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https://www.readbyqxmd.com/read/29236162/bisphosphonates-prevent-age-related-weight-loss-in-japanese-postmenopausal-women
#1
Tomohiko Urano, Masataka Shiraki, Tatsuhiko Kuroda, Shiro Tanaka, Fumihiko Urano, Kazuhiro Uenishi, Satoshi Inoue
Decline of body weight with aging is a major risk factor for frailty, osteoporosis and fracture, suggesting that treatment for osteoporosis may affect body composition. Recently, we have shown that 5-year treatment with raloxifene prevented age-related weight loss, suggesting some other drugs for osteoporosis may also prevent a decrease in body weight with aging. The present study aimed to identify the relationship between bisphosphonate treatment and body composition markers. We measured bone mineral density (BMD), body composition, and bone remodeling markers in 551 Japanese postmenopausal women with bisphosphonate treatment, which included risedronate or alendronate treatment (BP-treatment group; N = 193) and without treatment by any osteoporosis drug (no-treatment group; N = 358) for 4-7 years (mean observation periods; 5...
December 13, 2017: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/29229198/combined-raloxifene-and-letrozole-for-breast-cancer-patients
#2
Divya Vohora, Abul Kalam, Ankita Leekha, Sushama Talegaonkar, Anita Kamra Verma
Raloxifene, an anti-osteoporotic drug, is recently approved for prevention of breast cancer in postmenopausal women and thus the drug may be employed to combat the bony adverse effects of letrozole, another anticancer drug. However, the cytotoxic effect of their combination on human breast cancer (MCF-7) and human embryonic kidney (HEK) cell lines is not known. MCF-7 and HEK cell lines were treated with different graded doses of letrozole, raloxifene and their combination, then incubated for 24-48 h. MTT assay was performed to check the cytotoxicity of the drugs...
December 8, 2017: Archives of Medical Research
https://www.readbyqxmd.com/read/29227547/a-network-meta-analysis-on-the-short-term-efficacy-and-adverse-events-of-different-anti-osteoporosis-drugs-for-the-treatment-of-postmenopausal-osteoporosis
#3
Gui-Feng Liu, Zong-Qiang Wang, Lin Liu, Bu-Tian Zhang, Ying-Ying Miao, Shao-Nan Yu
A network meta-analysis was conducted to compare the short-term efficacy and adverse events of different drugs for the treatment of postmenopausal osteoporosis (PMO), providing a more effective treatment for PMO. We initially searched through various databases like PubMed, Cochrane Library and EMBASE from inception till October 2016. All randomized controlled trials (RCTs) of drugs for the treatment of PMO were included for direct and indirect comparison. A combination of direct and indirect evidence of different inhibitors of antidiabetic drugs for treatment of PMO were considered for calculating the weighted mean difference (WMD) value or odd ratio (OR) value and to draw surface under the cumulative ranking (SUCRA) curves...
December 11, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29214794/retraction-paper-comparison-of-effects-of-alendronate-and-raloxifene-on-lumbar-bone-mineral-density-bone-turnover-and-lipid-metabolism-in-elderly-women-with-osteoporosis-by-iwamoto-j-et-al-yonsei-med-j-2008-49-1-119-128
#4
https://www.readbyqxmd.com/read/29210666/a-newly-synthetized-ferrocenyl-derivative-selectively-induces-apoptosis-in-all-lymphocytes-through-mitochondrial-estrogen-receptors
#5
Marjan Aghvami, Jalal Pourahmad, Afshin Zarghi, Peyman Eshghi, Mohammad Hadi Zarei, Shabnam Farzaneh, Fatemeh Sattari
BACKGROUND: Estrogens, as the main female steroid hormones have multiple proven effects on reproductive and non- reproductive systems. Expression of ERα and ERβ, two dominant estrogen receptors, in peripheral blood mononuclear cells in certain B-cell malignancies and the existence of estrogens receptors on mitochondria is open to question that estrogen likely has an impact on the cancerous lymphocytes life span. Acute lymphoblastic leukemia (ALL) is the frequent pediatric malignity which is recurrent and hardly curable in many cases...
