprotegerin (OPG) and sRANKL (ELISA) were determined after incubation with glicerophosphate, estradiol , raloxifene, glicerophoshate and estradiol, glicerophosphate and raloxifene in comparison with control group at four designated time points (0, 1, 2 and 4 days of incubation)...
2017: Ginekologia Polska
https://www.readbyqxmd.com/read/28492856/treatment-of-low-bone-density-or-osteoporosis-to-prevent-fractures-in-men-and-women-a-clinical-practice-guideline-update-from-the-american-college-of-physicians
#4
Amir Qaseem, Mary Ann Forciea, Robert M McLean, Thomas D Denberg
Description: This guideline updates the 2008 American College of Physicians (ACP) recommendations on treatment of low bone density and osteoporosis to prevent fractures in men and women. This guideline is endorsed by the American Academy of Family Physicians. Methods: The ACP Clinical Guidelines Committee based these recommendations on a systematic review of randomized controlled trials; systematic reviews; large observational studies (for adverse events); and case reports (for rare events) that were published between 2 January 2005 and 3 June 2011...
May 9, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28489426/preparation-characterization-and-in-vitro-evaluation-of-microemulsion-of-raloxifene-hydrochloride
#5
Shiva Golmohammadzadeh, Nafiseh Farhadian, Amir Biriaee, Faranak Dehghani, Bahman Khameneh
Raloxifene hydrochloride (RLX) is a selective estrogen receptor modulator which is orally used for treatment of osteoporosis and prevention of breast cancer. The drug has low aqueous solubility and bioavailability. The aim of the present study is to formulate and characterize oil-in-water microemulsion systems for oral delivery of RLX. To enhance the drug aqueous solubility, microemulsion based on sesame oil was prepared. Sesame oil and Tween 80 were selected as the drug solvent oil and surfactant, respectively...
May 10, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28449705/large-scale-detection-of-drug-off-targets-hypotheses-for-drug-repurposing-and-understanding-side-effects
#6
Matthieu Chartier, Louis-Philippe Morency, María Inés Zylber, Rafael J Najmanovich
BACKGROUND: Promiscuity in molecular interactions between small-molecules, including drugs, and proteins is widespread. Such unintended interactions can be exploited to suggest drug repurposing possibilities as well as to identify potential molecular mechanisms responsible for observed side-effects. METHODS: We perform a large-scale analysis to detect binding-site molecular interaction field similarities between the binding-sites of the primary target of 400 drugs against a dataset of 14082 cavities within 7895 different proteins representing a non-redundant dataset of all proteins with known structure...
April 28, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28439061/-calcium-and-bone-metabolism-across-women-s-life-stages-bone-quality-and-treatment-of-osteoporosis-by-serm
#7
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
#8
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...
May 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28407578/a-peek-into-the-drug-development-scenario-of-endometriosis-a-systematic-review
#9
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...
June 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
#10
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
#11
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...
May 2, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28357643/raloxifene-but-not-alendronate-can-compensate-the-impaired-osseointegration-in-osteoporotic-rats
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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