December 5, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29199359/risk-of-venous-thromboembolism-among-users-of-different-anti-osteoporosis-drugs-a-population-based-cohort-analysis-including-over-200-000-participants-from-spain-and-the-uk
#6
E Martín-Merino, I Petersen, S Hawley, A Álvarez-Gutierrez, S Khalid, A Llorente-Garcia, A Delmestri, M K Javaid, T P Van Staa, A Judge, C Cooper, D Prieto-Alhambra
The venous thromboembolism risk among anti-osteoporotics is unknown. In this primary care study, the risk with other bisphosphonates [1.05 (0.94-1.18) and 0.96 (0.78-1.18)], strontium [0.90 (0.61-1.34) and 1.19 (0.82-1.74)], in the UK and Spain respectively, and denosumab [1.77 (0.25-12.66)] and teriparatide [1.27 (0.59-2.71)] in Spain, did not differ versus alendronate. INTRODUCTION: Most of the known adverse drug reactions described for anti-osteoporosis medication (AOM) have been described in studies comparing AOM users to non-users...
December 3, 2017: Osteoporosis International
https://www.readbyqxmd.com/read/29198613/mechanochemically-induced-solid-state-transformations-the-case-of-raloxifene-hydrochloride
#7
Yara Santiago de Oliveira, Alcemira Conceição Oliveira, Alejandro Pedro Ayala
Raloxifene hydrochloride is a benzothiophene derivative mainly used in the prevention and treatment of osteoporosis, but exhibits a low bioavailability hindered by its poor water solubility. In this study, a mechanochemical approach based on neat and liquid-assisted grinding was applied to produce new solid forms of raloxifene hydrochloride. The solids obtained were characterized by several solid-state techniques, such as powder X-ray diffraction, thermal analysis, infrared and Raman spectroscopy. These results showed that depending on the processing conditions solvated or amorphous forms can be produced...
November 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29196083/the-good-and-the-bad-about-the-2017-american-college-of-physicians-osteoporosis-guidelines
#8
Violet Lagari, Tara Gavcovich, Silvina Levis
PURPOSE: The American College of Physicians (ACP) published a set of guidelines on how to prevent fractures in men and women with low bone density or osteoporosis. As the population ages, the overall risk of fractures increases, thus burdening the health care system. These guidelines review current evidence for osteoporosis management, providing an update to the previous 2008 ACP's guidelines. METHODS: The ACP put forth 6 recommendations addressing the complexities in osteoporosis management based on evidence available through October 2016 with a focus on bisphosphonates, calcium, vitamin D, and estrogen...
November 28, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/29196024/poly-methyl-vinyl-ether-co-maleic-acid-for-enhancement-of-solubility-oral-bioavailability-and-anti-osteoporotic-effects-of-raloxifene-hydrochloride
#9
J Varshosaz, Mohsen Minayian, Ladan Dayyani
Raloxifene HCl (RH) has poor water solubility and due to its extensive first pass metabolism; its bioavailability is only 2%. The purpose of the present study was to enhance the aqueous solubility, oral bioavailability and anti-osteoporotic effects of RH by electro-sprayed nanoparticles (NPs) in ovariectomized rats. NPs containing RH and different ratio of poly(methyl vinyl ether-co-maleic acid) (PMVEMA) were electrosprayed. The voltage, distance of needle to the collector, flow rate of the solution and polymeric percentage were optimized according to the size of NPs and drug solubility...
November 28, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29194351/identification-of-a-raloxifene-analog-that-promotes-ahr-mediated-apoptosis-in-cancer-cells
#10
Hyo Sang Jang, Martin Pearce, Edmond F O'Donnell, Bach Duc Nguyen, Lisa Truong, Monica J Mueller, William H Bisson, Nancy I Kerkvliet, Robert L Tanguay, Siva Kumar Kolluri
We previously reported that raloxifene, an estrogen receptor modulator, is also a ligand for the aryl hydrocarbon receptor (AhR). Raloxifene induces apoptosis in estrogen receptor-negative human cancer cells through the AhR. We performed structure-activity studies with seven raloxifene analogs to better understand the structural requirements of raloxifene for induction of AhR-mediated transcriptional activity and apoptosis. We identified Y134 as a raloxifene analog that activates AhR-mediated transcriptional activity and induces apoptosis in MDA-MB-231 human triple negative breast cancer cells...
December 1, 2017: Biology
https://www.readbyqxmd.com/read/29181706/self-assembling-raloxifene-loaded-mixed-micelles-formulation-optimization-in-vitro-cytotoxicity-and-in-vivo-pharmacokinetics
#11
Radhika Kanade, Mithila Boche, Varsha Pokharkar
Raloxifene (RLX) has been strongly recommended for postmenopausal women at high risk of invasive breast cancer and for prevention of osteoporosis. However, low aqueous solubility and reduced bioavailability hinder its clinical application. The objective of this study was to explore the potential of RLX loaded mixed micelles (RLX-MM) using Pluronic F68 and Gelucire 44/14 for enhanced bioavailability and improved anticancer activity on human breast cancer cell line (MCF-7). RLX-MM were prepared by solvent evaporation method and optimized using 32 factorial design...
November 27, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29180905/effects-of-minodronate-in-postmenopausal-women-with-osteoporosis-who-received-prior-treatment-with-raloxifene
#12
Aska Toda, Kenjiro Sawada, Akihiko Yoshimura, Erika Nakatsuka, Hiromasa Kuroda, Katsumi Kozasa, Mayuko Miyamoto, Kae Hashimoto, Seiji Mabuchi, Tadashi Kimura
Background: In clinical practice, patients with postmenopausal osteoporosis have often shown a poor response to treatment with an antiresorptive agent for several years. The purpose of this study was to investigate the efficacy of switching raloxifene with minodronate in patients who responded poorly to the treatment of postmenopausal osteoporosis with raloxifene. Patients and methods: This observational study was conducted based on a single-arm, non-randomized, open-label design and was approved by the institute's institutional review board...
2017: International Journal of Women's Health
https://www.readbyqxmd.com/read/29177974/antitumor-activity-of-raloxifene-targeted-poly-styrene-maleic-acid-poly-amide-ether-ester-imide-co-polymeric-nanomicelles-loaded-with-docetaxel-in-breast-cancer-bearing-mice
#13
Saeede Enteshari, Jaleh Varshosaz, Mohsen Minayian, Farshid Hassanzadeh
Purpose Raloxifene (RA) receptors have over-expressed GPER-positive breast cancer tumors. The purpose of this work was to evaluate the antitumor activity and pharmacokinetic behavior of docetaxel (DTX), loaded in RA-targeted nanomicelles, which were designed to overcome a lack of specific distribution and inadequate DTX concentration in tumor tissues, as well as its cytotoxicity and damage to normal tissues. Methods DTX-loaded RA-targeted poly(styrene maleic acid) (SMA)- poly(amide-ether-esterimide)-poly(ethylene glycol) (PAEEI-PEG) nanomicelles were prepared; then, their antitumor activity and survival rate were studied in MC4-L2 tumors induced in BALB/c mice...
November 27, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/29168671/oral-bioavailability-enhancement-of-raloxifene-by-developing-microemulsion-using-d-optimal-mixture-design-optimization-and-in-vivo-pharmacokinetic-study
#14
Nirmal Shah, Avinashkumar Seth, R Balaraman, Girish Sailor, Ankur Javia, Dipti Gohil
The objective of present work was to utilize a potential of microemulsion for the improvement in oral bioavailability of raloxifene hydrochloride, a BCS class-II drug with 2% bioavailability. Drug loaded microemulsion was prepared by water titration method using Capmul MCM C8, Tween 20 and Polyethylene glycol 400 as oil, surfactant and co-surfactant respectively. The pseudo-ternary phase diagram was constructed between oil and surfactants mixture to obtain appropriate components and their concentration ranges that result in large existence area of microemulsion...
November 23, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29164806/enhanced-cytotoxicity-and-apoptosis-by-raloxifene-in-combination-with-estrogen-and-methotrexate-in-human-endometrial-stromal-thesc-cells
#15
Ivana Nikolic, Marija Andjelkovic, Milan Zaric, Ivanka Zelen, Zoran Milosavljevic, Petar Canovic, Marina Mitrovic
Endometrial hyperplasia is a condition that may lead to the development of endometrial carcinoma. Initially, changes of the endometrium are caused by the estrogen's hyperstimulation that may lead to the development of an irregular bleeding and the infertility problems. Therapy of endometrial hyperplasia's is limited to medical and surgical approaches. During the past decade, the new types of drugs were developed for the treatment of the endometrial hyperplasia. Here, for the first time, we investigated the cytotoxic effects of the various combinations of estrogen, raloxifene and methotrexate in human ThESC cell line as a possible potential treatment of the endometrial hyperplasia...
November 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29098120/effects-of-atrial-natriuretic-peptide-on-p53-and-estrogen-receptor-in-breast-cancer-cells
#16
Katie Aleck, Kelly Hallman, Meghan Quigley, Victoria Lloyd, Monica Szmyd, Dana Ruskin, Tyler Bedgood, Sumi Dinda
The atrial natriuretic peptide (ANP) hormone is secreted by cardiac atrial myocytes and acts to regulate blood pressure homeostasis in humans. Previous research indicates ANP treatment significantly decreases the proliferation of human prostate cancer cells, pancreatic adenocarcinoma, and breast cancer cells. Minimal studies have been conducted with regard to ANP regulating tumor suppressor genes and steroid hormone receptors in breast cancer cells. Our study analyzed the effects of ANP in combination with 17β-estradiol (E2) and antiestrogen treatments on p53 and ERα levels in T-47D breast cancer cells...
2017: BioResearch Open Access
https://www.readbyqxmd.com/read/29097444/razor-a-phase-ii-open-randomized-trial-of-screening-plus-goserelin-and-raloxifene-versus-screening-alone-in-pre-menopausal-women-at-increased-risk-of-breast-cancer
#17
Anthony Howell, Linda Ashcroft, Lesley Fallowfield, Diana M Eccles, Rosalind A Eeles, Ann Ward, Adam R Brentnall, Mitchell Dowsett, Jack M Cuzick, Rosemary Greenhalgh, Caroline Boggis, Jamie Motion, Jamie C Sergeant, Judith Adams, D Gareth R Evans
BACKGROUND: Ovarian suppression in premenopausal women is known to reduce breast cancer risk. This study aimed to assess uptake and compliance with ovarian suppression using the LHRH analogue, goserelin, with add-back raloxifene, as a potential regimen for breast cancer prevention. METHODS: Women at ≥30% lifetime risk breast cancer were approached and randomized to mammographic screening alone(C-Control) or screening in addition to monthly subcutaneous injections of 3...
November 2, 2017: Cancer Epidemiology, Biomarkers & Prevention
https://www.readbyqxmd.com/read/29089563/effects-of-strength-training-and-raloxifene-on-femoral-neck-metabolism-and-microarchitecture-of-aging-female-wistar-rats
#18
Camila Tami Stringhetta-Garcia, Samuel Rodrigues Lourenço Morais, Fernanda Fernandes, Melise Jacon Perez-Ueno, Ricardo de Paula Almeida, Mário Jefferson Quirino Louzada, Antonio Hernandes Chaves-Neto, Edilson Ervolino, Rita Cássia Menegati Dornelles
The aim of this study was to prevent female osteoporosis using strength training (ST), raloxifene (Ral) or a combination of ST plus Ral during the natural female aging process, specifically in the periestropause period. For a total of 120 days, aging female Wistar rats at 18-21 months of age performed ST on a ladder three times per week, and Ral was administered daily by gavage (1 mg/kg/day). Bone microarchitecture, areal bone mineral density, bone strength of the femoral neck, immunohistochemistry, osteoclast and osteoblast surface were assessed...
October 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29083977/examining-the-effect-of-medication-adherence-on-risk-of-subsequent-fracture-among-women-with-a-fragility-fracture-in-the-u-s-medicare-population
#19
Allison Keshishian, Natalie Boytsov, Russel Burge, Kelly Krohn, Louise Lombard, Xiang Zhang, Lin Xie, Onur Baser
BACKGROUND: In the United States, osteoporosis affects approximately 10 million people, of whom 80% are women, and it contributes a significant clinical burden to the community. Poor adherence to osteoporosis medications adds to the overall burden of illness. OBJECTIVE: To examine the association of osteoporosis medication adherence and the risk of a subsequent fracture among Medicare-enrolled women with a previous fragility fracture. METHODS: This study was a retrospective observational analysis of U...
November 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/29081020/a-model-of-fracture-risk-used-to-examine-the-link-between-bone-mineral-density-and-the-impact-of-different-therapeutic-mechanisms-on-fracture-outcomes-in-patients-with-osteoporosis
#20
Rena J Eudy-Byrne, William Gillespie, Matthew M Riggs, Marc R Gastonguay
A hazard model of fracture was developed using individual patient data (IPD) from the NHANES (2005-2008) database and summary-level data from an aggregate dataset (AD). The AD was built by performing a comprehensive and systematic literature search of clinical studies published from 1995 to 2015, recording fracture rate and bone mineral density (BMD) for both treatment and placebo arms. The search resulted in a metadata set comprised of 21 studies investigating the effects of various bisphosphonates, teriparatide, denosumab, and raloxifene in 65,254 patients over a cumulative 56...
December 2017: Journal of Pharmacokinetics and Pharmacodynamics
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